Abstract

FORMULATION, DEVELOPMENT AND EVALUATION OF FLOATING MICROSPHERES OF NIZATIDINE FOR GASTRORETENTIVE DRUG DELIVERY

Biru Kumar Thakur*, Dr. Nilesh Jain, Dr. R.B. Goswami

Sagar Institute of Research Technology & Science–Pharmacy Ayodhya Bypass Road, Bhopal

ABSTRACT

Nizatidine is a histamine H2-receptor antagonist that inhibits stomach acid production and used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. The present study involves preparation and evaluation of floating microspheres using nizatidine as a model drug for improving the drug bioavailability by prolongation of gastric retention time. HPMC, Eudragit RL 100, Eudragit RSPO microspheres loaded with nizatidine were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies, zeta potential and In-vitro release. The yield of the microspheres (F1-F6) was range from 65.58±0.25to 78.85±0.36% and F5 microspheres entrapped the maximum amount of the drug. Particle size and zeta potential of optimized microsphere formulation F5 was found to be 210.25 nm and -38.58 mV. The prepared microspheres (F5) exhibited prolonged drug release and percentage buoyancy was found to 79.92±0.36. The formulations were subjected to stability studies and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of nizatidine 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: Nizatidine, Solvent diffusion evaporation method, Hydroxyl propyl methyl cellulose, Eudragit