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目的研究三七素的理化性质及渗透促进剂对三七素体外透皮性能的影响。方法采用摇瓶法测定三七素的表观溶解度及油水分配系数;采用Franz扩散池法,以小鼠皮和猪皮为模型皮肤,采用HPLC法测定三七素,评价最佳促渗剂。结果三七素水溶性强,lg P值低,三七素在皮肤上体外释放符合Higuchi方程;在小鼠皮上的渗透效果比猪皮好;通过对促渗剂种类和用量的筛选,发现5%N-甲基-2-吡咯烷酮(NMP)促渗效果最好。结论三七素具有一定的经皮吸收能力,其经皮吸收与药物在皮肤中的扩散速率有关,5%NMP显著增加三七素经皮渗透速率。
Objective To study the physical and chemical properties of panax notoginseng and the effects of penetration enhancers on the transdermal performance of penicillin in vitro. Methods The apparent solubility and oil-water partition coefficient of penicillin were determined by shake flask method. Franz diffusion cell method was used. Mouse skin and porcine skin were used as model skins. The method was used for the determination of penicillin by HPLC and the best penetration enhancer was evaluated. RESULTS Panax notoginseng had high water solubility, low lg P value, and the release of trichosthenin on the skin complied with the Higuchi equation; penetration on mouse skin was better than that on pig skin; screening of the type and amount of penetration enhancer was found. 5% N-methyl-2-pyrrolidone (NMP) promotes the best effect. [Conclusion] There is a certain percutaneous absorption capacity of the drug, and its percutaneous absorption is related to the diffusion rate of the drug in the skin. 5% NMP significantly increases the percutaneous penetration rate of the drug.