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Objective To explore the clinical curative effect of Pingchuan prescription combined with montelukast sodium on patients with bronchial asthma. Methods A total of 102 patients with bronchial asthma admitted to the hospital were enrolled between May 2022 and December 2023. According to simple randomization method, they were divided into control 1 group (montelukast sodium, n=34), control 2 group (Pingchuan prescription, n=34) and observation group (Pingchuan prescription combined with montelukast sodium, n=51). All patients were treated for 21 d. The clinical curative effect in the three groups was evaluated. The scores of TCM syndromes, inflammatory factors [interleukin (IL)-4, IL-17, interferon (IFN)-γ, transforming growth factor-β1 (TGF-β1), immunoglobulin (Ig)E] and scores of the test for respiratory and asthma control in kids (TRACK) in the three groups were compared before and after treatment. The adverse reactions were recorded. Results Compared with control 1 group and control 2 group, total response rate was higher in observation group (P<0.05). After treatment, scores of TCM syndromes (wheezing due to phlegm in throat, tachypnea, choking)in observation group were lower than those in control 1 group and control 2 group (P<0.05). After treatment, levels of IL-4, IL-17, TGF-β1 and IgE in observation group were lower than those in control 1 group and control 2 group, while IFN-γ level and TRACK score were higher than those in control 1 group and control 2 group (P<0.05). There was no difference in adverse reactions among the three groups (P>0.05). Conclusion Pingchuan prescription combined with montelukast sodium could improve clinical curative effect in patients with bronchial asthma, which was beneficial to alleviate inflammatory response and disease severity, with certain safety. [ABSTRACT FROM AUTHOR]

The development of sustainable analytical methodologies that minimize hazards, waste generation, and energy consumption has become crucial. This study introduces pioneering green‒blue-white approaches for the simultaneous quantification of montelukast sodium (MLK) and fexofenadine hydrochloride (FEX) in combination formulations. The first approach employs an ultra-performance liquid chromatographic method (UPLC) with a green micellar mobile phase of 0.02 M sodium dodecyl sulfate and 10% 1-pentanol (65:35%). The method demonstrated excellent resolution, peak symmetry, and a short analysis time, with retention times of 3.53 min for MLK and 1.67 min for FEX. The MLK and FEX linearities were 1–260 and 1.2–312 μg/mL, respectively. The second approach involves complementary built-in spectroscopic techniques (second derivative, third derivative, and ratio difference methods) using water as a solvent, providing a green, simple, low-cost alternative in laboratories where expensive chromatographic devices may not be readily available. The MLK and FEX linearities were 3–50 and 3–60 μg/mL, respectively. All methods were comprehensively validated and showed satisfactory results. The proposed methods demonstrated excellent linearity (r2 ≥ 0.9990), accuracy (recovery 98.5–101.5%), and precision (RSD ≤ 2%) across wide concentration ranges. A multifaceted evaluation was conducted to assess the environmental sustainability, real-world applicability, and economic viability of the proposed methods in comparison with previously reported techniques. This comprehensive assessment leveraged several state-of-the-art tools, including NEMI, ComplexGAPI, AGREE, ESA, BAGI, and RGB12. The suggested approaches exhibited favorable quadrant profiles in the NEMI and ComplexGAPI assessments, coupled with higher AGREE scores (0.90, 0.86) than reported (0.62, 0.74, 0.75, 0.69, 0.74, 0.74, and 0.75), in addition to higher ESA score (88, 92) than reported (75, 84, 85, 79, 82, 82, and 83), collectively affirming their environmentally friendly credentials. Moreover, we embraced the innovative notions of 'blueness' and 'whiteness' assessment by harnessing the recently formulated BAGI and RGB12 algorithms. The higher BAGI score (90, 82.5) than reported (72.5, 70, 70, 67.5, 67.5, 67.5, and 72.5), confirmed the excellent real-world applicability of the proposed methods, while the notable RGB12 indices (89.8, 88.1) than reported (67.8, 72.8, 71.5, 67.1, 73.7, 70.3, and 73.2), validated their cost-effectiveness and overall sustainability, contributing to an eco-friendly future for quality control processes. [ABSTRACT FROM AUTHOR]

A simple, accurate and economical UV spectroscopic method has been developed for the simultaneous estimation of olopatadine hydrochloride and montelukast sodium. The developed method is based on the determination of the two drugs using UV absorbance correction principle. The wavelengths chosen for analysis were 352 nm for montelukast sodium (as absorbance due to the other drug was nil at this wavelength) and 298.5 nm for olopatadine hydrochloride (corrected for absorbance due to montelukast sodium) with water as diluent. The Beer-Lambert's range for the two drugs was found to be 2-100 μg mL-1 at 298.5 nm and 2-70 μg mL-1 at 352 nm for montelukast sodium with r2 of ≥ 0.990. The developed method was validated as per ICH guidelines and the percentage assay results were within acceptable limits. The developed method can thus be successfully used for the regular analysis of olopatadine hydrochloride and montelukast sodium in bulk and in combination. [ABSTRACT FROM AUTHOR]

For the treatment of rhinitis and asthma, a combination of Montelukast sodium and Bilastine has just been approved. Based on the first derivative of synchronous fluorescence, the current work developed a green, highly accurate, sensitive, and selective spectroscopic approach for estimating Montelukast sodium and Bilastine in pharmaceutical dosage form without previous separation. The selected technique focuses on measuring the synchronized fluorescence of the studied medications at a fixed wavelength range (Δλ) = 110 nm, and using the amplitude of the first derivative's peak at 381 and 324 nm, for quantitative estimation of Montelukast sodium and Bilastine, respectively. The impacts of different factors on the referred drugs' synchronized fluorescence intensity were investigated and adjusted. The calibration plots for were found to be linear over concentration ranges of 50–2000 ng mL−1 for Montelukast sodium and 50–1000 ng mL−1 for Bilastine. Montelukast sodium and Bilastine have LODs of 16.5 and 10.9 ng mL−1, respectively. In addition, LOQs were: 49.9 and 33.0 ng mL−1, for both drugs, respectively. The developed method was successfully employed to quantify the two drugs in synthetic tablets mixture and in laboratory prepared mixtures containing varied Montelukast and Bilastine ratios. To compare the results with the published analytical approach, a variance ratio F-test and a student t-test were used, which revealed no significant differences. [ABSTRACT FROM AUTHOR]

Background: Since inflammatory mediators play a crucial role in the pathophysiology of neonatal sepsis. Montelukast, as an anti-inflammatory drug, could be a beneficial therapy. In searching the literature, no previous research addressed the role of Montelukast in neonatal sepsis; hence, this study aimed to explore the adjuvant role of Montelukast in regulating the inflammatory response associated with neonatal sepsis and its associated effect on the clinical outcomes. Methods: An open-label, randomized controlled intervention trial conducted on 40 late preterm newborn infants (gestational age 340/7 to 366/7 weeks) admitted to NICU, with clinical evidence of sepsis. In the Montelukast group (n = 20), infants received oral Montelukast once daily for 10 days (infant's weight < 2 kg received 1.5 mg whereas > 2 kg received 2 mg) with antibiotics plus routine supportive care. In the routine care group (n = 20), infants received antibiotics plus routine supportive care. Primary outcome was the serum level of tumor necrosis factor (TNF) alpha at day 10 of therapy. Secondary clinical and laboratory outcomes were reported along hospital admission. Results: Baseline characteristics were non-significantly different between both groups. After 10 days of therapy, TNF alpha level was significantly lower in the Montelukast group (80.73 ± 50.25 versus 119.54 ± 58.46; p = 0.03). There were non-significant differences between both groups regarding duration of NICU admission, antibiotics duration or modalities and duration of respiratory support. C-reactive protein didn't differ between both groups (p = 0.256). No documented significant adverse effects of Montelukast during the study period. Conclusions: In late preterm neonates with sepsis, 10 days of Montelukast therapy as an adjuvant to antibiotics lowered TNF alpha level without any impact on clinical outcomes. Trial registration: The study was approved by Mansoura Faculty of Medicine institutional research board (IRB) (MS/17.06.95) and it was registered in clinical trials database (clinicaltrials.gov, ID: NCT04474327; registered July 16, 2020). [ABSTRACT FROM AUTHOR]

