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A PHYSICOCHEMICAL AND DISSOLUTION STUDY OF KETOCONAZOLE – PLURONIC F127 SOLID DISPERSIONS

AGATA GÓRNIAK¹, BOŻENA KAROLEWICZ^2*, HANNA CZAPOR-IRZABEK¹, OLIMPIA GŁADYSZ³

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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.