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

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 t...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2008-02, Vol.33 (2), p.159-165
Main Authors: Woo, Jong Soo, Song, Yun-Kyoung, Hong, Ji-Yeon, Lim, Soo-Jeong, Kim, Chong-Kook
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Area Under Curve
Bioavailability
Biological and medical sciences
Biological Availability
Drug Delivery Systems - methods
Emulsions
Fasting - metabolism
Food-Drug Interactions
Food-effect
General pharmacology
Humans
Itraconazole
Itraconazole - administration & dosage
Itraconazole - blood
Itraconazole - pharmacokinetics
Male
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Self-microemulsifying drug delivery systems
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Summary: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.
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2007.11.001