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This study aims to develop semisolid pharmaceutical forms for the topical administration of mometasone furoate.

Itraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibers. Fibrous mats were prepared under the following experimental conditions: 10, 12.5, and 15 cm needle–collector distance, 20 kV tension, and 1, 1.5, and 2 mL/hour flow rate. The fibers were characterized by SEM, DSC, FTIR, assays, disintegration tests, dissolution tests, and in vitro antifungal activity. Using a 22 factorial design, the effects of preparation variables on the characteristics of the fibrous sheets were described. The electrospinning process led to smooth-surfaced, randomly oriented, and bead-free fibers. The average fiber diameter ranged from 887 nm to 1175 nm. The scanning calorimetry of pure ITZ revealed a sharp endothermic melting point at a temperature of 170 °C, not present in the curves of the fibers. After 60 min, between 70 and 100% of ITZ was released. The antifungal assay revealed that the fibers inhibited the growth of Candida albicans and Candida parapyilosis. The obtained fiber mats prepared from the hydrophilic polymer presented almost instantaneous disintegration, with potential applications for rapid antifungal delivery in oral or topical pharmaceutical form. [ABSTRACT FROM AUTHOR]

One class of cosmetic compounds that have raised interest of many experts is peptides. The search for ingredients with good biocompatibility and bioactivity has led to the use of peptides in cosmetic products. Peptides are novel active ingredients that improve collagen synthesis, enhance skin cell proliferation, or decrease inflammation. Based on their mechanism of action, they can be classified into signal peptides, carrier peptides, neurotransmitter inhibitor peptides, and enzyme inhibitor peptides. This review focuses on the main types of peptides and their application in the cosmetic field, underlining their main limitations. One of the most significant drawbacks of cosmetic peptides is their poor permeability through membranes, which limits their delivery and effectiveness. As a result, this review follows the methods used for improving permeability through the stratum corneum. Increasing peptide bioavailability and stability for enhanced delivery to the desired site of action and visible effects have become central points for the latest research due to their promising features. For this purpose, several methods have been identified and described. Physical techniques include thermal ablation (radiofrequency and laser), electrical methods (electroporation, iontophoresis), mechanical approach (microneedles), and ultrasounds. As an alternative, innovative formulations have been developed in nano-systems such as liposomes, niosomes, ethosomes, nanoemulsions, and other nanomaterials to reduce skin irritation and improve product effectiveness. The purpose of this review is to provide the latest information regarding these noteworthy molecules and the reasoning behind their use in cosmetic formulations. [ABSTRACT FROM AUTHOR]

Miconazole nitrate containing soaps were formulated using one commercially available soap base and three cold process soap bases with various lipids. The aim of our work was to investigate the antimicrobial activity and physicochemical properties of the obtained formulations. The water loss and hardness of the soaps was determined 1, 2, 4 and 9 weeks after preparation. The pH and foamability were determined after 9 weeks of curing time. Two Gram-positive, four Gram-negative bacteria and two yeast (Candida spp.) strains were used in the microbial study. The miconazole content was determined with HPLC-UV analysis. Antimicrobial assay showed that all medicated soaps were effective against Candida albicans. The API had minimal influence on the physicochemical properties (water loss, pH, foamability and consistency) of the soaps. All soaps possessed good lathering properties and an alkaline pH (9.2-11.3). The miconazole content of the soaps varied from 2.72 % to 5.12 % as revealed by HPLC-UV analysis. [ABSTRACT FROM AUTHOR]

