中国临床药学杂志

目的制备三七总皂苷复方脂质体凝胶剂,并进行体外透皮吸收研究。方法以薄膜分散法制备脂质体,通过正交实验设计优化三七总皂苷复方脂质体的处方,再以卡波姆为基质制成凝胶剂。通过智能透皮试验仪,进行体外透皮实验,研究三七总皂苷中人参皂苷Rg₁及β-蜕皮激素的体外透皮吸收情况,并采用HPLC法检测透过及滞留在皮肤内的Rg₁和β-蜕皮激素量。结果卵磷脂与胆固醇用量比为9:1,Rg₁质量浓度为40 g·L^-1β-蜕皮激素质量浓度为3g·L^-1,脂药比为5:1时的处方为最佳脂质体处方,卡波姆-934重量比为1%时,药物的皮肤滞留量最大。结论将三七总皂苷制备成复方脂质体凝胶剂,能够增加药物的皮肤滞留量,提高药物在皮肤局部的生物利用度。

AIM To prepare saponins of panax notoginseng(PNS)/β-ecdysone(EDS)compound liposomal gel and study the drug percutaneous absorption in vitro.METHODS The PNS/EDS compound liposomes were prepared by the film-dispersion method.The compound liposome formulation was optimized by the orthogonal experimental design and car- bomer was added as a supportive base for the preparation of liposomal gel.Drug permeation tests were performed through excised rat skin in diffusion ceils.RESULTS The final liposomal formulation was as follows:lecithin:cholesterin=9: 1,Rg₁ content was 40 g·L^-1,EDS content was 3g·L^-1,lipid:drug=5:1,and the highest accumulative drug concen- tration in the skin was obtained when the content of carbopol was 1%.CONCLUSION The liposomal gel has the ability to increase the drug concentration in the excised rat skin,which can improve the bioavailability of the local skin.