Montelukast sodium (MS) as an anti‐inflammatory agent in asthma requires a drug delivery system to sustain release at specific doses. ZIF‐8 commonly used in drug delivery systems due to its low cytotoxicity and biodegradability was functionalized with 3‐aminopropyltrimethoxysilane (APTES) as a carrier (ZIF‐8@APTES) for MS. The particles were characterized with Field emission scanning electron microscopy (FE‐SEM), Fourier transform infrared (FTIR), X‐ray diffraction (XRD), Brunauer‐Emmett‐Teller (BET) method, and thermogravimetric analysis (TGA). Furthermore, the biocompatibility of ZIF‐8@APTES‐MS on a normal murine cell line (L929) and its antioxidant activity were investigated. The results showed that MS was gradually released from ZIF‐8@APTES‐MS in phosphate buffer solution (pH 7.4) over 6 hours. ZIF‐8@APTES and ZIF‐8@APTES‐MS also had good biocompatibility properties, and significantly (P≤0.05) enhanced total antioxidant activity at high doses (32 μg/mL). In conclusion ZIF‐8@APTES‐MS can be a promising drug delivery system for MS. [ABSTRACT FROM AUTHOR]

This study aimed to determine the effects of Xiebai Zengye decoction (XBZY) on airway inflammation and respiratory function in rats with postinfectious cough (PIC), and its regulatory effects on the extracellular signal‐regulated kinase (ERK) signaling pathway. Compared with the normal group, the rats from the PIC group had significantly shortened expiratory time (TE) and enhanced pause (EEP), increased resistance (RT), and enhanced pause (Penh), along with increased levels of serum interleukin‐4 (IL‐4) and IL‐6, and decreased levels of IL‐10. The lung and colon tissues of rats from the PIC group showed histopathological changes, including inflammatory cell infiltration, damaged mucosal epithelium, and crypt structure, with significantly increased ERK mRNA and protein expression levels. Treatment with XBZY and montelukast sodium (MAS) improved the respiratory function and serum cytokine levels, reduced tissue inflammation, and decreased ERK mRNA and protein expression levels in the lung and colon tissues. In the lung tissues, XBZY treatment significantly decreased the expression of phosphorylated‐ERK (p‐ERK) protein, as well as p‐MEK1/2, p‐ERK1/2, and p‐c‐Fos proteins, while in the colon tissues, XBZY significantly decreased the expression of p‐ERK1/2 and p‐c‐Fos proteins. However, MAS treatment only showed significant improvement in the lung tissue inflammation score, and the expression level of p‐ERK protein in the lung tissue was decreased. In conclusion, the present study suggests that XBZY has a potential therapeutic effect on PIC by improving respiratory function and attenuating inflammation, and this effect may be associated with the inhibition of the ERK signaling pathway. These findings could provide a new direction for the development of treatments for PIC. However, further research is needed to elucidate the underlying molecular mechanisms of XBZY and to confirm its safety and efficacy in clinical trials. Significance statement: Postinfectious cough (PIC) accounts for 21.73% of the causes of chronic cough in Chinese children and has a higher incidence rate in preschool children. This study aims to observe the effects of Xiebai Zengye decoction (XBZY) on airway inflammation and reactivity in young rat model of PIC cough, and to explore its regulatory effects on the ERK signaling pathway, to preliminarily elucidate the mechanism of XBZY in treating PIC. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the clinical efficacy of modified Shenqi Bufei decoction combined with montelukast sodium in the treatment of chronic cough after non-small cell lung cancer surgery. METHODS: Totally 104 patients with chronic cough after non-small cell lung cancer suegery admitted into the hospital from Jun. 2020 to Jun. 2022 were extracted to be divided into the control group and the observation group via the random number table method, with 52 cases in each group. The control group was treated with Montelukaster sodium tablets, while the observation group received Shenqi Bufei decoction based on the control group. The cough symptom score, Lessister cough quality of life score, serum humoral immune indicators [immunoglobulin A (IgA), immunoglobulin M (IgM), immunoglobulin G (IgG)], serum inflammatory cytokines [C-reactive protein (CRP), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α)] before and after treatment and safety were observed in two groups. RESULTS: After treatment, daytime cough symptom score, nighttime cough symptom score, CRP, IL-6 and TNF-α levels in both groups were lower than those before treatment, and the observation group was lower than the control group, with statistically significant differences (P<0. 05). After treatment, Lycester cough life quality score, IgA, IgM and IgG levels in both groups were higher than those before treatment, and the observe group was higher than the control group, with statistically significant difference (P < 0. 05). CONCLUSIONS: Shenqi Bufei decoction combined with montelukast sodium can reduce the occurrence of chronic cough after non-small cell lung cancer surgery, reduce cough symptom score and serum inflammatory factor expression, and improve the immune function and quality of life of patients. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the clinical efficacy of modified Shenqi Bufei decoction combined with montelukast sodium in the treatment of chronic cough after non-small cell lung cancer surgery. METHODS: Totally 104 patients with chronic cough after non-small cell lung cancer suegery admitted into the hospital from Jun. 2020 to Jun. 2022 were extracted to be divided into the control group and the observation group via the random number table method, with 52 cases in each group. The control group was treated with Montelukaster sodium tablets, while the observation group received Shenqi Bufei decoction based on the control group. The cough symptom score, Lessister cough quality of life score, serum humoral immune indicators [immunoglobulin A (IgA), immunoglobulin M (IgM), immunoglobulin G (IgG)], serum inflammatory cytokines [C-reactive protein (CRP), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α)] before and after treatment and safety were observed in two groups. RESULTS: After treatment, daytime cough symptom score, nighttime cough symptom score, CRP, IL-6 and TNF-α levels in both groups were lower than those before treatment, and the observation group was lower than the control group, with statistically significant differences (P<0. 05). After treatment, Lycester cough life quality score, IgA, IgM and IgG levels in both groups were higher than those before treatment, and the observe group was higher than the control group, with statistically significant difference (P < 0. 05). CONCLUSIONS: Shenqi Bufei decoction combined with montelukast sodium can reduce the occurrence of chronic cough after non-small cell lung cancer surgery, reduce cough symptom score and serum inflammatory factor expression, and improve the immune function and quality of life of patients. [ABSTRACT FROM AUTHOR]

Objective: To investigate the efficacy of Xiyanping injection combined with montelukast sodium in the treatment of children with acute bronchitis and its influence on inflammatory cytokines and cellular immune function. Methods: 180 cases of children with acute bronchitis who were admitted to the Department of Pediatrics of Hefei Second People’s Hospital from January 2021 to April2022 were selected, and they were divided into control group and observation group with 90 cases in each group according to random number table method. On the basis of conventional treatment, the control group was treated with montelukast sodium granules, and the observation group was treated with Xiyanping injection combined with montelukast sodium granules. The efficacy, symptom relief situation, inflammatory cytokines, cellular immune function indexes and the occurrence of adverse reactions were compared in the two groups. Results: Compared with the total clinical effective rate of 87.78% in the control group, 96.67% in the observation group was higher (P＜0.05). The antipyretic time, cough disappearance time and lung rale disappearance time of children in the observation group were shorter than those in the control group (P＜0.05). After treatment, the levels of serum high-sensitivity C-reactive protein (hs-CRP), interleukin-6 (IL-6) and procalcitonin (PCT) in the two groups decreased, and the observation group was lower than the control group (P＜0.05). After treatment, CD8+in the two groups decreased, and the observation group was lower than the control group. CD3+, CD4+, CD4+/CD8+increased, and the observation group was higher than the control group (P＜0.05). There were no serious adverse reactions in the two groups. Conclusion: Xiyanping injection combined with montelukast sodium in the treatment of children with acute bronchitis can improve the clinical therapeutic effect, which may be related to regulating the level of inflammatory cytokines and improving the cellular immune function of the body. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the efficacy of Xiao’er Xiaoji Zhike granules combined with montelukast sodium in the treatment of cough variant asthma (CVA) in children. METHODS: Totally 96 children with CVA admitted into the hospital from Mar. 2020 to Dec. 2021 were extracted to be divided into the control group and the research group via the two-color ball method, with 48 cases in each group. The control group was treated with montelukast sodium, while the research group received Xiao’ er Xiaoji Zhike granules. The efficacy, levels of inflammatory factors [interleukin-6 (IL-6), C-reactive protein (CRP) and tumor necrosis factor-α (TNF-α)], pulmonary function [peak expiratory flow (PEF), forced expiratory volume at one second (FEV1 ) and forced vital capacity (FVC)] and related scale scores before and after treatment, the incidence of adverse drug reactions during treatment in two groups were observed. RESULTS: The total clinical effective rate of the research group was 93. 75% (45/48), higher than 75. 00% (36/48) of the control group, the difference was statistically significant (P<0. 05). After 7 d of treatment, the levels of IL-6, CRP and TNF-α in two groups decreased compared with before treatment, and the research group was lower than the control group, with statistically significant differences (P <0. 05). The PEF, FEV1 and FVC of two groups after treatment were higher than those before treatment, and the research group was higher than the control group, the differences were statistically significant (P <0. 05). After 7 d of treatment, the Leicester Cough Quality of life questionnaire score, Asthma Control Test score and Bronchial Asthma Medication Adherence Scale score in two groups after treatment were higher than those before treatment, and the research group was higher than the control group, the differences were statistically significant (P <0. 05). There were no severe adverse drug reactions in both groups. CONCLUSIONS: Xiao’ er Xiaoji Zhike granules combined with montelukast sodium can effectively alleviate the cough symptoms, improve lung function and reduce the level of inflammatory factors in children with CVA. [ABSTRACT FROM AUTHOR]