Background/Objectives: The search for novel ways of providing treatment also targets the development of formulations used in drug delivery. Among the important characteristics of pharmaceutical gels are their ability to penetrate membranes, their capability to offer rapid response, and their capacity to avoid the hepatic metabolization route followed by many drugs. Bigels combine the advantages of both hydrogels and oleogels, creating a biphasic system that might improve the solubility of amiodarone in water, which is otherwise poorly soluble. This study aimed to succeed in formulating stable amiodarone hydrochloride bigels (coded from ABG1-ABG6) destined for atrial application and evaluating them from a pharmacotechnical perspective. Methods: Three of the six initial formulations presented stability and underwent studies of spreadability, rheology, drug content, textural properties, and microbiological activity. A statistical analysis was performed on penetrometry and drug assay data. Results: The spreadability varied from 1734.07 mm2 (ABG1) to 2163.85 mm2 (ABG6), while the drug concentration ranged between 1.35 and 1.49% (w/w). The textural profile analysis highlighted superior hardness, cohesiveness, and resilience for ABG6 and higher adhesion for ABG2. Both presented pseudoplastic thixotropic behavior, while a plastic thixotropic flow was registered in the case of ABG1. Conclusions: All three bigels are suitable for amiodarone incorporation; however, the influence of the type of ingredients chosen on the texture and properties of the formulations was reflected in the data gathered upon evaluation. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This study aimed to develop and validate an HPLC method in order to assay the indomethacin from therapeutic transdermal systems (TTS). A TTS with indomethacin and HPMC15k as a film-forming agent was developed. The performance of the method was verified in terms of specificity, linearity, detection limit, quantification limit, and precision. The results proved the developed method specificity no interference being observed in a placebo sample at the retention time corresponding to indomethacin. To evaluate the linearity, concentrations in the range of 1-100 µg/mL were used, proving the existence of a linear relationship between the selected points. The detection limit was 0.93 µg/mL and the quantification limit was 2.80 µg/mL. Indomethacin concentration in the analysed samples indicated a concentration of 95.15±4.15% respecting the official data. The statistical parameter used to evaluate the precision was the relative standard deviation, being used in the case of the evaluated concentrations smaller than 2%. In conclusion, the developed method is specific, reproducible and precise. An advantage of the developed method consists of the short analysis time of 3.53 min, whilst the presence of a single characteristic signal in the TTS samples chromatograms certifies that the indomethacin was quantified successfully from the TTS. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from Cannabis sativa used in the treatment of Lennox–Gastaut and Dravet syndromes. The tablets were obtained using an eccentric tableting machine and 9 mm punches. To develop CBD ODTs, the following parameters were varied: the Poloxamer 407 concentration (0 and 10%), the type of co-processed excipient (Prosolv® ODT G2—PODTG2 and Prosolv® EasyTab sp—PETsp), and the type of superdisintegrant (Croscarmellose—CCS, and Soy Polysaccharides—Emcosoy®—EMCS), resulting in eleven formulations (O1–O11). The following dependent parameters were evaluated: friability, disintegration time, crushing strength, and the CBD dissolution at 1, 3, 5, 10, 15, and 30 min. The dependent parameters were verified according to European Pharmacopoeia (Ph. Eur.) requirements. All the tablets obtained were in accordance with quality requirements in terms of friability (less than 1%), and disintegration time (less than 180 s). The crushing strength was between 19 N and 80 N. Regarding the dissolution test, only four formulations exhibited an amount of CBD released higher than 80% at 30 min. Taking into consideration the results obtained and using the Modde 13.1 software, an optimal formulation was developed (O12), which respected the quality criteria chosen (friability 0.23%, crushing strength of 37 N, a disintegration time of 27 s, and the target amount of CBD released in 30 min of 99.3 ± 6%). [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: In the current era of the cosmetic industry, there is an increasing emphasis on quality products, and consumers are starting to pay more attention to the skincare products. An important aspect in this regard is the texture of the product and the way it feels on the skin, which contributes to the general perception of product quality and user satisfaction. Objective: The aim of this research is to investigate and compare the texture characteristics of two cosmetic products (P1 - moisturizing mask, and P2 - repair mask) from the facial masks category. Material and methods: The practical aspect of this study focused primarily on the texture profile analysis (TPA) and compression properties of the cosmetic samples using a Texture analyzer TX-700 instrument (samples evaluated at 23.5°C±0.2°C). Texture profile analysis allows the evaluation of the following parameters: hardness (the strength needed to cause a deformity), cohesiveness (the inherent bond of the load that must be defeated to distribute the product on the skin's surface), adhesion (correlated to the stickiness and responsible for the formation of a bound with the facial surface area), and elasticity (the ability of the material to go back to its original height between the two compression cycles). Results : The results of this analysis highlighted a deep understanding of the differences between mask textures, providing objective data for their comparison and evaluation. The highest hardness was observed in the case of product P1. Products with greater hardness have poorer spreadability. The cohesiveness ranged between 0.476 for P1 and 0.517 for P2. Even if the face mask P2 had a value of adhesiveness (646.9 mJ) almost double compared with the value of P1 (383.1 mJ), the two products had similar values of elasticity (0.5000). Conclusions: These findings hold valuable practical implications for the cosmetics industry, providing pertinent information for the development and continuous improvement of products to effectively meet users' needs and expectations. [ABSTRACT FROM AUTHOR]

