Search

Salbutamol sulphate is an antiasthamatic and bronchodilator agent, with half life of 1.6 hours and requires multiple daily doses to maintain adequate plasma concentrations. The objective of this present study is to develop a sustained release tablet of salbutamol sulphate which releases the drug in a sustained manner over a period, by using different polymers. The drug was formulated and evaluated as per standard procedure and it was found that F6 formulation gives optimum results. [ABSTRACT FROM AUTHOR]

INTRODUCTION When put on the tongue, fast dissolving tablets immediately dissolve, often in a matter of seconds. They do not need any additional water to make them easier to swallow. Salbutamol sulphate fast disintegrating tablets have a higher bioavailability and dissolving rate. MATERIAL AND METHODS This experimental study was conducted in the Pharmaceutic laboratory of Department of Pharmacy at Universal College of Medical Sciences, Bhairahawa, Nepal from February 2022 to July 2022. A tablet was created utilizing the direct compression method employing mannitol as a diluent and various quantities of super disintegrants, including sodium starch glycolate, croscarmellose sodium, and PVPK-30 as a binder. Pre-compression and post-compression parameters for the formulation were evaluated. RESULTS When examined for hardness, thickness, weight variation, in vitro disintegration time, drug content, and in vitro drug release, tablets were determined to be adequate. Among all formulations, F6 showed that its disintegration time is least and in-vitro dissolution test depicts that F6 formulation shows the maximum drug release (99.99%) within 30 minutes. CONCLUSION This study brings the effectiveness in dosing of patients who have problem in swallowing of conventional dosage form. Among formulations, 15 mg of croscarmellose sodium was found to be the best. [ABSTRACT FROM AUTHOR]

Salbutamol sulphate oral soft jelly in asthma has been formulated and evaluated as the goal of the current investigation. A person with asthma has inflamed, narrowed, swollen, and excess mucusproducing airways, which makes breathing difficult. Salbutamol is used to treat asthma and chronic obstructive pulmonary disease (COPD.It works by relaxing the muscle of the airways into the lungs, which makes it easier to breathe . It functions by loosening the muscles in the lungs' airways, which facilitates breathing. Salbutamol is available as an inhaler, tablets, and certain liquid oral dose forms, but due to patient noncompliance issues, oral jellies containing salbutamol sulphate were developed. This study's aim is to create oral jelly, which by avoiding first pass effect, promotes patient compliance and bioavailability while avoiding many negative effects of conventional dosage forms Salbutamol sulphate oral jelly is simple to swallow and improves patient compliance in paediatric patients. Many paediatric patients find it difficult to swallow tablets and capsules, as well as to use the salbutamol inhalation in cases of asthma. The best In vitro medication release was demonstrated by the salbutamol sulphate oral jelly (F2) batch at 85% in 60 minutes. The drug concentration was discovered to be between 98.23% and 99.25%, which was within the pharmacopoeial range of 98% to 101%. Salbutamol sulphate's UV spectra were examined, and it was discovered that its greatest absorption occurs at 217.50 nm. The cost-effective salbutamol sulphate oral soft jelly also demonstrated improved compliance and an increase in bioavailability. [ABSTRACT FROM AUTHOR]

Copyright of Baghdad Science Journal is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) 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.)

Medicine regulators require the melting points for crystalline drugs, as they are a test for chemical and physical quality. Many drugs, especially salt-forms, suffer concomitant degradation during melting; thus, it would be useful to know if the endotherm associated with melt degradation may be used for characterising the crystallinity of a powder blend. Therefore, the aim of this study was to investigate whether melt-degradation transitions can detect amorphous content in a blend of crystalline and amorphous salbutamol sulphate. Salbutamol sulphate was rendered amorphous by freeze and spray-drying and blended with crystalline drug, forming standards with a range of amorphous content. Crystalline salbutamol sulphate was observed to have a melt-degradation onset of 198.2±0.2°C, while anhydrous amorphous salbutamol sulphate prepared by either method showed similar glass transition temperatures of 119.4±0.7°C combined. Without the energy barrier provided by the ordered crystal lattice, the degradation endotherm for amorphous salbutamol sulphate occurred 50°C below the melting point, with an onset of 143.6±0.2°C. The enthalpies for this degradation transition showed no significant difference between freeze- and spray-dried samples (p>0.05). Distinct from convention, partial integration of the crystalline melt-degradation endotherm was applied to the region 193–221°C which had no contribution from the degradation of amorphous salbutamol sulphate. The linear correlation of these partial areas with amorphous content, R2=0.994, yielded limits of detection and quantification of 0.13% and 0.44% respectively, independent of drying technique. Melt-degradation transitions may be re-purposed for the measurement of amorphous content in powder blends, and they have potential for evaluating disorder more generally. [ABSTRACT FROM AUTHOR]