An extended release dosage form based on encapsulating the challenging drug busulfan within microspheres of the biodegradable, biocompatible and biosynthesized poly(3-hydroxybutyrate- co -3-hydroxyvalerate) (PHBV) polyester was achieved. The used (PHBV) polymer was biosynthesized by the halophilic archaeon Haloferax mediterranei from date waste biomass as feed-stock. PHBV microspheres of 1.2–2.1 μm diameter were successfully fabricated and loaded with busulfan with an encapsulation efficiency of 29.2 ± 0.2%. In addition, PHBV microspheres of 1.5–3.5 μm diameter and loaded with montelukast sodium (MK) drug were also fabricated with an encapsulation efficiency of 16.0 ± 0.4%. The double-emulsion solvent evaporation method was used to fabricate the drug-loaded microspheres. The drug-loaded microspheres have been characterized by XRD, FTIR and SEM, and confirmed to be successfully fabricated. The drugs in vitro release profiles have shown extended release for up to 3 days in case of busulfan and 8 h in case of montelukast sodium. The in vitro release profiles for busulfan and montelukast suggest that these drug-loaded microcapsules can be efficiently used as new dosage forms to solve the current issues of busulfan administration protocols, and to introduce a new dosage form for montelukast with extended release performance. • Biocompatible, biodegradable and green drug-encapsulating materials of poly(3-hydroxybutyrate- co -3-hydroxyvalerate) (PHBV) biosynthesized from date waste. • Anticancer drug busulfan loaded into PHBV polymer microspheres as promising intravenous dosage form. • Extended release microcapsules for the drugs busulfan and montelukast with up to 3 days continuous release. [Display omitted] [ABSTRACT FROM AUTHOR]

Montelukast is a highly potent and selective receptor antagonist of cysteinyl leukotrienes (CysLT1) used in chronic asthma and vasoconstriction reduction and also used in allergies, swelling, hay fever, and shortness of breath. For the measurement of montelukast sodium in biological and pharmaceutical samples, there are different asynchronous and concurrent analytical methods, such as high‐performance thin layer chromatography, UV spectroscopy, capillary electrophoresis, high‐performance liquid chromatography, and liquid chromatography‐mass spectrometry, have been developed. The pathogenesis of asthma, mechanism of action, and various analytical methods for the detection of montelukast sodium and its combination of dosage forms and biological samples have been described in the present review. Ranjan et al. suggested the reverse phase high‐performance liquid chromatography approach for estimating montelukast in rabbit plasma and found the best limit of detection result of 1.0 ng/mL. Ezzeldin et al. developed a liquid chromatography with tandem mass spectrometry system for the simultaneous detection of combinations of montelukast, gliclazide, and nifedipine. The authors conclude that the studies described in the present manuscript will assist researchers in choosing a simple, rapid, and responsive method for the analysis of montelukast sodium and its combinations. [ABSTRACT FROM AUTHOR]

Objectives: To investigate the effects of Montelukast sodium combined with Budesonide aerosol on airway function and T lymphocytes in asthmatic children. Methods: The records of 86 pediatric asthma patients, treated in Huzhou Maternal and Child Health Hospital from February 2020 to March 2021, were studied retrospectively. Of them, 40 children received routine treatment + budesonide atomizer (Group-I), and 46 patients received routine treatment + budesonide atomizer + montelukast sodium (Group-II). The improvement in airway and lung function, and T-lymphocyte count in both groups after 3 months of corresponding treatment were analyzed. Results: After three months of treatment, expiratory flow rate (TEF) with the tidal volume of 25%, 50% and 75%, was significantly higher in Group-II than Group-I (P<0.05). CD8+ expression in Group-II was lower, and CD3+, CD4+ and CD4+/CD8+ were higher than those in Group-I (P<0.05). There was a significant difference in the levels of inflammatory factors between the two groups. The levels of IL-4, IL-5 and IFN-γ in Group-II were lower than those in Group-I (P<0.05). Conclusions: In the clinical treatment of asthmatic children, in combination with routine treatment, budesonide atomizer and montelukast sodium can effectively promote the improvement of airway function, regulate T lymphocytes levels, reduce inflammatory reaction and improve the total clinical curative effect. [ABSTRACT FROM AUTHOR]

Oral drug delivery is the most preferred and convenient option as the oral route provides maximum active surface area among all drug delivery system for administration of various drugs. In present work, Bilayer tablet of Acebrophylline (Sustain Release) & Montelukast Sodium (Immediate Release) were prepared by direct compression method. All trials of Acebrophylline & Montelukast Sodium and were subjected to precompression, post compression & in vitro drug release study. Bilayer tablet were prepared with passed trials of Acebrophylline & Montelukast sodium (i.e. FP-02) compared with ACEBRO-M (Marketed Product) for its pot compression parameters && in vitro drug release study. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To systematically evaluate the efficacy and safety of montelukast sodium combined with azelastine hydrochloride in the treatment of allergic rhinitis. METHODS: PubMed, CNKI, the Cochrane Library, EMBase and Wanfang database were retrieved to collect the randomized controlled trial of montelukast sodium combined with azelastine hydrochloride in the treatment of allergic rhinitis ( the study group was treated with montelukast sodium combined with azelastine hydrochloride, while the control group received azelastine hydrochloride alone, without limitation of usage and dosage). The retrieval time was from the establishment of the database to Mar. 2021. Meta-analysis was performed by using RevMan 5. 4 software after data extraction by two researchers, selection of literature, and evaluation of risk of bias in the included literature. RESULTS: Totally 13 randomized controlled trials were collected, including 2 659 patients ( 1 330 patients in the study group and 1 329 patients in the control group) . Meta-analysis showed that in terms of effectiveness, the total effective rate ( OR = 6. 25, 95% CI= 4. 52-8. 65, P < 0. 000 01), significant effective rate ( OR= 2. 36, 95% CI= 1. 85-3. 01, P < 0. 000 01) and recurrence rate ( OR= 0. 30, 95%CI = 0. 14-0. 65,P = 0. 002) in the study group were significantly better than those in the control group, and the differences were statistically significant. There was no significant difference in the incidence of adverse drug reactions between two groups (OR= 1. 19,95%CI= 0. 52-2. 71,P= 0. 69>0. 05). CONCLUSIONS: Available evidence suggests that montelukast sodium in combination with azelastine hydrochloride is safe and effective in the treatment of allergic rhinitis, with significant advantages over the use of azelastine hydrochloride alone. Due to the limited number and quality of selected literature, the above conclusions need to be verified by more high-quality randomized controlled trials in the future. [ABSTRACT FROM AUTHOR]

Background: The goal of this research was to use the Quality by Design (QbD) approach to develop orally disintegrating tablets of Montelukast sodium, a leukotriene receptor antagonist used to treat asthma. Characterizing the reference product, defining the quality target product profile (QTPP), identifying critical quality attributes (CQAs), and performing initial testing are all parts of the QbD approach and relating the critical material attributes (CMAs) and critical process parameter (CPP) to drug product CQAs, as a result to develop the design space and defining control strategy. Method: Montelukast sodium tablets were designed using direct compression technique. Formulation were designed by using (DOE software v 13.2) 23 full factorial design in which three variables namely croscarmellose sodium (CCS), microcrystalline cellulose (MCC) and magnesium stearate were varied at two levels by considering one center point. Results: The disintegration time and in vitro dissolution were considered as responses and the prepared tablets have been evaluated for various quality control tests. Formulation F5 was considered as optimized as it showed minimum disintegration time and maximum drug release profile. Conclusion: The CMAs classified as high or medium risk in the initial risk assessment were mitigated to low risk based on the experimentation. Finally, a control strategy was defined giving better control over drug product development. [ABSTRACT FROM AUTHOR]