Cannabidiol (CBD) is one of the most studied alkaloids found in Cannabis species. Also, its occurrence in Cannabis plants is higher in most of cases compared with the addictive compound named tetrahydrocannabinol (THC). This study aimed to evaluate CBD concentrations and stability in different commercial products and reconstituted oil. An UHPLC method previously published was applied. Three CBD oils and two powders marketed online together with a reconstituted oil were analyzed. The oils presented concentrations lower than stated on the label. The content of reconstituted CBD oils prepared similarly to the commercial oils decrease linearly with small differences based on the storage conditions. Thus, the CBD oil kept at temperatures of 5±0.3°C tends to decompose slightly slower compared with the oil kept at room temperature. A stabilizer may be needed to slow the decomposition process. Future studies for reconstituted formulation may be needed to establish if the type of oil used is influencing the decomposition process. [ABSTRACT FROM AUTHOR]

The aim of this experimental work was the enhancement of water solubility of the lipid lowering drug, atorvastatin, by embedding it in polymer based micro-sized fibers, prepared by electrospinning. Characterization of the fibrous mats included morphological investigations, determination of drug content, disintegration time, small volume dissolution- and DSC studies. The electrospinning process was continuous without droplet formation. The obtained fibers were homogenous, continuous filaments with smooth surfaces. Average fiber diameters were slightly above 1 μm, while disintegration of fiber mats upon contact with water was almost instantaneous (three to ten seconds). Dissolution of the lipid lowering drug was almost complete, when using a solution feed rate of 1 mL/h. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Cutaneous administration is one of the preferred routes for local administration of therapeutic agents especially in pain and inflammation associated with musculoskeletal disorders. The development of hydrogels as semisolid drug delivery systems has increased the attention of researchers considering their easy administration and optimal pharmacological effect. Objective: This study aimed to prepare and evaluate the pharmaco-technical properties of new hydrogel formulations based on synthetic polymers (Carbopol940 and Carbopol980) that deliver diclofenac sodium (the active pharmaceutical ingredient - API) through the skin. Material and methods: Two series of hydrogels were prepared: a series of four hydrogel bases in which the type and concentration of gelling polymer were varied (B1-3% Carbopol940, B2-2% Carbopol940, B3-3% Carbopol980, B4-2% Carbopol980), and a series of four formulation F1-F4 in which 5% w/w API was incorporated. The physicochemical evaluation of the prepared hydrogels included visual evaluation (macro- and microscopically), pH (potentiometric method), rheological properties (Rheotest RV viscometer), spreadability, and texture analysis (Texture analyzer TX-700). For permeability analysis, a UV-Vis Spectrophotometric method (276 nm) was applied using a Mullerman cell, a synthetic membrane (cellophane), and a phosphate buffer solution pH=6.8 (32°±0.2°C) as a receiving medium. Results : All the obtained formulations were homogeneous, without air bubbles and particle agglomerations. The pH ranged between 5.1 for B3 and 7.2 for F2, which is within the limits allowed by the official rules (Ph. Eur.10). For all hydrogels, a pseudoplastic-thixotropic flow was observed. Hydrogels based on 2% Carbopol980 (B4 and F4) had the highest spreadability (SB4=3017.54mm²; SF4=3419.46mm²). Texture profile analysis underlined two important parameters: cohesiveness (which influences the distribution of the product on the skin's surface) and adhesiveness (which influences the stickiness of the product). In the case of the hydrogel series B1-B4, the values of cohesiveness decreased in order: B3 (0.542)>B2 (0.504)>B4 (0.492)>B1 (0.393), and the adhesiveness decreased in order: B4 (3310 mJ)>B3 (2646 mJ)>B2 (2560 mJ)>B1 (1575 mJ). In the case of the hydrogels with API in composition, F4 had the highest value of cohesiveness (0.566) and F1 had the highest value of adhesiveness (3135 mJ). The amount of API after 8 hours decreased in order: F4 (36.59%±4.70)>F2 (19.91%±2.75)>F3 (17.90%±1.57)>F1 (16.35%±2.22). Conclusions: The characteristics of the developed formulations were directly influenced by the formulation variables and they generated differences between the hydrogels. However, it can be stated that all hydrogels presented satisfactory results, and F4 being the most optimal formulation will be integrated in future studies. [ABSTRACT FROM AUTHOR]

