Scholars Research Library

Scholars Research Library

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Der Pharmacia Lettre

Abstract

Solubility enhancement and physicochemical characterization of inclusion complexes of itraconazole

Author(s): Samip S Shah, T. Y. Pasha, Atanu Kumar Behera and Anil Bhandari

Itraconazole (ITZ) is an orally active, triazole antifungal drug. It is used for the management of local and systemic fungal infections. However, the effectiveness of ITZ is limited due to its poor aqueous solubility and low dissolution rate. In the present study, inclusion complexes of ITZ and hydroxyl propyl β-cyclodextrin (HPβCD) were prepared to enhance solubility and in vitro dissolution rate of the drug. Inclusion complex in solution was studied by phase solubility technique. The phase solubility study showed an APtype diagram which is a sign of the development of an inclusion complex in 1:1 molar ratio in solution with the apparent stability constant (Ka) 263 M-1. Solid inclusion complexes of ITZ-HPβCD were prepared in different ratios by numerous methods such as physical mixing, kneading, co-evaporation and spray drying methods. The prepared solid inclusion complexes were characterized by UV, differential scanning calorimetry and Fourier transform infrared (FTIR) spectroscopy. The result of studies confirmed inclusion of ITZ molecule into hollow space of cyclodextrin. From the in vitro studies it can be concluded that inclusion complexes of ITZ with HPβCD can improve the solubility and dissolution rate of ITZ significantly. In compare to all other methods, an inclusion complex obtained by spray drying method showed superior solubility and drug dissolution rate compared to other methods. The in vitro release from all the formulations followed first order kinetic


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