Background & Objectives: Generally, the blockage of upper respiratory tract in children is seen with the hypertrophy of adenoids and tonsils. Normally for patients with adenoid hypertrophy (AH), Adenoidectomy with or without Tonsillectomy is carried out, however it has its own complications like haemorrhage and recurrence of adenoid tissue. Consequently, therapeutic approach has increased extraordinary consideration rather than surgical procedure. The inflammatory process proposed for AH has prompted the utilization of anti-inflammatory drugs to treat this issue. The objective of this study was to assess the impacts of Montelukast sodium in children with enlarged adenoids. Methods: A randomized controlled trail was performed from April 2018 to March 2019 in the Otorhinolaryngology clinic of Dr. Akbar Niazi Teaching Hospital, Islamabad. In this randomized, placebo treatment-controlled trial, 60 children aged 4-12 years meeting inclusion criteria were isolated into two groups. The study group was treated with Montelukast sodium 5mg consistently for three months while the control group got placebo treatment for a similar timeframe. A questionnaire was filled by parents/ guardians of every child before and after the intervention to evaluate the severity of sleep discomfort, snoring and mouth breathing. Results: Following 3 months of treatment, significant reduction in size of the adenoids was seen in 76% of study group compared with just 3% of control group getting placebo treatment. Conclusion: Montelukast sodium seems to be effective in the reduction of the size of adenoids and improvement in clinical manifestations. It can be viewed as a viable option in contrast to surgical treatment in children with hypertrophy of adenoids. [ABSTRACT FROM AUTHOR]

Objectives: A precise, accurate and selective stability-indicating reverse phase high performance liquid chromatographic assay method has been developed for the simultaneous quantitative determination of Montelukast sodium and Ebastine in tablets. Methods: The chromatographic separation of drugs was attained by using Hypersil octadecyl silane C18 (250 x 4.6 mm, 5µm) column at room temperature. The composition of mobile phase was methanol, acetonitrile and 0.02M ammonium acetate buffer (pH 5.5 adjusted with dilute acetic acid) in the ratio of 80:15:05 v/v/v and flow rate of mobile phase 1.0 ml/min with isocratic elution. The signal of eluents was observed at 244 nm by using diode array detector. Results: The retention time of Montelukast sodium and Ebastine were found to be 4.28 min and 6.63 min, respectively. The linearity ranges for both drugs were found to be 10-50 µg/ml and the percent recoveries were found to be 99.16% and 100.12% for Montelukast sodium and Ebastine respectively. The drug substances and drug products were treated with various forced degradation conditions like acid hydrolysis, alkali hydrolysis, oxidative degradation, thermal degradation and photolytic degradation. The degradants were efficiently separated from the drugs by using optimized chromatographic conditions. The developed method was validated as per recommendation parameters of International conference on harmonization guidelines Q2(R1). Conclusion: The validation parameters indicate that the drug substances were efficiently separated from its degradants and developed method can be routinely applied for the simultaneous quantitative determination of Montelukast sodium and Ebastine in combined tablet formulation in the quality control laboratory. [ABSTRACT FROM AUTHOR]

To explore the efficacy of monclulast sodium combined with levorabastine nasal spray in the treatment of allergic rhinitis in children and the effects on serum levels of eosinophil cationic protein (ECP), eosinophil (EOS) and c-reactive protein (CRP). 151 cases of children with allergic rhinitis who treated from July 2016 to July 2018 in our hospital, according to random number table method thoese childre were divided into 69 control groups and 82 observation groups, the control group was treated with levocarbastine nasal spray, and the observation group was treated with montelukast sodium on the basis of the control group.then clinical curative effect, the symptoms and signs scores, the quality of life score, serum levels of ECP, EOS and CRP, total immunoglobulin E (TIgE) and specific immunoglobulin E (SIgE) before and after the treatment, and adverse reactions occur in both group were compared. The total effective rate in the observation group was higher than that in the control group, and the difference was statistically significant (P<0.05). Before treatment, the scores of symptoms and signs, quality of life, serum levels of ECP, EOS and CRP, total immunoglobulin E (TIgE) and specific immunoglobulin E (SIgE) showed no significant difference between the two groups (P>0.05). After treatment, the above indicators in both groups were decreased, and the observation group was lower than the control group, and the difference was statistically significant (all P<0.05). Both groups had gastrointestinal reactions, dry mouth, and headache, and there was no statistical difference in the incidence of total adverse reactions between the two groups (P>0.05). Montelukast sodium combined with levorabastine nasal spray is safe and effective in the treatment of allergic rhinitis in children, which can reduce serum levels of ECP, EOS and CRP and promote the recovery of children. [ABSTRACT FROM AUTHOR]

Objective: To observe the clinical effect of long-term inhalation of budesonide combined with montelulast sodium in children with gene positive allergic asthma. Methods: 88 cases of children with bronchial asthma according to simple random method were divided into the control group(n=46) and research group(n=42), both groups of conventional treatment, the control group on the basis of routine therapy long-term inhaled budesonide therapy, the research group was treated with montelukast sodium on the basis of the control group, then clinical curative effect, the symptoms and signs disappeared time comparison, acidophilic granulocyte cationic protein(ECP), acidophilic granulocyte(EOS) counting, immunoglobulin(Ig E), interleukin 4(IL-4) and pulmonary function changes before and after the treatment, and adverse reactions occur in both group were compared. Results: After treatment, the total effective rate in the research group was higher than that in the control group, and the disappearance time of shortness of breath, wheeze, rumble in lungs and cough was lesser than that in the control group, the difference was statistically significant(P<0.05). Before treatment, levels of ECP,EOS, Ig E and IL-4, PEF and FEV1 in the two groups were no significant difference(P>0.05). After treatment, the levels of ECP, EOS,Ig E and IL-4 in both groups were decreased compared with that before treatment, the above indexes in the research group were lower than those in the control group, PFE and FEV1 were higher than those before treatment, and the differences in the research group were statistically significant(P<0.05). There was no statistically significant difference in the incidence of total adverse reactions between the two groups(P>0.05). Conclusion: long-term inhalation of budesonide combined with monrostner can improve the efficacy of children with allergic asthma gene positive, reduce symptoms, control airway inflammation and improve lung function. [ABSTRACT FROM AUTHOR]

Clinical efficacy of montelukast sodium combined with budesonide or combined with loratadine in children with cough variant asthma was investigated. A retrospective analysis of the medical records of 72 children with cough variant asthma who were treated in Xuzhou Children's Hospital, Xuzhou Medical University from April 2015 to August 2017 was performed and the 72 child patients were divided into two groups: 35 children were treated with montelukast sodium combined with budesonide in Group A, and 37 children were treated with montelukast sodium combined with loratadine in Group B. The clinical efficacy of the two groups was evaluated according to the lung function indexes [forced expiratory volume in the first second (FEV1), ratio of the forced expiratory volume in the first second to the forced vital capacity (FEV1/FVC), the peak expiratory flow (PEF)], the inflammation biomarkers [tumor necrosis factor-α (TNF-α) and interleukin-4 (IL-4)], the level of eosinophil granulocyte, and the level of IgE at three time-points: before treatment, the 4th week after treatment, and the 12th week after treatment as well as adverse reactions, recurrence of symptoms, and treatment compliance were recorded. After treatment, the levels of FEV1, FEV1/FVC, PEF, TNF-α and IL-4, eosinophil granulocyte and IgE in the two groups were significantly improved (P<0.05). The treatment compliance of Group A was significantly lower than that of Group B (P<0.05). In conclusion, the method of montelukast sodium combined with budesonide or loratadine are both worthy of clinical promotion because they have equivalent efficacy in the treatment of cough variant asthma to effectively improve the lung function and inflammatory response in patients and both bring less adverse reactions and lower recurrence rate. [ABSTRACT FROM AUTHOR]

Objective: To explore the clinical effect of budesonide combined with montelukast sodium in the treatment of children with asthma and it’s effect on the immune function, serum cysteine leukotriene(Cys LTs) and the expression of 5-lipoxygenase activator protein(FLAP). Methods: 118 cases of bronchial asthma were selected in our hospital from March 2015 to January 2017, and divided them into control group and observation group according to the principle of randomization, with 59 cases in each group. The control group was treated with Budesonide Aerosol, and the observation group was treated with montelukast sodium on the basis of the control group. The clinical effect and the changes of lung function, immune index, Cys LTs, FLAP level and clinical effect between the two groups before and after treatment were compared and analyzed. Results: After treatment, the total effective rate of the observation group(93.22%) was significantly higher than that of the control group(77.97%)(P<0.05); the index of FEV1, FVC and FEV1/FVC in two groups increased significantly compared with those before treatment(P <0.05), and the index of FEV1, FVC and FEV1/FVC in the observation group were significantly higher than those in the control group(P <0.05); the CD4+and CD4+/CD8+of two groups were significantly increased before treatment, and CD8+was significantly lower than before treatment(P<0.05), the CD4+and CD4+/CD8+in the observation group were significantly higher than those in the control group, and the CD8+was significantly lower than the control group(P<0.05); the two groups of Cys LTs and FLAP were significantly lower than those before treatment(P<0.05), and the Cys LTs and FLAP in the observation group were significantly lower than those in the control group(P <0.05). Conclusions: The combination of budesonide and montelukast can effectively improve the clinical efficacy and improve the pulmonary function of children with asthma.The mechanism may be related to the enhancement of immune function and the reduction of the expression of serum Cys LTs and FLAP. [ABSTRACT FROM AUTHOR]

