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Abstract

FORMULATION DEVELOPMENT AND EVALUATION OF FLOATING MICROSPHERE OF TRAZODONE HYDROCHLORIDE

Ritu Bhati*1, Girijesh Kumar Pandey1, Amit Joshi1, B.K. Dubey1, Salaj Khare1, Prabhat Jain2

1 Technocrats Institute of Technology-Pharmacy Education and Research, Bhopal (M.P.).

2 Scan Research laboratories Bhopal (M.P.).

ABSTRACT

Trazodone hydrochloride (TRZ), a serotonin reuptake inhibitor antidepressant. TRZ undergoes first pass metabolism on oral administration resulting in reduced bioavailability (60%). Gastro retentive dosage forms have potential for use as controlled- release drug delivery systems. Gastro retentive floating drug delivery systems have a bulk density lower than that of gastric fluids and thus increase residence time of drug in stomach and provide controlled delivery of many drugs. The present study involves preparation and evaluation of floating microspheres using Trazodone hydrochloride (TRZ) as a model drug for improving the drug bioavailability by prolongation of gastric retention time. Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with TRZ were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres was up to 85.65±0.62 % and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures withsizes in 178.5 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to 73.98±0.65. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of TRZ offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved.

Keywords: Solvent diffusion evaporation method, Trazodone hydrochloride, Ethyl cellulose, Hydroxyl propyl methyl cellulose.


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