Abstract

OPTIMIZATION DISSOLUTION RATE BY INCLUSION COMPLEXATION OF REPAGLINIDE USING ? CYLCLODEXTRIN

Simanchal Panda* and Monalisa Nayak

ABSTRACT

In the current research, Repaglinide is a carbonoyl methyl benzoic acid derivatives insulinotropic agent used for treatment of NIDDM (non insulin dependent diabetes mellitus) and belongs to class II BCS drugs. The present research work is an attempt to enhance the solubility of the poorly soluble drug, Repaglinide(RPG). The drug also having poor flow properties, which is significantly enhanced by complexation with beta cyclodextrin (BCD). Micromeritics study of pure drug (Repaglinide) measured by tapped density, bulk density, angle of repose, carr’s index, hausner’s ratio which found to be 0.1742,0.2632,33.82%,1.52,33.52 respectively. After complexation it optimized to 0.294,0.384,23.43%,30.064ᵒ,1.306 of above parameters respectively. The calibration curve of RPG with 0.1N HCL and distilled waters with enhanced ratio calibrated a straight line with regression value of 0.999 at 242 nm. Solubility study with solvents distilled water and 0.1N HCl found as 15.78, 84.29mg/100mL respectively. Dissolution of pure drug was found to 20.18%DR after 30min. Complexation made by physical mixture (PM) and kneading method (KM). Phase solubility study shown 5.76,6.24,6.88,7.74, 7.06, 5.54 mg/100ml with molar concentration of BCD 0.5,1,1.5,2.0,2.5,3 respectively. Which was optimized at 1:2. In PM and KM % drug content found 83.82 and 85.62 respectively. The kneading method was optimized by altering solvents at various temperature which shown 15ml ethanol at 45ͦ C was the maximum. The complexation was confirmed by XRD and dissolution carried out at IMMT, BBSR. The fuse peak confirmed the complexation. The optimized dissolution rate found to be 86.43% compared to pure RPG of 20.18 at 30min.

Keywords: Repaglinide, ?-cyclodextrin, XRD, Complexation.