Objective: To study the curative efficacy of montruset sodium combined with albuterol in the treatment of severe bronchial asthma and its effects on the serum eosinophil cationic protein(ECP), lipid peroxidase(LPO), exhaled nitric oxide(FeNO) and lung function. Methods: 80 cases of patients with severe bronchial asthma who were diagnosed in our hospital from May 2014 to May2017 were selected and divided into the observation group(n=40) and the control group(n=40) the random number table. The control group was treated with salbutamol, and the observation group was treated with montelukast sodium on the basis of control group. The clinical efficacy, changes of lung function, serum ECP, LPO and FeNO levels before and after treatment and the occurrence of adverse reactions were compared between the two groups. Results: After treatment, the total effective rate of observation group was 92.20%, it was significantly higher than that of the control group(70.00%, P<0.05). The 1-second forced expiratory volume(FEV1), forced lung volume(FVC) and FEV1/FVC levels of observation group were significantly higher than those of the control group(P<0.05). The serum ECP, LPO and FeNO levels were significantly lower than those of the control group(P<0.05). The total incidence of adverse reactions in observation group was 10.00%, it was significantly lower than that of the control group(30.00%, P<0.05). Conclusion: Montruset sodium combined with albuterol was more effective than albuterol alone in the treatment of severe bronchial asthma, it could effectively improve the lung function, which may be related to the significant reduce of serum ECP, LPO, FeNO levels. [ABSTRACT FROM AUTHOR]

Study of oxidative stability of pharmaceutical actives and formulations is important as oxidation pathway is the second most significant route for the decay of pharmaceuticals. Montelukast sodium, a leukotriene receptor antagonist, is prone to oxidation reactions owing to sensitive moieties in its structure. It is also known to be light sensitive. This study was aimed to understand the degradation behaviour of the drug in different oxidative media containing hydrogen peroxide, AIBN, Fe 3+ , Fenton’s reagent and O 2 environment under normal laboratory light conditions. The degradation behaviour of the drug was also evaluated in solid sate under ICH recommended accelerated stability condition of 40 °C/75% RH to correlate with the degradation products (DPs) formed in a solid oral formulation. A total of nine DPs (MTK 1 to MTK 9) were formed from both the drug substance and the marketed tablet formulation on storage under controlled oxygen environment in normal laboratory light and temperature conditions. These DPs were well separated on a C-18 column using a gradient HPLC method. The characterization of DPs was done based on HRMS and multi-stage tandem mass spectrometric (MS n ) data. The knowledge of the structure of DPs helped in laying down degradation pathway of the drug. Also, mechanism for the formation of each DP was postulated. Finally, physicochemical as well as absorption, distribution, metabolism, excretion and toxicity (ADMET) properties of the DPs were predicted by ADMET Predictor™ software. [ABSTRACT FROM AUTHOR]

Objective： To explore the efficacy of montelukast sodium combined with budesonide formoterol powder inhalation in the treatment of bronchial asthma. Methods： A total of 104 patients with bronchial asthma，who sought medical care in the Department of Respiratory and Critical Care Medicine， were randomly divided into the observation group (n=52) and the control group (n=52). The patients in the control group were treated with routine therapy and budesonide formoterol powder inhalation. The patients in the observation group were given montelukast sodium 10 mg once a day in addition to the treatment received by the control group. The clinical treatment efficiency， improvement of lung function，symptom relief and adverse drug reactions (ADRs) were compared between the two groups.Results： Total effective rate of the observation group was significantly higher than that of the control group(92.3% vs 69.2%)，with statistical significance (P<0.01). Improvement of lung function and symptom relief time in the observation group were significantly better than those in the control group， also with statistical significance(P<0.01). In addition，there was no significant difference in the incidence of ADRs when comparisons were made between the two groups. Conclusion： Administration of montelukast sodium on the basis of budesonide formoterol powder inhalation in the treatment of bronchial asthma could quickly relieve clinical symptoms， improve pulmonary function significantly， with higher effective rate. For this reason， it is worth further clinical extension. However， incidence of ADRs demands further study. [ABSTRACT FROM AUTHOR]

Objective: To explore the effect of montelukast sodium combined with budesonide inhalation suspension on serum eosinophilic cell (EOS), eosinophile cationic protein (ECPJand lung function in children with acute episoded asthma. Methods: Selected 200 children with acute episoded asthma who were treated in our hospital from October 2015 to October 2016. they were divided into control group and observation group according to the random number table method, with 100 patients in each group. Patients in control group were treated with montelukast sodium, while patients in observation group were treated with montelukast sodium combined with budesonide inhalation suspension, the treatment course of two groups was lweek. Statistically analyzed the clinical efficacy, pulmonary function, which including forced expiratory volume in the first second (FEV1), forced vital capacity (FVC)and FEV1/FVC, and the changes of serum EOS, ECP levels in two groups before and after treatment. Results: The total effective rate in observation group was 97%, which was significantly higher than control group(P<0.05). The pulmonary function indexes of two groups after treatment were significantly improved than before treatment, and the observation group were significantly better than control group (P<0.05). The serum EOS and ECP levels in two groups after treatment were significantly improved than before treatment, and the observation groups were significantly lower than control group, the differences were statistically significant (P< 0.05). Conclusion: Montelukast sodium combined with budesonide inhalation suspension has a good clinical effect in treatment for children with acute astlima. which can significantly improve the pulmonary function and reduce the serum EOS, ECP levels, so as to relieve the inflammatory reaction of children, it is worth popularizing in clinical application. [ABSTRACT FROM AUTHOR]

Objective: To investigate the cysteinyl aminoacyl receptor antagonist agent montelukast sodium (montelukast) for coxsackievirus B3 (CVB3) infection the protective effect of myocardial injury in mice model. Methods: 65 SPF BALB / c mice, male, weight is 16 to 20 gram were randomly divided into four groups: group a blank control group (10 rats); group B virus control group (15 rats); group C for montelukast sodium group of small dose (20 rats), group D for montelukast sodium group of large dose (20 rats). The inoculation of the virus on the 14th day were all surviving mice, take heart, differences in each group of mice the myocardial lesion score, nuclear factor kB (NF-κB) was observed through various detection technologies. Results: Montelukast sodium treatment group myocardial NF-κB mRNA and protein expression levels were lower than that of the virus control group (P ＜ 0.05), and high dose group significantly; at the same time of montelukast sodium in treatment group and virus control group myocardial NF-κB mRNA and protein expression level and the myocardial lesion score was positively correlated (r =0.77, P ＜ 0.05). Conclusion: Montelukast sodium on myocardial injury in mice serum nuclear factor κB (NF-κB) inhibition, especially significant effect of high dose group and montelukast sodium on CVB3 infection of myocardium in mice has a protective effec. [ABSTRACT FROM AUTHOR]

Objective ：To investigate the influential factors of asthma control during chronic persistent period in elderly pa唱 tients with bronchial asthma ．Methods ：Totally ，８６ elderly outpatients with bronchial asthma who sought medical care in the Drum Tower Hospital Affiliated to Medical College of Nanjing University from October ２０１４ to December ２０１６ were selected and followed up for a long time ．The influential factors of asthma control were analyzed by single唱factor and multi唱factors analysis ．Results ：Seventy唱seven patients had pharmaceutical follow唱ups ，and there was correlation between allergic rhinitis and asthma control （P＜ ０ ．０５） ．The rank sum test analysis indicated that the improvement of asthma control test scores in those pa唱 tients with combined treatment of inhalants and montelukast sodium was obviously better than that of the patients with single treatment of inhalants ，in the ６２ patients with improved asthma ．Conclusion ：It would be more difficult to control asthma in elderly patients combined with bronchial asthma and allergic rhinitis ．Routine inhalants combined with montelukast sodium should be used in the treatment ，so as to enhance therapeutic efficiency. [ABSTRACT FROM AUTHOR]

[Display omitted] • -Using of silica-matrix for the encapsulation and releasing of Montelukast drug for the first time. • -Investigation of kinetic models such as zero, first degree, Higuchi and Korsemeyer-Peppas for the releasing of two type salt of drug; sodium and imidazolium. • - The findings shown that the kinetic model of the releasing of Montelukast sodium is Kerosmayer-Peppas, and montelukast imidazolium is Higuchi. In this research, sol gel method (xerogel) was utilized to investigate the release of encapsulated Montelukast drug in silica matrix. Encapsulation of montelukast was examined in the presence of various parameters such as temperature, loading rates and type of montelukast salt (Sodium or imidazolium). The findings showed that the best conditions for drug release are achieved in the presence of montelukast sodium salt and at room temperature. The releasing data‌ of montelukast sodium and imidazolium were studied using mathematical kinetic models such as zero, first degree, Higuchi and Korsemeyer-Peppas. The results shown that the kinetic model of Montelukast sodium is Kerosmayer-Peppas, and montelukast imidazolium is Higuchi. For the characterization of sol–gel process and encapsulation of drug in silica matrix a number of different analyses including thermal decomposition (TGA), Fourier transform infrared spectroscopy (FT- IR), transient electron microscopy (TEM), and N 2 adsorbtion-desorbtion (BET) were employed. UV spectrophotometry was utilized to determine releasing of drug at different times at 287 nm. The mechanism of drug release is a combination of dissolution and diffusion processes. [ABSTRACT FROM AUTHOR]

