A PHYSICOCHEMICAL AND DISSOLUTION STUDY OF
KETOCONAZOLE - PLURONIC F127 SOLID DISPERSIONS
AGATA GÓRNIAK1, BOŻENA KAROLEWICZ2*, HANNA CZAPOR-IRZABEK1, OLIMPIA GŁADYSZ3
Wroclaw Medical University, Faculty of Pharmacy, 211A Borowska, 50-556 Wroclaw, Poland
1Laboratory of Elemental Analysis and Structural Research
2Department of Drug Form Technology
3Department of Inorganic Chemistry
*corresponding author: bozena.karolewicz@umed.wroc.pl
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Abstract:
Ketoconazole is classified as a BCS Class II drug whose dissolution rate is the rate limiting step in the intestinal absorption.
In the presented study, solid dispersions (SDs) of ketoconazole (KET) with Pluronic F127 (PLU) prepared by kneading and
fusion methods were compared with the drug in its pure form. The physicochemical properties of obtained dispersions were
characterized by DSC, XRPD and FTIR techniques and intrinsic dissolution profiles (IDR) of these formulations were
evaluated. On the basis of DSC, XRD and FTIR studies the lack of drug-polymer interactions were stated. The significant
enhancement of ketoconazole dissolution rate in 0.5% sodium lauryl sulphate solution compared with the pure drug were
observed for the obtained solid dispersions. The solid dispersion prepared by kneading method containing 70 wt% of
ketoconazole showed a 32-fold dissolution rate improvement in comparison to the pure drug. Solid dispersions of KET
showed IDR greater than 0.1 mg/cm2/min, therefore a better KET bioavailability than the pure drug should be expected.
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