ISSN 2321–3647
Sun, 19 Nov 2017

Solubility Enhancement of Ketoconazole by different techniques and its comparison study

Md.Sahabuddin Ansari1, Mamta Arora1, Md. Sabir Azim2, Md.Adil Hussain1, Gopal Kumar3, Md. Rahmat Ali2,*

1.Translam Institute of Pharmaceutical Education and Research, Meerut (U.P) and Research, Meerut- 250001, (U.P). India.

2.Dept. of Pharmaceutical Chemistry, Faculty of pharmacy, Jamia Hamdard, New Delhi-110062, India.

3.Dept. of Pharmacognosy and Phytochemistry, Faculty of pharmacy, Jamia Hamdard, New Delhi-110062, India.


Enhancement of the solubility is an important physicochemical parameter which affects the absorption of drug and its therapeutic activity. The poor aqueous solubility of drug affects the lack of formulation development. In this study the antifungal drug ketoconazole were prepared with β-cyclodextrin and PEG-6000 by four different methods with an intention to improve its dissolution properties. Solubility of ketoconazole was prepared by sonocrystallization, solid dispersion, hydrotropy and Inclusion complex formation technique. In vitro release profile were evaluated and compared with standard ketoconazole. Solubility by the hydrotropy method was found to be 12.159 fold increases while by inclusion complex, solid dispersion, and melt sonocrystallization method was found to be 9.644, 7.349, and 5.517 fold respectively. Dissolution profile of all four formulations (aqueous suspension), it was found that the formulation prepared by the hydrotropy method showed the best release profile that is 83.16%. Investigations of the properties of the dispersions were performed using release studies with analytical studies, Differential scanning calorimetery (DSC), and Fourier transform infrared (FTIR). FT‐IR spectra revealed no chemical incompatibility between drug and ß‐cyclodextrin. Interaction of Drug-polymer was investigated using differential scanning calorimetry (DSC).

Keywords: Ketoconazole, β-cyclodextrin, PEG-6000, Solubility enhancement, Hydrotropy.

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