目的：探讨孟鲁斯特纳联合玉屏风颗粒治疗小儿过敏性鼻炎患者的临床疗效及安全性。方法：选取于我院进行治疗的小儿 过敏性鼻炎患者60 例，根据电脑生成的随机数字表将所有患者随机分为实验组与对照组，每组各30 例。对照组患者给予孟鲁斯 特纳进行治疗，实验组患者在对照组的基础上联合使用中药制剂玉屏风颗粒进行治疗。比较两组患者治疗前后血清免疫球蛋白 A(IgA)、免疫球蛋白G(IgG)、免疫球蛋白E(IgE)、白介素6(IL-6)、白介素17(IL-17)及白介素23(IL-23)水平，并对两组患者治疗过程 中的不良反应进行记录，评价两组患者的临床疗效。结果：与治疗前相比，两组患者治疗后的血清IgA、IgG水平均升高(P＜0.05)， IgE、IL-6、IL-17 及IL-23 水平均降低(P＜0.05)；与对照组相比，实验组患者血清IgA、IgG水平及临床总有效率较高(P＜0.05)，IgE、 IL-6、IL-17、IL-23 水平及不良反应发生率较低(P＜0.05)。结论：孟鲁斯特纳联合玉屏风颗粒治疗小儿过敏性鼻炎安全有效，可能与 其影响机体血清IgA、IgG、IgE、IL-6、IL-17 及IL-23水平有关。 [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of montelukast sodium and Yupingfeng particles on the total serum immunoglobulin levels and clinical efficacy in the treatment of allergic rhinitis in children. Methods: 60 children with allergic rhinitis from our hospital were selected and randomly divided into the the control group and the experiment group with 30 cases in each group. The control group were treated with montelukast sodium and the experiment group were treated with Yupingfeng particles on the basis of the control group. Then the levels of serum immune globulin protein A (IGA), immunoglobulin protein G (IgG), immunoglobulin protein E (IGE), interleukin 6(IL-6), interleukin 17 (IL) and interleukin 23 (IL-23) between two groups were observed and compared before and after the treatment, and the adverse reactions of the two groups were recorded, and the clinical effect were evaluated. Results: Compared with before treatment, the serum levels of IgA and IgG were higher, and the levels of IgE, IL-6, IL-17 and IL-23 were lower in the two groups after the treatment (P<0.05); Compared with the control group, the serum levels of IgA and IgG were higher, and the levels of IgE, IL-6,IL-17 and IL-23 levels were lower in the experiment group after the treatment (P<0.05). Compared with the control group, the incidence of adverse reactions in the experiment group was lower, and the clinical total effective rate was higher (P<0.05). Conclusion: Montelukast sodium combined with Yupingfeng granules in the treatment of children with allergic rhinitis is safe and effective, which is worthy of clinical application. [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of budesonide combined with montelukast on cytokines,immune function in children with asthma.Methods:96 cases of children with asthma were randomly divided into two groups with 48 cases each group.The children in control group were received montelukast treatment,and the children in observation group were treated with budesonide based on the control group. The treatment lasted 4 weeks.The level of cytokines,immune function and lung function levels were observed and compared,and the clinical efficacy and the incidence of adverse reactions were detected. Results: The total effective rate in observation group was 95.83 ％,obviously higher than 79.17 ％ of control group (P＜0.05).Compared with control group after treatment,the serum IL-5 content was lower,and the IL-12 level was higher in observation group (P＜0.05).Compared with control group after treatment,the serum IgE levels was lower,while the IgA,IgM level was higher in observation group (P＜0.05).The FEV1 and FVC level was higher in the observation group after treatment compared with control group (P＜0.05).The two groups had no significant adverse reactions. Conclusions: Budesonide combined with montelukast sodium has good clinical effect in the treatment of bronchial asthma in children,which may be related to improvement of cytokines,immune function and pulmonary function. [ABSTRACT FROM AUTHOR]

Objective To study the physicochemical properties of aqueous solution of surface active drug montelukast sodium (MS), which could provide experimental basis for further development of micelle or mixed micelle preparations. Methods Critical micelle concentration (CMC) of MS at different temperatures were determined by conductivity measurements. The absorbance and transmittance of MS aqueous solution were measured by UV at different sodium chloride concentration levels. The micelle stability was evaluated via high speed centrifugal. Results The CMC of MS aqueous solution at 25 °C, 30°C, 35°C were 0. 75, 0. 82, 0. 90 mmol/L. The absorbance and transmittance of MS aqueous solution were affected by the sodium chloride concentration and the concentration of MS itself. It was observed that a clear solution was obtained when MS concentration >7. 5 mmol/L and no precipitation was noticed even after high speed centrifugal. Conclusion Montelukast sodium is a surface active drug. Its solubility is related to MS concentration. The solubility is also sensitive to the temperature and the electrolyte concentration. These unique physicochemical properties could be used to develop micelle or mixed micelle pharmaceutical preparations. [ABSTRACT FROM AUTHOR]

A sensitive and validated high performance liquid chromatographic method was developed for determination of montelukast sodium S-enantiomer, A5 and A5 R-enantiomer in montelukast sodium bulk drug. Chromatographic analysis was performed on a Daicel Chiralpak® AD-H column at 30°, the flow rate was set 0.9 ml/min, eluent was n-hexane:isopropanol:ethanol:trifluoroacetic acid:diethylamine (65:15:20:0.1:0.1, v/v/v/v/v), determination wavelength was 280 nm and the injection volume was 10 μl. The high performance liquid chromatography was validated for system suitability, precision, limit of detection and limit of quantitation, linearity, accuracy and robustness. The results indicated that the system suitability test met the requirement with resolution more than 2.0 between montelukast sodium enantiomers and greater than 6.0 between A5 enantiomers. The values of relative standard deviation were not more than 4.0% for precision test, the limit of detection from 0.11 to 0.24 μg/ml, and the limit of quantitation from 0.22 to 0.61 μg/ml, respectively. The linearity correlation coefficients (r) were greater than 0.99 for three analyses. The recovery values were ranged from 89.35 to 108.78%. The proposed method was adequate for the determination of montelukast sodium S-enantiomer, A5 and A5 R-enantiomer in montelukast sodium bulk drug. [ABSTRACT FROM AUTHOR]