Capillary zone electrophoresis (CZE) could be a useful technique for the quantification of active substances from transdermal therapeutic systems (TTSs). TTSs are pharmaceutical forms in development that may release one or more active substances with some significant advantages as increased compliance to treatment, avoidance of first hepatic passage and low manufacturing costs. A simple, reliable, efficient, and lowcost CZE method was developed and validated for the simultaneous determination of levofloxacin (fluoroquinolone) and meloxicam (non-steroidal anti-inflammatory) from TTSs. The selected experimental parameters were 50 mM borax (pH 9.3) as background electrolyte, +25 kV applied voltage, 50 mbar/5 seconds hydrodynamic injection and 40°C temperature, using an uncoated fused-silica capillary with (51 cm total length/43 cm effective length, 50 µm i.d.). CZE experiments were performed in less than four minutes with a resolution of 7.79 at a wavelength of 335 nm. Validation of the method presented good linearity data, precision (RDS% < 1 for migration times and RDS% < 2 for peaks area) and sensitivity (LOD 3.43 and 16.05 µg·mL-1, LOQ 10.38 and 54.55 µg·mL-1 for levofloxacin and meloxicam, respectively). Recovery of the active substances ranged between 85.14% and 96.38%. Our developed CZE method proved its applicability for analysis of the two substances from TTSs. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background and aims. The individualization of cosmetic products or personalized dermatology preparations are in great demand at the present time. Methods. 24 emulsifying cream bases were proposed which were prepared by the classical, automatic and semi-automatic methods, respectively, and the physical stability resulted from the three types of homogenization was taken into account. Texture parameters were also studied for the most stable cream bases in the preformulation stage and the t - statistical test was applied. In order to choose the most optimal preservative, the effectiveness of the NipaEster solution 0.1%, Cosgard and Euxyl® PE 9010 was tested on the strains of Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. Results. 9 cream bases were stable through all the preparation methods used, and preservation was achieved with Euxyl® PE 9010. Following the texture parameters, significant differences were observed for the same formula in the case of choosing a different preparation method. Conclusions. Formulas F1, with methyl glucose sesquistearate as emulsifier, F8, with cetearyl glucosite as emulsifier, and F14, with Ceteareth-20 can be used as cream bases for customized products. [ABSTRACT FROM AUTHOR]

