促渗剂对三七中人参皂苷Rh_1体外透皮的影响  

Influence of penetration enhancers on transdermal delivery of ginsenoside Rh_1 from Panax notoginseng

作　　者：张定[1] 王承潇[1] 杨晓艳[1] 崔秀明[1] 

机构地区：[1]昆明理工大学生命科学与技术学院,云南昆明650500

出　　处：《中成药》2015年第3期511-517,共7页Chinese Traditional Patent Medicine

摘　　要：目的研究三七中人参皂苷Rh1的理化性质及其体外透皮性能。方法采用摇瓶法测定人参皂苷Rh1的表观溶解度和油/水分配系数;采用体外扩散池法测定小鼠皮和猪皮对Rh1体外经皮渗透系数以及对不同促渗剂和质量浓度对其体外经皮促渗效果;并采用高效液相色谱法对人参皂苷Rh1进行分析。结果人参皂苷Rh1的表观溶解度为(60.70±3.21)μg/mL,其油水分配系数lgP值为2.49±0.04,人参皂苷Rh1在小鼠皮上的经皮吸收性能强于猪皮,促渗剂对人参皂苷Rh1的透皮能力大小为:5%N-甲基-2-吡咯烷酮(NMP)>5%丙二醇(PG)>5%氮酮(AZ)>5%油酸(OA);不同质量浓度的促渗剂促渗能力大小为1%NMP>3%NMP>5%NMP和1%PG>3%PG>5%PG。结论人参皂苷Rh1在小鼠皮肤上具有更强通透性,且1%NMP和1%PG可作为人参皂苷Rh1经皮吸收的促渗剂。AIM To study the physical and chemical properties and in vitro transdermal delivery of ginsenoside Rh1 from Panax notoginseng（ Burk.） F.H.Chen.METHODS Shake-flask method was applied to determining the apparent solubility and oil / water partition coefficient of ginsenoside Rh1.In vitro skin permeation was conducted by means of Franz diffusion cell with pigs＇ and mice＇s skin as models.Transdermal absorption profiles of different species and concentrations of penetration enhancers were investigated and the HPLC analyses were performed.RESULTS The apparent solubility of ginsenoside Rh1 was（ 60.70 ± 3.21） μg/mL with an apparent oil /water partition coefficient of 2.49 ± 0.04.The mice＇s skin transdermal absorption was better than that of the pigs＇.NMP showed that the best skin enhancement was produced by PG,AZ and OA.Concentrations of enhancers were inverse related to the skin enhancement.The order of the permeation influence was kept as： 5% N-methyl-2-pyrrolidone（ NMP）〉 5% propylene glycol（ PG） 〉5% azone（ AZ） 〉5% oleic acid（ OA）,while the order of the enhancer concentrations in change to the transdermal delivery was 1% NMP 〉3% NMP〉 5% NMP,and1% PG 〉3% PG 〉5% PG.CONCLUSION Ginsenoside Rh1 can penetrate easily through mice＇s skin,and 1%NMP and 1% PG ensures the best penetration of ginsenosides Rh1.

关 键 词：人参皂苷RH1 三七 经皮渗透 促渗剂 

分 类 号：R969.1[医药卫生—药理学]