Formulation and pharmacokinetics of the parenteral fat nano-emulsion of ubenimex

作     者：孙晓利 刘东华 李鹏 徐文方 张娜 

作者机构：山东大学药学院山东济南250012 

基　　金：Shandong Province Natural Science Foundation (Grant No.ZR2009CM011) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2011年第20卷第5期

页      码：483-492页

摘      要：The fat nano-emulsion, which has been used as a drug carrier, especially for the poorly water soluble drug, has drawn favorable attention recently. Ubenimex is a poorly soluble drug with no parenteral treatment available for patients. This study was aimed at the manufacture of a ubenimex loaded fat nano-emulsion for intravenous delivery by SolEmuls~ technology. The formulation and the process parameters were optimized by single-factor design and the obtained ubenimex loaded fat nano-emulsion was stable even after autoclaving. The average particle size was near 200 nm with narrow size distribution and a negative zeta potential of -44 mV. The in vitro release behavior of ubenimex from the fat nano-emulsion could be described by the double phase kinetics model and expressed by the following equation： 100 - Q = 75.27e^-0.369t ＋ 15.94e^-0.0324t, Rα = 0.9863, Rβ = 0.9878. The pharmacokinetic study showed that the pharmacokinetic curves of both the ubenimex fat nano-emulsion and the i.v. ubenimex suspension, were similar and the main parameters showed no significant difference except t1/2. In conclusion, the fat nano-emulsion with ubenimex has potential as a safe and effective parenteral delivery system for poorly water soluble anti-cancer drugs.

主 题 词：Fat nano-emulsion Ubenimex High pressure homogenization Pharmacokinetics 

学科分类：1007[医学-药学类] 1006[医学-中西医结合类] 100706[100706] 100602[100602] 10[医学] 

D　O　I：10.5246/jcps.2011.05.061

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