Background: Ibuprofen a nonsteroidal anti-inflammatory drug (NSAID) derived from propionic acid utilized for its anti-inflammatory and analgesic effect was selected as an active substance for incorporation into hydrogel matrices since this active ingredient is recommended for pain therapy, rheumatoid arthritis, and osteoarthritis. Objective: The purpose of this study is to develop and optimize a suspension-type gel containing 5% ibuprofen using a full factorial design and to highlight and optimize the rheology and consistency of the products. Material and methods: In this study, the following substances were used: ibuprofen 5%, sodium carboxymethylcellulose (CMCNa, gel-forming agent), glycerol (humectant), menthol (penetration enhancer), alcohol (co-solvent), and preservative solution. Using Modde 13 software, a full factorial 22 design with 3 central points resulting in 7 formulations was applied, where the gel-forming agent and the humectant represented independent variables as follows: GI1 (CMCNa 2.5g, glycerol 2g), GI2 (CMCNa 2.5g, glycerol 3g), GI3 (CMCNa 5g, glycerol 2g), GI4 (CMCNa 5g, glycerol 3g), and three central points GI5, GI6, GI7 (CMCNa 3.75g, glycerol 2.5g). The remaining substances were added in equal amounts to all gels. The outputs selected were consistency, spreadability, shear stress, and viscosity at shear rates of 6 and 12 during both shear thinning and recovery phases. Results : The evaluated statistical parameters include R² (coefficient of determination) and Q² (measuring the predictive ability of the model), model validity, and reproducibility. All dependent variables exhibit positive predictability values, and all selected inputs highlight an R² close to 1, besides, the validity being > 0.25 indicates the lack of fit of the model. Increasing the concentration of the gel-forming agent produced a significant decrease in the spreadability and consistency while for the outputs selected during the destructuration and restoration phase (viscosity and tangential stress), a complex correlation behavior was noticed. The results obtained from the rheological test were graphically represented, indicating a pseudoplastic thixotropic flow. Conclusions: In conclusion, this study has demonstrated the success of utilizing a full factorial 22 design for the development of an optimal formulation of 5% ibuprofen gel, used in the treatment of local pain. Through the evaluation of 7 formulations, an optimal formulation with specific concentrations of sodium carboxymethylcellulose and glycerol was assessed, which provides the desired characteristics of spreadability, consistency, viscosity, and tangential stress. [ABSTRACT FROM AUTHOR]

Background: Orodispersible films (ODFs) are utilized in medical practice for the ease of administration by patients with dysphagia, as they do not require water for administration. Benzocaine is an anesthetic drug with a dual therapeutic role (treating oral ulcers and throat pain) that can be used in combination with menthol (taste-masking agent). Objective: The objective of this study is to develop a bilayered orodispersible film (FPBS) incorporating 1.5 mg benzocaine/ODF (3.14 cm²). Material and methods: FPBS was obtained by sticking two monolayered films previously obtained through the solvent casting method, one composed of Vivapharm®HPMCE6 and sodium bicarbonate-blank film (FPMB1), and another composed of PVA, benzocaine, menthol, and citric acid (FPMS2). When exposed to saliva in the oral cavity, the components interact and undergo a reaction. Solvents such as alcohol and ultrapure water, plasticizer (glycerol), and sweetener (sucralose) were used. Tests were conducted to evaluate average mass, thickness, folding endurance, pH, adhesiveness, elongation, tensile strength, disintegration in Petri dishes, disintegration according to pharmacopeial methods, and release of the active substance (Erweka, basket) using a phosphate buffer as a dissolution media, pH = 6, 45. Results : The average mass ranged between 108.2±17.03 mg of FPMB1 and 326.9 ±42.85 mg for the bilayered films. The thickness of FPBS was 759.84±35.74 µm while for the monolayered ODFs values between 246.92±32.90 µm (FPMB1) and 509.6±30.3 µm (FPMS2) were recorded. During the folding endurance evaluation, FPBS was influenced by the low resistance of FPMB1, which ruptured after 1-2 folds, whereas FPMS2 was resistant, requiring >60 folds for film rupture. The pH of FPBS reached 2.93 due to the high amount of citric acid while the FPMB1 exhibited a pH of 8.7. In the elongation test, the PVA-ODFs underscored better values compared to the HPMC-based ODFs. Regarding adhesiveness, FPBS exhibited two different values depending on the type of film adhered to the membrane, with the FPMB1 side being more adhesive (25.4±7.1 N/cm²). In terms of tensile strength, FPBS underscored the highest value 6.27 (N*mm-2). The bilayered films disintegrated in 263.6±150.1s in phosphate buffer media, pH = 6, 45, through the pharmacopeial method, results correlated with the amount of benzocaine released (λ = 285 nm) at 30 minutes (>98 %). Conclusions: In conclusion, our study demonstrates that benzocaine can be successfully incorporated into a bilayered film that meets the necessary mechanical, dimensional, and release requirements, making it a practical option for treating oral ulcers. [ABSTRACT FROM AUTHOR]