This study is about a tablet, which disintegrates or dissolves quickly when placed in the oral cavity. Studies on formulation development of Salbutamol Sulphate Immediate Release Tablet, suitable for manufacturing by direct compression have been carried out. Trial formulations using various excipients were developed and evaluated for various qualities like hardness, friability, disintegration time, content uniformity and dissolution. Study concluded that Immediate Release Tablet of Salbutamol Sulphate can be prepared successfully with added patient benefit and increased consumer satisfaction.

Copyright of Journal of Education & Science is the property of Republic of Iraq Ministry of Higher Education & Scientific Research (MOHESR) 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.)

A simple and sensitive method was developed for spectrophotometric determination of etilefrine hydrochloride, salbutamol sulphate and tiemonium methyl sulphate in pure form and in their pharmaceutical formulations. The method was based on reduction of gold solution to gold nanoparticles by the studied drugs in presence of sodium dodecyl sulphate as stabilising agent. Gold nanoparticles (Au NPs) showed a new absorption band at 530 nm that was used for quantitative determination of the cited drugs. Different variables were examined and optimised in the experiment as gold solution concentration, type of buffer, suitable pH, stabilising agent, order of addition, time and temperature of the reaction. Under optimum conditions, the calibration curves were linear with concentration ranges of 3.0-20.0, 5.0-18.0 and 2.0-26.0 μg/mL for etilefrine Hydrochloride, salbutamol sulphate and tiemonium methyl sulphate respectively. The method was applied successfully to determine the studied drugs in pure form and in their pharmaceutical dosage forms, exhibiting good reproducibility and accuracy.

Hydrogels warrant attention as a potential material for use in sustained pulmonary drug delivery due to their swelling and mucoadhesive features. Herein, hyaluronic acid (HA) is considered a promising material due to its therapeutic potential, the effect on lung inflammation, and possible utility as an excipient or drug carrier. In this study, the feasibility of using HA hydrogels (without a model drug) to engineer inhalation powders for controlled pulmonary drug delivery was assessed. A combination of chemical crosslinking and spray-drying was proposed as a novel methodology for the preparation of inhalation powders. Different crosslinkers (urea; UR and glutaraldehyde; GA) were exploited in the hydrogel formulation and the obtained powders were subjected to extensive characterization. Compositional analysis of the powders indicated a crosslinked structure of the hydrogels with sufficient thermal stability to withstand spray drying. The obtained microparticles presented a spherical shape with mean diameter particle sizes from 2.3 ± 1.1 to 3.2 ± 2.9 μm. Microparticles formed from HA crosslinked with GA exhibited a reasonable aerosolization performance (fine particle fraction estimated as 28 ± 2%), whereas lower values were obtained for the UR-based formulation. Likewise, swelling and stability in water were larger for GA than for UR, for which the results were very similar to those obtained for native (not crosslinked) HA. In conclusion, microparticles could successfully be produced from crosslinked HA, and the ones crosslinked by GA exhibited superior performance in terms of aerosolization and swelling.

The search for best performing carriers for dry powder inhalers is getting a great deal of interest to overcome the limitations posed by lactose. The aerosolization of adhesive mixtures between a carrier and a micronized drug is strongly influenced by the carrier solid-state properties. This work aimed at crystallizing kinetically stable D-mannitol polymorphs and at investigating their aerosolization performance when used in adhesive mixtures with two model drugs (salbutamol sulphate, SS, and budesonide, BUD) using a median and median/high resistance inhaler. A further goal was to assess in vitro the cytocompatibility of the produced polymer-doped mannitol polymorphs toward two lung epithelial cell lines. Kinetically stable (up to 12 months under accelerate conditions) α, and δ mannitol forms were crystallized in the presence of 2% w/w PVA and 1% w/w PVP respectively. These solid phases were compared with the β form and lactose as references. The solid-state properties of crystallized mannitol significantly affected aerosolization behavior, with the δ form affording the worst fine particle fraction with both the hydrophilic (9.3 and 6.5%) and the lipophilic (19.6 and 32%) model drugs, while α and β forms behaved in the same manner (11–13% for SS; 53–58% for BUD) and better than lactose (8 and 13% for SS; 26 and 39% for BUD). Recrystallized mannitol, but also PVA and PVP, proved to be safe excipients toward lung cell lines. We concluded that, also for mannitol, the physicochemical properties stemming from different crystal structures represent a tool for modulating carrier-drug interaction and, in turn, aerosolization performance.