Objective: To investigate the effect of budesonide combined with montelukast on cytokines, immune function in children with asthma. Methods: 96 cases of children with asthma were randomly divided into two groups with 48 cases each group. The children in control group were received montelukast treatment, and the children in observation group were treated with budesonide based on the control group. The treatment lasted 4 weeks. The level of cytokines, immune function and lung function levels were observed and compared, and the clinical efficacy and the incidence of adverse reactions were detected. Results: The total effective rate in observation group was 95.83 %, obviously higher than 79.17 % of control group (P<0.05). Compared with control group after treatment, the serum IL-5 content was lower, and the IL-12 level was higher in observation group (P<0.05). Compared with control group after treatment, the serum IgE levels was lower, while the IgA, IgM level was higher in observation group (P<0.05). The FEV1 and FVC level was higher in the observation group after treatment compared with control group (P<0.05). The two groups had no significant adverse reactions. Conclusions: Budesonide combined with montelukast sodium has good clinical effect in the treatment of bronchial asthma in children, which may be related to improvement of cytokines, immune function and pulmonary function. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the efficacy of Montelukast sodium tablets combined with azelastine hydrochloride nasal spray in treatment of allergic rhinitis. METHODS: 76 patients with allergic rhinitis admitted into Hubei Provincial Government Hospital from May 2016 to May 2017 were extracted to be divided into observation group and control group via the admission sequence, with 38 cases in each. The observation group was given Montelukast sodium tablets combined with azelastine hydrochloride nasal spray, while the control group received azelastine hydrochloride nasal spray. Differences of clinical efficacy, relief time of clinical symptoms and relapse of two groups were compared. RESULTS: The total effective rate of observation group was 94.74%(36/38), significantly higher than that of control group(73.68%,28/38), with statistically significant difference(P<0.05). The relief time of sneezing, nasal congestion and salivation in observation group was significantly shorter than that in control group, and the difference was statistically significant(P<0.05). After follow-up of 6 and 12 months, the relapse rate of observation group were 5.26%(2/38) and 10.53%(4/38), significantly lower than those of control group [ 18.42%(7/38) and 23.68%(9/38)], the differences were statistically significant(P<0.05). CONCLUSIONS: The efficacy of Montelukast sodium tablets combined with azelastine hydrochloride nasal spray in treatment of allergic rhinitis is accurate, which can reduce the inflammatory reaction of patients, relieve the clinical symptoms and have lower relapse rate. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the efficacy of Montelukast sodium tablets combined with budesonide fumotrol powder inhalation in treatment of cough variant asthma. METHODS: 92 patients with cough variant asthma admitted into Yuzhou Traditional Chinese Medicine Hospital from Feb.2016 to Sept.2017 were extracted to be divided into observation group and control group via the random number table, with 46 cases in each. The control group was treated with budesonide fumotrol powder inhalation, while the observation group received Montelukast sodium tablets combined with budesonide fumotrol powder inhalation; both groups were treated for 2 months. The cough symptom scores, lung function-related indicators levels (the percentage of forced expiratory volume in 1 s, respiratory peak flow rate), the Medical Outcomes Study item short from health survey (SF-36) and incidence of adverse drug reactions of two groups were observed. RESULTS: After treatment of 2 months, the scores of nighttime and daytime cough symptoms in the two groups were significantly lower than those before treatment, and the observation group was significantly lower than the control group; the percentage of forced expiratory volume in 1 s and the peak flow rate of two groups were significantly higher than those before treatment, and the observation group was significantly higher than the control group; the SF-36 scores of two groups were significantly higher than those before treatment, and the observation group was significantly higher than the control group, with statistically significant differences (P < 0.05). The incidence of adverse drug reactions in observation group and control group were 8.70% (4/46) and 4.35% (2/46), respectively, and the difference was not statistically significant (P >0.05). CONCLUSIONS: Montelukast sodium tablets combined with budesonide fumotrol powder inhalation in treatment of cough variant asthma can significantly relieve the cough symptoms and improve the lung function in patients with higher safety. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the efficacy of ketotifen combined with montelukast sodium in treatment of pediatric bronchitis. METHODS: 120 children with pediatric bronchitis admitted into Zhengzhou Maternal and Child Health Hospital from Sept. 2016 to Sept. 2017 were extracted to be divided into control group and observation group via random number table, with 60 cases in each. The control group was given routine treatment combined with montelukast sodium, while the observation group additionally received ketotifen based on the control group. After treatment of 2 weeks, the clinical efficacy, disappearance time of main symptoms and incidence of adverse drug reactionsof two groups were observed. RESULTS: The total effective rate of observation group was 95. 00%(57/60), significantly higher than that of control group76. 67%(46/60), with statistically significant difference(P < 0.05). The disappearance time of pulmonary dry and wet rales, cough, sputum, fever and lung wheezing of observation group were significantly shorter than those of control group, with statistically significant difference(P < 0.05). The incidence of adverse drug reactions of observation group was significantly lower than that of control group, with statistically significant difference(P < 0.05). CONCLUSIONS: The efficacy of ketotifen combined with montelukast sodium in treatment of pediatric bronchitis is significant, which can effectively improve patients’ main symptoms, accelerate the process of rehabilitation with fewer adverse drug reactions. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the effects of montelukast sodium combined with fluticasone propionate on improving symptoms and life quality in patients with allergic rhinitis. METHODS: 104 patients with allergic rhinitis admitted into the First People's Hospital of Xiantao from May 2016 to May 2017 were selected and divided into observation group and control group via randomly lot drawing, with 52 cases in each. The control group was treated with fluticasone propionate, while the observation group was given montelukast sodium combined with fluticasone propionate. Improvements of clinical symptoms and life quality of two groups were observed. RESULTS: After treatment, scores of rhinocnesmus, running nose, nasal obstruction and sneezing were significantly decreased than those of before treatment,and those of observation group were significantly lower than the control group, with statistically significant differences(P<0.05); after treatment, the average IQRQ scores of observation group was(18.97 ± 3.48) points, which was significantly lower than that of the control group [(23.46 ± 5.34) points], with statistically significant difference(P<0.05). CONCLUSIONS: Montelukast sodium combined with fluticasone propionate in treatment of allergic rhinitis can significantly improve patients' symptoms and life quality. [ABSTRACT FROM AUTHOR]

Objective: To explore the efficacy and recurrence of Montelukast Sodium and SALMETEROL Fluticasone Powder Inhalation on childhood bronchial asthma. Methods Selected 100 cases of children bronchial asthma from Sep, 2011 to Dec, 2012 in our hospital, which were randomly divided into two groups: control group and study group, 50 cases in each. The control group were taken SALMETEROL Fluticasone Powder Inhalation for 6 months, while the study group were taken Montelukast Sodium and SALMETEROL Fluticasone Powder Inhalation. observed the recurrence and control of asthma. Results: Two groups of indices of pulmonary function were improved after drug treatment. The lung function of study group was obviously improved than control group by 3 months, 6 months, and 6 months after discontinuation, the differences were statistically significant (P<0.05); The clinical control rates have improved significantly in two groups, but only the study group had significant difference (P<0.05). The clinical control rate of study group was higher than that of control group by 3 months, 6 months, and 6 months after discontinuation, and the recurrence rate was significantly lower than the control group by 6 months, and 6 months after discontinuation (P<0.05), the differences were statistically significant (P<0.05).Conclusion: Montelukast Sodium and SALMETEROL Fluticasone Powder Inhalation on childhood bronchial asthma have obvious curative effect and low recurrence rate than treated with SALMETEROL Fluticasone Powder Inhalation alone. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe into the clinical efficacy of montelukast sodium combined with salmeterol and fluticasone in treatment of chronic obstructive pulmonary disease ( COPD). METHODS: 124 patients with COED admitted into Henan Tanghe County Traditional Chinese Medicine Hospital from Jun. 2015 to May 2016 were extracted to be divided into observation group and control group via the random number table, with 62 cases in each. The control group was given salmeterol and fluticasone propinate for inhalation, while the observation group additionally received montelukast sodium tablets based on the control group; the treatment course was 12 weeks. The clinical efficacy, lung function indices, dyspnea score, daily life ability score, number of admissions and incidence of adverse drug reactions within one year of follow-up of two groups were observed. RESULTS: The total effective rate of observation group was 96. 77% (60/62) , significantly higher than that of control group [80. 65% (50/62) ]. After treatment, the EVC and LEV, of observation group were better than those of control group, the dyspnea score was significantly lower than the control group, and the daily life ability score was higher than that of control group, with statistically significant differences( P < 0. 05 ). After follow-up of 1 year, the average number of admissions of observation group was (0. 4 ± 0. 2) times, significantly lower than that of control group (1. 1 ±0. 1) times, with statistically significant difference ( P < 0. 05). The incidence of adverse drug reactions of two groups were respectively 3.23% (2/62) and 4.84% (3/62), without any statistically significant differences( P > 0. 05 ). CONCLUSIONS: The efficacy of montelukast sodium combined with salmeterol and fluticasone in treatment of COPD is remarkable, which can improve patients' lung function and life quality with few adverse drug reactions. [ABSTRACT FROM AUTHOR]

OBJECTIVE:To probe into the effects of azithromycin combined with montelukast sodium in treatment of children with mycoplasma pneumonia and effects on serum level of CRP. METHODS:112 children with mycoplasma pneumonia admitted into the First Affiliated Hospital of Henan University of Science and Technology from Jan. 2013 to Dec. 2016 were extracted to be divided into observation group and control group via the random number table, with 56 cases in each. The control group was given azithromycin, while the observation group additionally received montelukast sodium based on the control group. The clinical efficacy, serum CRP and incidence of adverse drug reactions of two groups were observed. RESULTS:The total effective rate of observation group was significantly higher than that of control group, with statistically significant difference(P<0.05). After treatment, the serum CRP of observation group was significantly lower than that of control group, with statistically significant difference(P<0.05). There was no statistically significant difference between two groups in the incidence of adverse drug reactions(P>0.05). CONCLUSIONS:The efficacy of azithromycin combined with montelukast sodium in treatment of children with mycoplasma pneumonia is remarkable, which can effectively reduce the serum CRP with few adverse drug reactions. [ABSTRACT FROM AUTHOR]