Objective: The aim of this study is to develop lactose-free orodispersible tablets with loratadine for patients with lactose intolerance. Materials and methods: Seven compositions (F1-F7) of 10 mg loratadine were prepared in form of orally disintegrating tablets, by direct compression, using croscarmellose sodium and pre-gelatinized starch in various concentrations as superdisintegrants, diluted with microcrystalline cellulose and combined with mannitol and maltodextrin as binder agents. The tablets had been studied in terms of their pharmacotechnical characteristics, by determining: the weight uniformity of the tablets, their friability, breaking strength and disintegration time, drug content and the dissolution profile of loratadine. The statistical analyses were performed with GraphPad Prism Software Inc. As dependent variables, both the hardness of the tablets and their disintegration ability differ between batches due to their compositional differences (as independent variables). DDSolver were used for modeling the kinetic of the dissolution processes by fitting the dissolution profiles with time-dependent equations (Zero-order, First-order, Higuchi, Korsmeyer-Peppas, Peppas-Sahlin). Results: All proposed formulas shows rapid disintegration, in less than 15 seconds, and the dissolution loratadine spans a period of about 10 minutes. Akaike index as well as R2 adjusted parameter have demonstrated that the studied dissolution profiles are the best fitted by Zero-order kinetic. Conclusion: In conclusion, association of croscarmellose sodium (7.5%) with pre-gelatinized starch (6%) as superdisintegrants and mannitol as the binder agent (35%), positively influences the dissolution properties of loratadine from orally fast dispersible tablets. [ABSTRACT FROM AUTHOR]

Aim: The development of a new pellets formulation which is able to modulate the release of metoprolol tartrate, an active pharmaceutical ingredient very soluble in water and therefore very difficult to process., Materials and Methods: Two types of different viscosity grade hydroxypropyl methylcellulose (Methocel K100; HPMC 15.000) and Eudragit NE30D are used as prolonged drug release agents, thus resulting in three formulations which have been prepared in form of pellets, in a conventional coating pan. The obtained pellets are characterized and compared in terms of: particles size distribution, drug loading efficiency, drug content and kinetic of in vitro drug release., Results: Lower amounts of Eudragit NE30D (7.5%) determine more uniform size distributions of particles. Drug content and charging efficiency is higher in case of fractions ranging in size from 0.80 to 1.25 mm. The combination of HPMC 15000 with 10% Eudragit NE30D leads to a prolongation for a period of 11.5 hours of metoprolol tartrate release. Release kinetics analysis was performed by fitting the in vitro release profile with different kinetic models., Conclusions: It was developed a pellets formulation that release in vitro the metoprolol tartrate in an extended mode, with Korsmeyer-Peppas kinetic-type.