The use of physiologically based pharmacokinetic (PBPK) models to support drug product development has become increasingly popular. The in vitro characterization of the materials of the formulation provides valuable descriptors for the in silico prediction of the drug’s pharmacokinetic profile. Thus, the application of an in vitro–in silico framework can be decisive towards the prediction of the in vivo performance of a new medicine. By applying such an approach, this work aimed to derive mechanistic based insights into the potential impact of carrier particles and powder bulk properties on the in vivo performance of a lactose-based dry powder inhaler (DPI). For this, a PBPK model was developed using salbutamol sulphate (SS) as a model drug and the in vitro performance of its low-dose blends (2% w/w) with different types of lactose particles was investigated using different DPI types (capsule versus reservoir) at distinct airflows. Likewise, the influence of various carrier’s particle and bulk properties, device type and airflow were investigated in silico. Results showed that for the capsule-based device, low-dose blends of SS had a better performance, when smaller carrier particles (Dv0.5 ≈ 50 μm) with about 10% of fines were used. This resulted in a better predicted bioavailability of the drug for all the tested airflows. For the reservoir type DPI, the mean particle size (Dv0.5) was identified as the critical parameter impacting performance. Shear cell and air permeability or compressibility measurements, particle size distribution by pressure titration and the tensile strength of the selected lactose carrier powders were found useful to generate descriptors that could anticipate the potential in vivo performance of the tested DPI blends.

The present work deals with the development of controlled release tablets of salbutamol sulphate (SS) using graft copolymers of methyl methacrylate (St-g-PMMA and Ast-g-PMMA) on starch and acetylated starch. Formulations were evaluated for physical characteristics like hardness, friability, drug release, drug content and weight variations, which fulfilled all the official requirements of tablet dosage form. The release rates from formulated matrix tablets were studied at SGF (pH 1.2) followed by SIF (pH 6.8). Drug release from the graft copolymer based tablets was found to be sustained upto the 14 h with >75% drug release. The in-vitro release study showed that the graft copolymer based matrix formulations (F3 & F4) exhibited highest correlation value (r2) for higuchi kinetic model and Korsmeyer's model with n values between 0.61 and 0.67 proved that release mechanisms were governed by both diffusion and erosion mechanism. There was no significant difference in the pharmacokinetic parameters (tmax, Cmax, AUC, Ke, and t1/2) of the graft copolymers matrices and HPMC K100M matrix tablets, indicating their comparable sustained release effect. The potential of graft copolymers to sustain the drug release is well supported by in-vivo pharmacokinetic studies and their adequate physicochemical properties make them promising excipients for controlled drug delivery system.

The main aim of the intended investigation was to establish an analytical method for the assessment of salbutamol sulphate and budesonide in a mixture by UV spectrophotometer. The method involves formation and solving a simultaneous equation for the estimation of individual component in mixture containing salbutamol sulphate and budesonide. Standard solution of salbutamol sulphate shows maximum absorbance at 224 nm and budesonide at 247 nm. Both the drugs followed Beer Lambert's law in the concentration range of 2-10 µg/mL. The method was developed by performing the analytical parameters like linearity, precision, reproducibility, accuracy, recovery, ruggedness, and robustness, limit of detection, and limit of quantitation. The result of all the parameters indicated a good adaptability of the method for the estimation of individual components in a binary mixture of salbutamol sulphate and budesonide. [ABSTRACT FROM AUTHOR]

Graphical abstract Highlights • Aerogels are prepared by thermal inkjet printing followed by supercritical drying. • Process has a printability region restricted by the gel precursor concentration. • Aerogel microspheres have narrow size distribution and high textural properties. • The processing technique is compatible with incorporation of bioactive compounds. • Aerogels are relevant for pulmonary administration and for personalized medicine. Abstract Inkjet printing is as an emerging technique in the biomedical field offering cost-effective solutions for flexible production and the engineering of personalized medicine solutions. Thermal inkjet printing technology in the "drop on demand" mode allows the design of fully automated deposition patterns with high spatial resolution for applications ranging from microparticles in drug formulations to cell deposition in regenerative medicine. In particular, novel formulations in the form of porous particles are sought for the treatment of respiratory disorders and the systemic administration of bioactive compounds using the pulmonary route. Aerogel particles, i.e. highly porous and light-weight nanoporous powders, are particularly promising as carriers for the pulmonary route. In this work, the preparation of aerogel microspheres by thermal inkjet printing followed by supercritical drying is presented for the first time to overcome the current processing limitations. Alginate aerogel particles were loaded with salbutamol sulphate, a bronchodilator used for the treatment of asthma attacks and chronic obstructive pulmonary disease, as a model drug for sustained pulmonary delivery. The optimized processing method allowed the preparation of reproducible nanostructured microparticles with modified salbutamol sulphate release profile and aerodynamic performance of relevance for oral inhalation purposes. [ABSTRACT FROM AUTHOR]

