Formulation and Evaluation of Gastro Retentive Drug Delivery System for Ofloxacin

Abstract

The purpose of this investigation was to prepare a gastroretentive drug delivery system of Ofloxacin. Ofloxacin is a fluoroquinolone antibacterial which acts by inhibiting the topoisomerase enzyme which is essential in the reproduction of the bacterial DNA. It is highly soluble in acidic media and precipitates in alkaline media thereby losing its solubility. Hence, a gastroretentive system was developed to enhance the bioavailability by retaining it in the acidic environment of the stomach. Different formulations were formulated using various concentrations of hydroxy propyl methyl cellulose, sodium carboxy methyl cellulose, sodium bicarbonate and citric acid. The formulations were evaluated for quality control tests and all the physical parameters evaluated are within the acceptable limits of Indian Pharmacopoeia. All the formulations were subjected to in-vitro dissolution studies and compared with the marketed formulation. The floating lag time was below 15 seconds for all the formulations except F1 and F2. The floating duration was found to be more than 24 hours in all except F1, F2 and F10. Formulations F7 and F8 were used to study the effect of sodium bicarbonate and formulations F9 and F10 for the effect of hardness on the drug release. Drug release kinetics was studied for prepared formulations and optimized formulation F5 was found to follow zero order kinetics with r² =0.993. The statistical analysis of the parameters of dissolution data obtained before and after storage for 3 months at 25°C/ 60%RH and 40°C/75%RH showed no significant change indicating the two dissolution profiles were similar.