Formulation and Evaluation of Chlorzoxazone Floating Microspheres

Selva Meena, M (2021) Formulation and Evaluation of Chlorzoxazone Floating Microspheres. Masters thesis, College of Pharmacy, Madurai Medical College, Madurai.

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The aim of the study was to prepare Gastro retentive floating microspheres of chlorzoxazone by solvent evaporation method using ethyl cellulose and HPMCK15 as polymers to provide the drug release in sustained manner and to increase the bioavailability of drug. ❖ The λmax of chlorzoxazone was found to be 282nm using acid buffer pH 1.2 at concentration 10μg/ml. ❖ The chlorzoxazone obey Beer’s law within the concentrations 5-25μg/ml. ❖ The solubility studies of pure drug showed, that the chlorzoxazone was not soluble in water. Sparingly soluble in ethanol, methanol. Soluble in chloroform and ether. ❖ FT-IR studies provided that there was no interaction between the drug and polymers. ❖ Chlorzoxazone floating microspheres were prepared by solvent evaporation method, by changing polymer concentration, rpm, and surfactant concentration. ❖ Percentage yield of floating microspheres were lied in the range of 51.98% - 81.48%. Formulation F9 has highest percentage yield – 81.48%. ❖ Micromeritic properties of microspheres were evaluated. Angle of repose, Bulk density, tapped density, Carr’s index and hausner’s ratio of all formulations was within the acceptable limit. ❖ Particle size of the microspheres was determined by microscopic method, particle size was in the range between 99.9- 399.9μm. ❖ Floating lag time determined using acid buffer pH 1.2; all formulations starts float within 40 seconds. ❖ The % entrapment efficiency of the formulation was lied in the range of 54.42%- 84.47%. Formulation F9 has highest entrapment efficiency with 84.47% this is because of the increasing concentration of polymer. ❖ % buoyancy of the formulation was lied in the range of 50 % - 85 %. Formulation F9 showed better floating ability. ❖ Cumulative % drug release of floating microspheres was found to be 54.27% - 95.79%. Formulation F9 shows 54.27 % of release in 8 hours. ❖ The drug release kinetics of the microspheres was complied with higuchi kinetics model with R2 value 0.977 followed by diffusion drug release mechanism. The ‘n’ value of the korsmeyer peppas was found to be between 0.5 – 1.00 which indicted anomalous non Fickian diffusion i.e. both diffusion and dissolution mediated drug release. CONCLUSION: Gastro retentive floating microspheres of chlorzoxazone were prepared by emulsion solvent evaporation technique, using ethyl cellulose and HPMC K15 in order to retain drug in body for longer period of time to increase bioavailability. Overall results suggest that most variables (polymer concentration, emulsifying agent concentration, type and volume of dispersed phase and stirring speed) had a significant effect on the physical characteristics along with the drug release profile of the formulated floating microspheres. On the basis of data obtained from in-vitro dissolution studies, it can be concluded that formulation F9 was promising formulation suitable for the sustained release of chlorzoxazone for gastro retention purpose that may be giving rise to enhance the bioavailability of the drug. Chlorzoxazone floating drug delivery system promises to be a potential approach for gastric retention used in the treatment of muscular pain by its muscle relaxing property.

Item Type: Thesis (Masters)
Additional Information: 261911308
Uncontrolled Keywords: Formulation, Evaluation, Chlorzoxazone, Floating Microspheres.
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ramakrishnan J
Date Deposited: 15 Aug 2022 06:31
Last Modified: 18 Aug 2022 09:01

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