FORMULATION AND DEVELOPMENT OF NOVEL GASTRORETENTIVE MICROBALLOONS OF REPAGLINIDE

Abstract

The present study involves preparation and evaluation of Microballoons of Repaglinide which is having poor solubility in water and low oral bioavailability. Repaglinide, an oral hypoglycemic agent, is rapidly absorbed and eliminated from the body after oral administration. The peak plasma level occurs within an hour of oral administration with elimination half life of 1 hr. The objective of the present work is to prepare floating microballoons of Repaglinide for delivering the drug in controlled manner which will help to reduce dosing frequency and maintain the plasma concentration of drug for longer time without fluctuations. This will be helpful in having better control over clinical maintenance of the type 2 diabetic condition. The Microballoons were prepared by solvent evaporation emulsification technique using Sodium Alginate as coating agent and Calcium Chloride as cross-linking agent. The formation of spherical and hollow Microballoons was confirmed by SEM studies ranging from 220 to 310 μm. The percentage of drug entrapment was found to be 70-80%. The Micromeritic properties indicated better flowability of the spheres. The Buoyancy test showed good floatability for more than 12 hrs. Formulation B5, C5 and D3 showed higher buoyant percentage after 12 hours and percentage yield. Microballoons of Repaglinide were designed to increase the Solubility, Bioavliability and to improve the patient compliance. The microballoons with the smaller particle size enhanced the in vitro drug release of the Repaglinide. Thus, microballoons approach may be a promising carrier for Repaglinide and other BCS class II drugs.