湿疹乳膏离体透皮与释药特性试验研究  

Experimental study on eczema cream in vitro transdermal absorption and release properties

作　　者：何群[1] 肖海英[1] 杨鹏 陈光宇[1] 彭思源[1] 颜学军[1] 钟鸣[1] 谢名君 

机构地区：[1]湖南中医药大学药学"十二五"重点学科,长沙410208 [2]湖南省药物安全评价研究中心,长沙410331

出　　处：《中华中医药杂志》2015年第6期2118-2123,共6页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金："十一五"国家科技支撑计划项目(No.2008BAI53B042)~~

摘　　要：目的:通过研究湿疹乳膏透皮与释药两个过程的药物动力学特性,为湿疹乳膏药效、毒理试验及临床给药方案设计研究提供理论依据。方法:以有效成分丹皮酚、苦参碱及氧化苦参碱、盐酸小檗碱累积透皮百分率为测定指标,用改良的Franz扩散池及离体猪耳皮进行实验,高效液相测定不同时间透皮接收液中各成分的含量。比较透皮与释药速度、透皮量与释药量及各成分皮肤储量的差别。结果:湿疹乳膏释药速度快于透皮速度,释药速度(t50%)是透皮速度的2倍以上;释药量高于透皮量,最大释药量是透皮量(Qmax)的2倍以上,皮内储存量(以丹皮酚计)占透皮总量的50%以上。结论:湿疹乳膏属于皮肤限速型乳膏,基质对药物的透皮有促进作用,各项透皮参数可满足湿疹局部治疗需要,透皮特性达到临床局部治疗目的;每天用药1次或给药间隔时间确定为15.16-28.40h,科学、合理、可行。Objective： To provide a theoretical basis for eczema cream on the toxicological test and the clinical efficacy and the clinical dosage regimen design, by studying the pharmacokinetics characteristics of eczema creams on the transdermal and release processes. Methods： Transdermal cumulative percentage of effective constituent Dan phenol, Matrine, Oxymatrine, Berberine hydrochloride as measurement indicators, improved Franz diffusion cell and excised pig ear skin were used for the experiment, and each component of transdermal receiving liquid in different time was determine by HPLC. The differences of the transdermal and release rate, the transdermal and release quantity, and the skin reserves quantity of each component were compared. Results： The release speed of eczema cream was higher than that of transdermal speed, and more than 2 times higher as its transdermal speed. The drug release was higher than that of transdermal flux. The Maximum release amount was more than 2 times as the amount of transdermal （Qmax）. The intradermal storage capacity （with paeonol meter） accounted for more than 50% of the total amount of transdermal. Conclusion： Eczema cream was a rate limiting skin cream, and its matrix had a promoting effect on trausdermal absorption of drug. The transdermal parameters could meet the needs of local treating in eczema cream, and its transdermal permeability reached clinical purpose local treatment; when administered once daily or dosing interval was determined as 15.16-28.40h, was scientific, reasonable, feasible.

关 键 词：湿疹乳膏 离体透皮试验 高效液相色谱法 丹皮酚 苦参碱及氧化苦参碱 盐酸小檗碱 FRANZ扩散池 累积透皮百分率 

分 类 号：R285[医药卫生—中药学]