Abstract

FORMULATION AND DEVELOPMENT OF CONTROLLED RELEASE TABLET USING OPTIMIZATION APPROACH FOR ALZHEIMER’S DISEASE

Pankaj Kumar Patel*, Divya Barua and Anu Hardenia

Abstract

This research work aims to optimize and formulate the controlled release tablet of Rivastigmine Tartrate using 32 factorial design by direct compression method to provide controlled release of drug at the desired site of absorption. The preformulation studies were carried out in terms of test for identification (physical appearance, melting point, IR spectrum) solubility profile. The tablets were prepared by direct compression method. The 32 full factorial design was used to study the effect of independent variables (Carbopol 971 & HPMC K15 M) on dependent variable (drug dissolution, floating time and bioadhesive strength). Tablets were prepared using these polymers, with the ratios of drug to polymer kept as 1:3. The preliminary and screening studies were performed using different polymers Carbopol 971, Carbopol 934, HPMC E5 LV and HPMC K 15 M. The polymers Carbopol 971 P and HPMC K 15M promised excellent properties for controlled release and muco-adhesion. Sodium bicarbonate at the concentration of 12% w/w was found to be ideal in achieving the buoyancy and 9 batches were made using 32 factorial design. The batch F1 with Carbopol 971 P (35mg) and HPMC K 15 M (20mg) showed the best ex-vivo muco-adhesion result with (20.03gm) which released 98% of drug in 12 hrs. The research work resulted into the successful formulation of floating bioadhesive tablet with excellent ex-vivo muco-adhesive properties, which might circumvent the problems in treatment of Alzheimer’s disease.

Keywords: Rivastigmine Tartrate, HPMC K15 M, Carbopol 971, 32 factorial design, bioadhesive strength.