天山雪莲微乳的小鼠局部药代动力学

Local Pharmacokinetic of Saussurea involucrata Microemulsion in Rat

目的:制备天山雪莲微乳,考察天山雪莲微乳在小鼠腹部皮肤滞留量与时间的关系及其局部经皮给药的药代动力学,探讨其皮肤吸收作用。方法:测定制备样品的Zeta电位、多分散指数、粒径分布等理化指标;以绿原酸、芦丁为指标性成分,采用HPLC测定不同给药时间皮肤中绿原酸、芦丁生物滞留量,DAS软件拟合药物动力学参数。结果:天山雪莲微乳平均粒径54.51 nm,多分散系数0.281,Zeta电位-0.687 mV;在小鼠皮肤中滞留量的动力学过程符合二室模型。结论:天山雪莲微乳中有效成分能较快渗透进入皮肤,并在皮肤局部较长时间蓄积。

retention volume pharmacokinetics Objective： To prepare Saussurea involucrata microemulsion, investigate relationship between and time of of S. involucrata microemulsion in abdominal skin of mice, investigate its of local transdermal drug delivery, and investigate its skin absorption effect. Method：Characteristics of prepared S. involucrata microemulsion were determined including polydispersity index, size distribution and Zeta potential and other physical and chemical properties. With chlorogenic acid and rutin as indexes, biological retention volume of chlorogenic acid and rutin in administration skin with different time was determined by HPLC~ and pharmacokinetic parameters were fitted by I）AS software. Result： Characteristics of prepared S. involucrata microemulsion including mean particle size, polydispersity index and Zeta potential were 54.51 nm, 0. 281 and-0. 687 mV. Pharmacokinetic process of microemulsion in rats＇ abdominal skin was fitted with two compartment model. Conclusion： Active ingredients of S. involucrata microemulsion could quickly permeate into skin, and accumulate long time in local skin.