Acta Pharm. 52 (2002) 9-18

Improvement and characterization of the in vitro dissolution behavior of sulindac by complexation with beta-cyclodextrin

AIMAN A. OBAIDAT^*,  SINA M. MATALQAH and NAJI M. NAJIB

aobaidat@just.edu.jo

¹Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid, Jordan

The specific aim of this study was to investigate the effect of using different methods in the preparation of an inclusion complex between sulindac and beta-cyclodextrin (beta-CD). The methods employed in the study were kneading, co-precipitation, evaporation, and heat under reflux, and all were compared to physical mixtures of sulindac and beta-CD. The formation of an inclusion complex between sulindac and beta-CD in the solid state was confirmed by X-ray diffractometry and differential scanning calorimetry (DSC). The apparent stability constant, Kc, calculated from the slope and intercept of the A_L solubility diagram was found to be 651.53, 88.28, and 38.89 L mol^-1 at pH 2.8, 5.8, and 6.8, respectively. The dissolution rate of sulindac from the inclusion complexes was more rapid than that of sulindac alone. The heat under reflux method was found to be the best of the methods used in this study to form a true inclusion complex and increase the rate of sulindac dissolution.

Keywords: sulindac, beta-cyclodextrin, inclusion complex, dissolution, X-ray diffraction, DSC