title: Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers.
abstract: 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 50mg itraconazole) to that of the currently marketed formulation (Sporanox capsule containing 100mg 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, AUC0-24 and Cmax 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.
authors.affiliation: Pharmaceutical Research Center, Hanmi Pharm Co., Ltd., Paltan-myeon, #893-5 Hwaseong-si, Gyeonggi-do, 445-913, Republic of Korea.
authors.forename: Jong Soo
authors.initials: JS
authors.lastname: Woo
authors.forename: Yun-Kyoung
authors.initials: YK
authors.lastname: Song
authors.forename: Ji-Yeon
authors.initials: JY
authors.lastname: Hong
authors.forename: Soo-Jeong
authors.initials: SJ
authors.lastname: Lim
authors.forename: Chong-Kook
authors.initials: CK
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions; D005215:Fasting / Q000378:metabolism*; D018565:Food-Drug Interactions; D006801:Humans; D017964:Itraconazole / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male
chemical_list: D004655:Emulsions; D017964:Itraconazole