Enhancement of Dissolution Rate of Aceclofenac by Formation of Aceclofenac-Nicotinic Acid Cocrystal using Water Soluble Polymers like PVPK-30, HPMCE5, SSG and Na-CMC

Abstract

The objective of the present research was to formulate and characterize aceclofenac-nicotinic acid cocrystal and enhancement of dissolution rate of aceclofenac by using water soluble polymers like polyvinylpyrrolidone (PVPK-30), hydroxypropylmethyl cellulose (HPMCE5), sodium starch glycolate (SSG) and carboxymethylcellulose sodium (Na-CMC). Aceclofenac cocrystals were prepared by using drug aceclofenac (ACF) and cocrystal former nicotinic acid (NI) in (1:1 molar ratio), solvent dimethyl sulfoxide (DMSO) and 3% water soluble polymers like PVPK-30, HPMCE5, SSG and Na-CMC by both solvent evaporation and neat grinding method. Tablet for pure drug aceclofenac and various aceclofenac cocrystal formulations were prepared by wet granulation method using Cadmach single station tablet punching machine. The prepared tablet was subjected to in vitro dissolution study using eight station USP type-I (basket) dissolution apparatus in phosphate buffer, PH 7.5. Pure drug aceclofenac (ACF) showed 31.34% drug release. Aceclofenac cocrystal formulation without 3% water soluble polymer like MUSE and MUNG showed drug release 78.98% and 78.51% respectively. Aceclofenac cocrystal formulation MUNG01 (containing 3% PVPK-30), MUNG02 (containing 3% HPMCE5), MUSE03 (containing 3% SSG) and MUSE04 (containing 3% Na-CMC) showed maximum drug release 99.1%, 97.51%, 99%, and 98.25% respectively. The best formulations are MUSE, MUSE03, MUSE04, MUNG, MUNG01 and MUNG02. The best formulations were further evaluated by Fourier transform infrared (FTIR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD) and Scanning electron microscopy (SEM).The result of analysis of FTIR, DSC, PXRD and SEM confirms the formation of a new solid phase i.e aceclofenac cocrystal.Copyright © 2015 iGlobal Research and Publishing Foundation.