Enhancing the solubility of Candesartan cilexetil-Inclusion Complexation using β-CD

Abstract

Candesartan is primarily used as Anti-Hypertensive which is poorly soluble drug. It is available as salt form of cilexetil i.e., Candesartan cilexetil included under class II of Biopharmaceutical classification system whose bioavailability is 15%.The aim of the study is to enhance the solubility of the Candesartan cilexetil using inclusion complexation technique with β-CD as complexing agent. The complexation is evaluated both in liquid and solid state. The phase solubility profiles in different media (Millipore water, O.1N HCl, PBS 7.4) showed AL- type. Binary Mixtures of Candesartan cilexetil with CDs were prepared in the different ratios of 1molar experimentally with three different techniques (Physical Mixture, Kneading method, co-evaporation method). The complexes were analyzed using Fourier transform infrared spectroscopy and X-Ray diffractometery. From the analysis the complexation was confirmed in the co-evaporation and kneading method. Invitro studies were performed for all the ratios prepared by different methods in order to define the most appropriate ratio and preparation method. The percentage drug release from different mixtures, Marketed product and API is given as follows: Co evaporated Mixture > Kneaded Mixture > > >Physical Mixture≈ Marketed >API