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논문 기본 정보

자료유형
학술저널
저자정보
Rhee, Yun-Seok (College of Pharmacy, Sungkyunkwan University) Park, Chun-Woong (College of Pharmacy, Sungkyunkwan University) Nam, Tae-Young (College of Pharmacy, Sungkyunkwan University) Shin, Yoon-Sub (College of Pharmacy, Sungkyunkwan University) Chi, Sang-Cheol (College of Pharmacy, Sungkyunkwan University) Park, Eun-Seok (College of Pharmacy, Sungkyunkwan University)
저널정보
대한약학회 Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 제30권 제1호
발행연도
2007.1
수록면
114 - 123 (10page)

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The aim of this study was to develop an aqueous parenteral formulation containing itraconazole (ITZ) using an o/w microemulsion system. A mixture of benzyl alcohol and medium chain triglyceride (3/1) was chosen as the oil phase. Pseudoternary phase diagrams of the micro-emulsion formations were constructed in order to determine the optimum ratio of oils, the concentration range of surfactant and cosurfactant and the optimum ratio between them. Consequently, the suitability of the chosen microemulsion system as a parenteral formulation was evaluated using droplet size analysis and hemolysis tests. Among the surfactants and cosurfactants screened, a mixture of polyoxyethylene (50) hydrogenated castor oil and ethanol (3/1) showed the largest o/w microemulsion region in the phase diagram. The average droplet size of the microemulsions was < 150nm, and the hemolysis test showed this formulation to be nontoxic to red blood cells. The pharmacokinetic profiles of the ITZ-microemulsion for itraconazole and its major metabolite, hydroxyitraconazole, were compared with those of a PEG 400 solution and cyclodextrin formulations in rats. Overall, these results highlight the potential of an ITZ-microemulsion formulation for the parenteral route.

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