난용성 항진균제 이트라코나졸의 액상제제화에 의한 생체이용율 개선

Enhanced Bioavailability of Itraconazole in Liquid Preparation

This study was to develop an effective itraconazole liquid preparation which exhibits an enhanced bioavailability. The solubility of itraconazole was increased (72-fold) in itraconazole liquid preparation as compared with itraconazole powder. The dissolution rate of itraconazole was higher for itraconazole liquid preparation filled into a hard gelatin capsule with 90% release within 20 min as compared to 55% for Sporanox(R) capsules. The oral absorption of itraconazole liquid preparation and Sporanox(R) tablets were studied in the rat. The area under the concentration-time curve (AUC0-24hr) of itraconazole liquid preparation (90.25+/-8.36mcg.hr/ml) increased by 6.2 times compared to that of Sporanox(R) tablets (14.58+/-1.26mcg.hr/ml) after oral administration of itraconazole 15mg/rat each. Cmax also increased to 6.87+/-1.15mcg/ml after administration of liquid preparation from 1.58+/-0.16mcg/ml of Sporanox(R) tablets. These results indicate that in vivo bioavailability of itraconazole liquid preparation was significantly enhanced as compared with Sporanox(R) tablets.