Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers

被引:76
作者
Woo, Jong Soo [2 ]
Song, Yun-Kyoung [1 ,3 ]
Hong, Ji-Yeon [1 ]
Lim, Soo-Jeong [4 ]
Kim, Chong-Kook [1 ]
机构
[1] Seoul Natl Univ, Coll Pharm, Lab Excellence Drug & Gene Delivery, Seoul 151742, South Korea
[2] Hanmi Pharm Co Ltd, Pharmaceut Res Ctr, Gyeonggido 445913, South Korea
[3] Korea Food & Drug Adm, Dept Drug Evaluat, Narcot & Neuropharmacol Drug Team, Seoul 122704, South Korea
[4] Sejong Univ, Dept Biosci & Biotechnol, Seoul 143747, South Korea
关键词
itraconazole; self-microemulsifying drug delivery systems; bioavailability; food-effect;
D O I
10.1016/j.ejps.2007.11.001
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Self-microemulsifying drug delivery systems (SMEDDS) represent a possible alternative to traditional oral formulations of lipophilic compounds. This study was designed to compare the oral bioavailability and food-effect of SMEDDS of itraconazole (ITRA-GSMP capsule containing 50 mg itraconazole) to that of the currently marketed formulation (Sporanox capsule containing 100 mg itraconazole). Eight healthy volunteers received Sporanox or ITRA-GSMP capsule in the fasted state or after a high-fat diet on four separate dosing occasions with a 2-week washout period. Blood samples were collected and analyzed. After administration of the ITRA-GSMP capsule, AUC(0-24) and C-max were 1.9- and 2.5-fold higher in the fasted state and 1.5- and 1.3-fold higher in the fed state, respectively, than those of the Sporanox capsule. Moreover, ITRA-GSMP capsules yielded more reproducible blood-time profiles than Sporanox capsules. Food had a marked effect on itraconazole absorption from the Sporanox capsule, whereas the influence was less pronounced for the ITRA-GSMP capsule. Collectively, our data suggest that a new self-microemulsifying formulation may provide an alternative oral formulation for itraconazole with improved oral bioavailability and reduced food-effect.
引用
收藏
页码:159 / 165
页数:7
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