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奥沙利铂长循环热敏脂质体的包封率测定及体外释放考察 被引量:10

Determination of entrapment efficiency of oxaliplatin liposome and its release profile in vitro
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摘要 目的:建立奥沙利铂脂质体的包封率和含量测定方法,并对其体外释放进行考察。方法:采用逆相蒸发法制备奥沙利铂脂质体,用葡聚糖凝胶G-50柱分离载药脂质体和游离药物,以水为洗脱液,RP-HPLC法测定包封率,采用透析法考察脂质体在37℃和41℃的体外释放规律。结果:柱层析分离方法的药物回收率为99.25%,柱加样回收率为100.37%;药物含量测定方法的工作曲线为A=3E+06 c-3290.8(n=5),r=0.9999,线性范围0.0201-2.0100 mg/m l,方法回收率为100.70%;脂质体在41℃条件下的释放规律符合一级动力学过程。结论:本方法简便、灵敏、准确,可以用于测定奥沙利铂脂质体的含量和包封率,所制得的脂质体具有明显的热敏释放特征。 Objective: To establish an HPLC method for determination of entrapment efficiency and content of oxaliplatin liposome and study its release profile in vitro. Methods:The reverse-phase evaporation vesicles (REV) method was used to prepare oxaliplatin liposome. The liposome and free oxaliplatin were separated by Sephadex G-50 chromatography and the eluent was H20. RP-HPLC was Used to determine the entrapment efficiency. The release behavior of the drug from liposome at 37℃ and 41 ℃ was studied by the dialysis method. Results:The drug recovery and the sample recovery of Sephadex G-50 chromatography were 99.25% and 100.37% ,respectively. The regression equation was A = 3E + 06c-3290.8 (n = 5 )and was linear in the range of 0. 0201 -2.0100 mg,/ml. The correlation coefficient was 0.9999. The release profile at 41 ℃ in vitro conformed to the first order model. Conclusion: The method is convenient, sensitive, accurate, and suitable for determining the content of oxaliplatin and entrapment efficiency of oxaliplatin liposome. The prepared liposomes are temperature sensitive.
出处 《军事医学科学院院刊》 CSCD 北大核心 2007年第5期448-450,共3页 Bulletin of the Academy of Military Medical Sciences
关键词 奥沙利铂 脂质体 包封率 葡聚糖凝胶 柱层析 oxaliplatin liposome entrapment efficiency Sephadex chromatography
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