Objectives: To design a formulation and develop ODTs of AMB hydrochloride and salbutamol sulphate in combination for the treatment of respiratory disorders and perform an in vitro evaluation using superdisintegrants in combination with a suitable binder and excipients. Direct compression was used to prepare the tablets. Materials and Methods: In the present research work, different concentrations of SSG as a superdisintegrant were used to optimize the concentration of SSG in the formulation of ODTs. Different concentrations of MCC and PVP K-30 were also studied along with the optimized SSG concentration. The tablets were evaluated for hardness, friability, weight variation, wetting time, in vitro DT, and percentage drug content uniformity. The optimized formulation was further evaluated in an in vitro release study, and drug-excipient compatibility and accelerated stability study. Results: The optimized concentration of SSG was found as 4% on the basis of the lowest DT. The 1% concentration of MCC was selected as the optimum binder concentration on the basis of the lowest DT. ODTs passed all the quality control tests viz., weight variation, hardness, friability, in vitro DT, drug content (%) and wetting time. The formulation satisfied the requirements of the FDA for rapid-dissolving tablets and allowed more than 85% drug to be released within 30 min. The fourier transform infrared spectroscopy study revealed that there was no interaction between the drug and excipients. The accelerated stability study shows that formulation is quite stable at normal temperature and humidity conditions as well as at extreme temperature conditions. Conclusion: By adopting a systematic formulation approach, ODTs of AMB hydrochloride and salbutamol sulphate in fixed-dose combination can be formulated using superdisintegrants in combination with appropriate binder and excipients; this was found to be economical and industrially feasible. [ABSTRACT FROM AUTHOR]

The objective was to investigate the effect of dry coating of salbutamol sulphate (SS) with magnesium stearate (MgSt) on the kinetics of powder de-agglomeration. The relative de-agglomeration of the MgSt coated SS powders was higher than uncoated SS at all air flow rates; the SS coated with 2 % MgSt showed the highest extent of de-agglomeration (> 5 % MgSt coated SS > 1 % MgSt coated SS). Rate of de-agglomeration was described by a cumulative de-agglomerated versus time profile. Profiles fitted a mono-exponential model and the de-agglomeration rate constant (kd) was estimated. No significant differences existed between any of the uncoated and coated powders. The significance of this study relates to the improved aerosolization and de-agglomeration performance of the MgSt coated SS powders with optimum performance of 2 % MgSt coated SS. More significant is the finding that no change existed in de-agglomeration rate constants between the coated and uncoated powders, with the potential implications that their aerosol plume concentration and deposition patterns were similar.

Drug delivery to the body via the inhaled route is dependent upon patient status, device use, and respirable formulation characteristics. Further to inhalation, drug‐containing particles interact and dissolve within pulmonary fluid leading to the desired pharmacological response. Pulmonary surfactant stabilises the alveolar air‐liquid interface and permits optimal respiratory mechanics. This material represents the initial contacting surface for all inhaled matter. On dissolution, the fate of a drug substance can include receptor activation, membrane partitioning and cellular penetration. Here, we consider the partitioning behaviour of salbutamol when located in proximity to a simulated pulmonary surfactant monolayer at pH 7. The administration of salbutamol to the underside of the surfactant film resulted in an expanded character for the 2‐dimensional ensemble and a decrease in the compressibility term. The rate of drug partitioning was greater when the monolayer was in the expanded state (ie, inhalation end‐point), which was ascribed to more accessible areas for molecular insertion. Quantum mechanics protocols, executed via Gaussian 09, indicated that constructive interactions between salbutamol and integral components of the model surfactant film took the form of electrostatic and hydrophobic associations. The favourable interactions are thought to promote drug insertion into the monolayer structure leading to the observed expanded character. The data presented herein confirm that drug partitioning into pulmonary surfactant monolayers is a likely prospect further to the inhalation of respirable formulations. As such, this process holds potential to reduce drug‐receptor activation and/or increase the residence time of drug within the pulmonary space. [ABSTRACT FROM AUTHOR]

