氧化苦参碱凝胶体外经皮渗透及大鼠药动学研究  

Transdermal Permeation of Oxymatrine Gel in Vitro and Its Pharmacokinetics in Rats

作　　者：何治芬 汤湛[1] 尹丽娜[1] 王胜浩[1] 金志敏[2] 王俏[1] 

机构地区：[1]浙江省医学科学院药物研究所,杭州310013 [2]浙江工业大学药学院,杭州310014

出　　处：《中国现代应用药学》2015年第11期1336-1342,共7页Chinese Journal of Modern Applied Pharmacy

基　　金：浙江省医学重点学科群项目(XKQ-010-001);2010年浙江省"新世纪151人才工程"二层次

摘　　要：目的研究氧化苦参碱凝胶的体外经皮渗透影响因素,并对其在大鼠体内的药动学进行研究。方法采用Valia-Chien双室扩散池,以大鼠离体皮肤为渗透屏障,HPLC测定氧化苦参碱浓度,以药物累积渗透量为指标,对药物及渗透促进剂的浓度进行筛选。结果氧化苦参碱经皮凝胶的最优处方12 h累积渗透量为(18.094±1.253)mg·cm?2,大鼠静注与经皮给药的血浆药动学研究表明,经皮给药的AUC(0-t)是注射给药的1.9倍(P<0.01)。结论氧化苦参碱凝胶的经皮吸收能力良好,能长时间持续释放药物,有望成为新的给药剂型。OBJECTIVE To investigate in vitro transdermal permeation ability of oxymatrine gel and its pharmacokinetics in rats. METHODS The skin permeation ability of oxymatrine was evaluated by using Valia-Chien permeation cells with isolated rat skin. The concentration of drug was determined by HPLC. The preparation formulation of the gel was optimized which took the permeation amount as the index. RESULTS The accumulative permeation amount of the optimal formulation of gel was（18.094±1.253）mg·cm^-2 in 12 h. The pharmacokinetic parameters showed that the AUC（0-t） of transdermal administration was 1.9 times of iv adminirtration. CONCLUSION Oxymatrine gel has good absorption and long-time substained release, it can be developed as a novel transdermal preparation.

关 键 词：氧化苦参碱 凝胶 水溶性氮酮 经皮渗透 药动学 

分 类 号：R969.1[医药卫生—药理学] R944.15[医药卫生—药学]