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Short Communication Open Access
Complex formation of itraconazole (ITR) with Î²-cyclodextrin (Î²CD) and hydroxy propyl Î²-cyclodextrin (HPÎ²CD) in aqueous solution and in solid state and the possibility of improving the solubility and dissolution rate of ITR via complexation with the above cyclodextrins were investigated. The phase solubility studies indicated the formation of a 1:1 M inclusion complex in solution with both Î²CD and HPÎ²CD. The apparent stability constant (Kc) was 206.2 M-1 and 270.7 M-1 for Î²CD and HPÎ²CD complexes, respectively. Differential Scanning Calorimetry (DSC) studies indicated the formation of solid inclusion complexes of ITR-Î²CD and ITR-HPÎ²CD at 1:4 ratio only. Solid complexes of ITR-Î²CD and ITR-HPÎ²CD (1:l and 1:2 M) prepared by kneading and coevaporation methods exhibited higher rates of dissolution and dissolution efficiency values than the corresponding physical mixtures and ITR itself. Higher dissolution rates were observed with kneaded complexes than with those prepared by coevaporation. Increases of 23.4 and 83.4-fold in the dissolution rate were observed respectively with ITR-Î²CD (1: 2 M) and ITR-HPÎ²CD (1:2 M) kneaded complexes.
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Author(s): K P R Chowdary Shaik Srinivasa Rao