A simple and sensitive method was developed for spectrophotometric determination of etilefrine hydrochloride, salbutamol sulphate and tiemonium methyl sulphate in pure form and in their pharmaceutical formulations. The method was based on reduction of gold solution to gold nanoparticles by the studied drugs in presence of sodium dodecyl sulphate as stabilising agent. Gold nanoparticles (Au NPs) showed a new absorption band at 530 nm that was used for quantitative determination of the cited drugs. Different variables were examined and optimised in the experiment as gold solution concentration, type of buffer, suitable pH, stabilising agent, order of addition, time and temperature of the reaction. Under optimum conditions, the calibration curves were linear with concentration ranges of 3.0-20.0, 5.0-18.0 and 2.0-26.0 µg/mL for etilefrine Hydrochloride, salbutamol sulphate and tiemonium methyl sulphate respectively. The method was applied successfully to determine the studied drugs in pure form and in their pharmaceutical dosage forms, exhibiting good reproducibility and accuracy. [ABSTRACT FROM AUTHOR]

This study investigates engineered carrier, as well as engineered API particles, and shows that there are distinct performance indicators of particle engineering for carrier-based dry powder inhalers (DPIs). Spray dried (SDSS) and jet-milled (JMSS) salbutamol sulphate (SS) was blended with untreated α-lactose monohydrate (LAC_R) and α-lactose monohydrate engineered (LAC_E). Subsequent capsule filling was performed with different process settings on a dosator nozzle capsule filling machine in order to reach a target fill weight of 20–25 mg. To evaluate the performance of the different mixtures, in vitro lung deposition experiments were carried out with a next generation impactor, the emitted dose (ED) and fine particle fraction (FPF) were calculated based on the specification of the European pharmacopoeia. The FPF of micronised powder blends is significantly higher (20%) compared to the FPF of spray dried blends (5%). Compared to API engineering, carrier engineering had a positive effect on the capsule filling performance (weight variability and mean fill weight) at lower compression ratios (setting 1). Results further showed that higher compression ratios appear to be beneficial in terms of capsule filling performance (higher fill weight and less fill weight variation). Concluding, it can be stated that the carrier engineering, or generally carrier properties, govern downstream processing, whereas the API engineering and API properties govern the aerosolisation performance and thereby significantly affect the dose delivery to the lungs. [ABSTRACT FROM AUTHOR]

As pulmonary drug delivery is extended from low doses to high doses, physicochemical characteristics of the active pharmaceutical ingredient gain importance in the development of dry powder inhalers. Therefore, the present work aims to understand the impact of distinct engineering techniques on the process induced physicochemical characteristics of salbutamol sulphate particles over time. The particle engineering techniques chosen were jet-milling and spray-drying, two well used processes in the production of predominately crystalline and amorphous inhalable particles, respectively. Fourier transform infrared spectroscopy, modulated differential scanning calorimetry, particle size distribution and tensiometry experiments were used to characterise the engineered powders immediately, 7, 14 and 21 days after production. The rugged spherical amorphous particles (3.75 ± 0.08 μm) obtained via spray-drying showed that they were capable of forming strong agglomerates (5.01 ± 0.22 μm) through “amorphous bridging”. On the other hand, jet-milling produced smaller (2.06 ± 0.08 μm), crystalline, irregular shaped particles with a very large surface area (11.04 ± 0.10 m 2 /g) that, over time, formed looser particle aggregates of decreasing size (3.76 ± 0.10 μm). Temporal evolution of the properties of spray-dried and jet milled particles showed a notable influence on the efficiency of blending with a model carrier at 0, 7 and 21 days (e.g. relative standard deviation of drug content of 11.3, 7.0 and 21.6%, respectively). [ABSTRACT FROM AUTHOR]

In this study, electrostatic charging of lactose and its mixtures with salbutamol sulphate (SS) were studied as a function of relative humidity (RH). Powder adhesion onto a steel pipe surface was also investigated. The powders were charged by sliding in a steel pipe. Increase in RH decreased the charging of lactose and mixtures, but the effect on SS was not evident. Furthermore, the charge of the mixtures reversed from negative to positive as RH was increased and remained positive as the samples were again dried. Humidification also changed the adhesion behavior of the mixtures onto the pipe surface. [ABSTRACT FROM AUTHOR]

