葛根素脂质体包封率测定及制备工艺优化

摘要

Objective:To prepare puerarin liposome and establish a method to determine its entrapment efficiency. Methods:Puerarin liposome was prepared through the way of flim dispersion. An optimal technique was chosen with orthogonal design. The entrapment efficiency of puerarin liposome was determined by dialysis method with UV for analyzing the amount of puerarin. Results:The optimal prescription was soy lecithin:cholesterol=2:1 (m: m), soy lecithin:puerarin =12:1 (m:m). The calibration curve was linear(r=0.9999) in the range of 2.0-10.0 mg/L for puerarin, and the RSDs of the intra-day and inter-day were less than 2%. The recoveries of free drug were 98.0%~99.9% which met the requirements. The leaking percentage in 24h was neglectable in the process of the dialysis which had no effect on determination. Conclusion:Film dispersion method can prepare puerarin liposome with high entrapment efficiency. Dialysis method is convenient and suitable for determining the entrapment efficiency of puerarin liposome.%目的 制备葛根素脂质体并建立其包封率的测定方法.方法 采用薄膜分散法制备葛根索脂质体,正交设计优化处方.利用透析法分离脂质体和游离药物,采用紫外分光光度法测定葛根索脂质体的包封率,在250nm处测定脂质体中的含药量.结果 最优处方为:大豆卵磷脂:胆固醇=2∶1(m∶m),大豆卵磷脂∶葛根素=12∶1(m∶m)；葛根素质量浓度在2.0～10.0mg/L范围内线性关系良好；低、中、高3种质量浓度的日内和日间RSD均小于2％；游离药物回收率为98.0％～99.9％,符合要求；空白脂质体透析24h内无渗漏,对葛根素质量浓度测定无影响.结论 薄膜分散法可制备出包封率较高的葛根素脂质体;透析结合紫外分光光度法简便可行,可用于葛根素脂质体包封率的测定.