Dissolution Enhancement of poorly Water Soluble Drug Using Complexation Technique

Abstract

Aim of present work was to enhance the dissolution rate of poorly water soluble drugs using complexion technique. Complexion is a reversible association between two or more molecules to form a non-bonded entity with a well-defined stoichiometry. Cyclodextrins are large molecules with molecular weight greater than 1000Da and are consists of glucose monomers arranged in a donut ring shaped. Cyclodextrins consists of ring which has hydrophilic exterior and lipophilic core in which drug entraps. Phase solubility curve was prepared with different molar concentrations. Complexation was done using kneading method in which drug and cyclodextrin were mixed with addition of solvent to make paste to facilitate drug penetration in hydrophobic cavity of cyclodextrin.Various parameters were optimized like drug to beta cyclodextrin ratio, type and amount of solvent (water: methanol). Effect of addition of hydrophilic components along with complexation using hypromellose was also studied. Phase solubility curve showed that drug: beta cyclodextrin ratio 1:2 was required for complexation. Optimization of various factors could improve dissolution rate and > 85% drug release was obtained with drug: beta cyclodextrin: hypromellose 5 cps in a ratio of 1:2:1. Tablets showed acceptation parameters and improve dissolution rate when compared to marketed product and pure drug. Thus, it can be concluded that complexion can successfully be used for solubility enhancement of hydrophobic drugs.