FORMULATION AND OPTIMIZATION OF FLOATING PULSATILE ACECLOFENAC MICROSPHERES USING RESPONSE SURFACE METHODOLOGY

Abstract

The purpose of present work is to develop aceclofenac microspheres for floating pulsatile release intended for chronopharmacotheraphy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The floating pulsatile microspheres were prepared by emulsion solvent diffusion technique. A 32 factorial design was employed to study the effect of independent variables, drug to polymer ratio and stirring speed, on dependent variables, particle size and drug entrapment efficiency. The best batch exhibited a high entrapment efficiency of 90.1% and mean particle size 118.66 μm. Polymers used for the preparation were Eudragit L100 and Eudragit S100 which gets solubilized at pH above 6 and 7 respectively. The floating microsphere provides two phase release pattern with initial lag time during floating in acidic medium followed by rapid release in phosphate buffer. This approach suggested the use of floating pulsatile microsphere as promising drug delivery for site and time specific release of aceclofenac for chronotheraphy of rheumatoid arthritis.