OBJECTIVE: To probe inlo the effects of azithromycin combined with monlelukast sodium in treatment of children with mycoplasma pneumonia and effects on serum level of CRP. METHODS: 112 children with mycoplasma pneumonia admitted into the First Affiliated Hospital of Henan University of Science and Technology from Jan. 2013 to Dec. 2016 were extracted to be divided into observation group and control group via the random number table, with 56 cases in each. The control group was given azithromycin, while the observation group additionally received monlelukast sodium based on the control group. The clinical efficacy, serum CRP and incidence of adverse drug reactions of two groups were observed. RESULTS: The total effective rate of observation group was significantly higher than that of control group, with statistically significant difference(P < 0. 05). After I treatment, the serum CRP of observation group was significantly lower than that of control group, with statistically significant difference (P < 0. 05). There was no statistically significant difference between two groups in the incidence of adverse drug reactions (P >0.05). CONCLUSIONS: The efficacy of azithromycin combined with montelukast sodium in treatment of children with mycoplasma pneumonia is remarkable, which can effectively reduce the serum CRP with few adverse drug reactions. [ABSTRACT FROM AUTHOR]

Radioactive iodine (131I) is a known radionuclide which is used both for diagnostic and therapeutic purposes in the treatment of hyperthyroidism and thyroid cancer. Montelukast sodium (Cysteinyl leukotriene receptor-1 antagonist) is also a well-known antioxidant drug. This study aimed to evaluate the histopathological changes in rat livers at the third month following 131I treatment and the radioprotective effect of Montelukast sodium (ML) against I-related liver damage. Thirty female Wistar Albino rats were randomly divided into three groups as control group (n=10), untreated rats; second (RAI) group (n=10), oral radioiodine (111 MBq) administrated rats, and third (ML) group (n=10), oral radioiodine and ML administrated rats. In the third group, ML administration was started 3 days before and ended 10 days after RAI administration. In the third month of radioiodine (RAI) administration, the animals were decapitated and the livers were removed for histopathological examination. The histopathologic data were evaluated comparatively by using Mann Whitney U and Fisher's Exact Tests Differences were determined in all the parameters in terms of intensity between the control and 131I groups, which showed the harmful effects of 131I. In the comparison of the 131I and ML groups, hyperemia was determined respectively 80% to 40%, the presence of inflammatory cells 70% to 60% and capsule thickening 70% to 40%. Montelukast sodium was observed to have a protective effect especially on hyperemia and capsule thickening. According to the study results, radioactive iodine (131I) treatment seems to cause morphological damage to the rat liver, and Montelukast sodium effectively protects the liver against damage. [ABSTRACT FROM AUTHOR]

Purpose: To design an orally disintegrating montelukast sodium tablet (ODT) that disintegrates in the oral cavity leaving an easy-to-swallow residue especially for pediatric and elderly patients who have difficulty swallowing tablets. Methods: Two different formulations of montelukast sodium (5 mg) orally disintegrating tablets were designed and manufactured by direct compression method, using microcrystalline (Avicel PH-102), mannitol, sodium bicarbonate, crospovidone and magnesium stearate as key excipients, and with cherry flavor and aspartame as flavor and sweetener, respectively. These formulations were then evaluated using pharmacopoeial and non-pharmacopoeial physical and chemical tests. Dissolution and assay tests were performed using USP apparatus II and ultraviolet (UV) spectrophotometry, respectively. Formulations with better results were further subjected for optimization study using central composite design method. Results: The results of prototype formulation batch (Trial-02) and the finest optimization formulation batch (FOB-01) reflected the successful development of new formulation of orally disintegrating montelukast sodium 5 mg tablet by direct compression technique. The value of similarity factor f > 50), indicating that both formulations have similar drug release profiles. The formulations were further evaluated for three and six months under accelerated conditions to ascertain their stability. Conclusion: The results obtained demonstrate the suitability of the formulation as an ODT for convenient delivery of montelukast sodium for asthmatic patients. However, clinical studies are required to confirm this. [ABSTRACT FROM AUTHOR]

The aim of the present study was to establish the potential of montelukast loaded nanostructured lipid carrier (MNLC) for pulmonary application. The formulated nanoparticles were evaluated in vitro for aerodynamic characterization and in vivo for pulmokinetics in Wistar rats. The in vitro cytotoxicity was performed on A549 cell line and compared with montelukast-aqueous solution. MNLC was prepared with montelukast (0.2%), Precirol ATO5 (solid lipid), and Capryol-90 (liquid lipid) in the ratio of 7:3 using melt-emulsification-homogenization method. dl -Pyrrolidonecarboxylic acid salt of l -cocyl arginine ethyl ester (CAE), a biodegradable surfactant in the concentration of 1% was used to stabilize the nanoparticles. The particle size and encapsulation efficiency (EE) were 184.6 ± 2.7 nm and >95%, respectively. MNLC-Dry powder for inhalation (DPI) was prepared by lyophilization using 3% mannitol as cryoprotectant and carrier. MNLC-DPI was evaluated for flow, crystallographic and thermal properties. Mass median diameters (MMD) and density for MNLC-DPI were found to be 15.1 ± 1.4 μm and 0.051 ± 0.002 g/cc, respectively. In vitro aerosol performance study indicated more than 95% of the emitted dose (ED) at both the flow rates studied. Mass median aerodynamic diameters (MMAD) of 3.24 ± 0.67 μm with 69.98 ± 1.9% fine particle fraction (FPF) were obtained at 30 L/min flow rate, whereas at 60 L/min MMAD and FPF were found to be 2.83 ± 0.46 μm and 90.22 ± 2.6%, respectively. In vitro cytotoxicity study on A549 cells revealed higher safety of MNLC than pure drug. The pulmonary pharmacokinetic study demonstrated improved bioavailability, longer residence of drug in the lung and targeting factor of 11.76 for MNLC as compared to montelukast-aqueous solution. Thus, the results of the study demonstrated the potential of montelukast lipidic nanoparticulate formulation to improve the efficacy with reduced toxicity leading to better performance of drug as MNLC-DPI for inhalation use. [ABSTRACT FROM AUTHOR]

A simple, selective, accurate and sensitive high performance liquid chromatography ( HPLC) method was developed and validated for the simultaneous determination of rupatadine fumarate ( RPT) and montelukast sodium ( MNT). Chromatographic separation achieved isocratically on a Hypersil BDS C (250 mm × 4.6 mm, 5 μm) column utilizing a mobile phase of methanol: acetonitrile: buffer (40: 30: 30), (pH 3 with HPO) at a flow rate of 1.0 mL/min and column oven temperature 40°C with UV detection at 270 nm. Statistical analysis proves that the method is reproducible and selective for the simultaneous estimation of RPT and MNT. As the method could effectively separate the drugs from their degradation products, it can be employed as stability indicating method. The developed method was validated as per ICH guidelines in terms of accuracy, precision, linearity and specificity. [ABSTRACT FROM AUTHOR]

In this study, radiation effect on an asthma drug Airfix and its ingredients (Montelukast sodium, Sorbitol) were analyzed by using EPR spectroscopy in the dose range of 10 Gy–30 kGy. The dependence of radiation-induced radicals on irradiation dose, temperature and time was investigated in detail. It has been determined that the radical observed predominantly in the Airfix structure originates from Sorbitol, and the characteristic features of this alkyl-type radical have been clearly defined using both experimental EPR and theoretical DFT methods. Dosimetric properties were investigated for all samples and it was suggested that Airfix drug and Sorbitol could be used as an EPR dosimeter through this radical agent which was determined to be very stable and sensitive to radiation. Moreover, it has been emphasized that other drugs containing Sorbitol excipient can also be used for dosimetric purposes in the dose range studied and even irradiation doses can be detected in case of radiation sterilization. • The identity of radical was definitively determined by combination of EPR and DFT. • The alkyl type radical in Sorbitol is quite stable and radiation sensitive. • Drugs contained Sorbitol can be EPR dosimeters in a wide dose range. • The radical in Sorbitol can be used as an indicator for radio-sterilization. [ABSTRACT FROM AUTHOR]

A simple, specific, and accurate reverse-phase liquid chromatographic method was developed for the estimation of Levocetirizine (LCZ), Ambroxol Hydrochloride (AMB), and Montelukast Sodium (MONT) in bulk and pharmaceutical dosage forms. A C18reverse phase column (Phenomenox- RP Aqueous) of 250 × 4.6 mm dimensions and 5 µm particle size with mobile phase containing 15 mm of Ammonium acetate:acetonitrile (40:60%, v/v) was used at isocratic mode and eluents were monitored at 215 nm. The retention times for LCZ, AMB, and MONT are 2.21, 4.46, and 13.35 nm, respectively, and showed a good linearity in the concentration range of 4–20 µg/mL of LCZ, 30–150 µg/mL of AMB, and 8–40 µg/mL of MONT with a correlation coefficient (R) of 0.998, 0.999, and 0.995. The percentage assays were found to be LCZ (99.1), AMB (98.5), and MONT (102.5), respectively. The proposed method was validated as per ICH guidelines and successfully applied to the simultaneous estimation of LCZ, AMB, and MONT in commercial formulations. [ABSTRACT FROM PUBLISHER]