ABSTRACT A quick, convenient and sensitive method has been developed for the determination of microgram amounts of salbutamol sulphate in its pure form and pharmaceutical preparations. The method is based on the coupling reaction of the drug with diazotized 2,4 - dinitroaniline reagent in an alkaline medium to produce an intense blue coloured Water soluble and stable azo dye which exhibits a maximum absorption at 558 nm. Beer's law was obeyed over the concentration range 0.2 - 6 µg/ml with a molar absorptivity of 9.33×104 L.mol-1.cm-1 and Sandell's sensitivity index of 0.0061 g/cm2. The limit of detection is 0.0089 µg/ml while the limit of quantitation is 0.029 µg/ml. The method shows high accuracy (average recovery 99.75%) and precision (relative standard division (RSD) is less than 2.2%.The suggested procedure was applied for determination of salbutamol sulphate without any interference from common pharmaceutical excipients. The proposed method is successfully compared with the official method.

A sensitive reverse phase-high performance liquid chromatography (RP-HPLC) method with fluorescent detector (FLD) was developed and optimized for salbutamol sulfate (SS) determination in human plasma. In this regard, mobile phase specifications, extraction procedures and excitation and emission wavelengths were optimized. The HPLC system consisted of a Lichrosorb RP-C18 analytical column (4.6 × 200 mm, 5 µm) with FLD operated at excitation 228 nm and emission 310 nm. Mobile phase {CH3OH/(NH4)H2PO4 (67 mM) (pH 3.0)/triethylamine (TEA), 50/50/0.02 (v/v/v %)} was run at a flow rate of 0.7 mL/min. To clean up the samples, a liquid-liquid extraction (LLE) procedure was selected and optimized. SS and tramadol hydrochloride (TH) eluted at 4.1 min and 5.2 min, respectively. Adequate extraction efficiency was achieved by DEHP (75.88-85.52 %). The standard curve was linear for the range tested (0.5−80 ng/mL) and the coefficient of determination was 0.9989. A detection limit of 0.17 ng/mL was achieved. The intra- and inter-day precision was less than 4 %. The present assay combines adequate accuracy and precision with sensitivity for SS determination in human plasma and can be applied to study pharmacokinetics of SS sustained release tablets after oral administration in human.

This article describes the preparation and characterization (in vitro and in vivo) of three different sustained-release salbutamol sulfate−ethylcellulose tabletted microparticles (T1, T2 and T3) and reference sustained release tablet (Ventolin 8 mg SR, GSK). In vitro characterization included dissolution study, scanning electron microscopy, UV and FTIR spectroscopy, X−ray diffractometry and thermal analysis. A validated HPLC−fluorescent detection method was adopted to conduct bioavailability studies in young healthy human volunteers. The microparticles exhibited an irregular and slightly aggregated morphology with fine rheological properties. No strong chemical interaction was found between drug and polymer. A good linear correlation (R2 = 0.9224, 0.945, 0.9363 and 0.9694 for T1, T2, T3 and reference formulations, respectively) was obtained between the percent cumulative drug released (in vitro) and the percent cumulative drug absorbed (in vivo) data of these formulations at specific time points to develop level A in vitro−in vivo correlation. However, T2 was found closer to the reference formulation that shows a reliable prediction of the plasma concentrations obtained following a single dose of salbutamol sulfate modified release formulations.

In silico modeling was used to predict the impact of carrier surface modifications on the in vivo plasma concentration of an active pharmaceutical ingredient (API) and as a tool to support formulation development. In vitro fine particle fraction (FPF) and mass median aerodynamic diameter (MMAD) of salbutamol sulphate delivered from Cyclocaps ® , detached from unmodified and surface engineered glass beads were measured using a Next Generation Impactor (NGI). Surface roughness was chosen to classify surface modification/engineering and it was evaluated via scanning electron microscopy (SEM) and image analysis. An in silico pharmacokinetic (PK) model was built and the quality confirmed with available literature data. Plasma profiles were generated combining the PK model with in silico deposition models for salbutamol sulphate released from Cyclocaps ® , unmodified and surface engineered glass beads. The increased roughness of the surface of engineered beads resulted in a FPF 1.36 times higher than that of untreated beads. C max from the in silico plasma profile of salbutamol released from the surface engineered beads was 1.20 fold higher than that from untreated beads. Increasing the surface roughness was found to augment the amount of drug loading and detaching from the carrier both in vitro and in silico . [ABSTRACT FROM AUTHOR]