KMID : 0043320120350071169
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Archives of Pharmacal Research 2012 Volume.35 No. 7 p.1169 ~ p.1175
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Inclusion complex effect on the bioavailability of clotrimazole from poloxamer-based solid suppository
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Balakrishnan Prabagar
Song Chung-Kil Cho Hyun-Jong Yang Su-Geun Kim Dae-Duk Yong Chul-Soon Choi Han-Gon
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Abstract
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To study the effect of ¥â-cyclodextrin (¥âCD) inclusion complex on the bioavailability of clotrimazole from poloxamer-based suppository, formulations composed of P 188, propylene glycol and different molar ratio of clotrimazole-¥âCD inclusion complex were prepared. Clotrimazole (1%) has been formulated in a suppository using the thermo sensitive polymer P188 (70%) together with propylene glycol (30%). To increase its aqueous solubility, clotrimazole was incorporated as its inclusion complex at various molar ratios with ¥âCD (1:0.25, 1:0.5, 1:1, and 1:2). The inclusion complex was characterized by differential scanning calorimetry (DSC), XRD and phase solubility studies. It was observed that the complexation with ¥âCD, particularly at high molar ratio (F3 (1:1) and F4 (1:2)) decreased the release profile of clotrimazole considerably. However, suppositories containing inclusion complex at low molar ratio (F1 (1:0.25) and F2 (1:0.5)) showed excellent release profile compared to control formulation. In vivo study in rats at 15 mg/Kg dose showed that the F1 and F2 (82.39 ¡¾ 15.40 and 67.05 ¡¾ 8.79, respectively) significantly increased the AUC compared to that of F3 (41.48 ¡¾ 11.51), F4 (23.34 ¡¾ 8.37) and control (46.7 ¡¾ 7.87) suppositories. Thus, the suppositories containing inclusion complexes prepared at low drug to ¥âCD molar ratio (F1) could be a potential suppository formulation to increase the bioavailability of hydrophobic drugs such as clotrimazole.
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KEYWORD
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Clotrimazole, ¥â-Cyclodextrin, Inclusion complex, Poloxamer 188, Suppository, Enhanced bioavailability
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