复方利多卡因乳膏体外经皮渗透比较研究  

Comparison of the in vitro percutaneous penetration of compound lidocaine cream

作　　者：李金红 贺亚静[2,3] 贺吉香[2] 周洁[2,3] 沈腾[3] 

机构地区：[1]陕西兴邦药业有限公司,西安710000 [2]山东中医药大学药学院,济南250355 [3]复旦大学药学院药剂学教研室智能化递药教育部重点实验室,上海201203

出　　处：《中国新药杂志》2015年第13期1541-1545,共5页Chinese Journal of New Drugs

摘　　要：目的：评价复方利多卡因乳膏供试药和对照药皮肤透皮率和贮留率的一致性。方法：采用HPLC-UV测定利多卡因和丙胺卡因样品浓度;采用巴马小香猪离体猪皮和改良Franz扩散池进行体外渗透试验。结果：利多卡因和丙胺卡因于0.3~6.0μg·m L-1浓度范围内与峰面积的线性关系良好;两药HPLC测定的回收率和精密度符合方法学的要求;供试药中利多卡因经猪皮1和2 h的透皮率分别为0.113%和0.519%,对应贮留率分别为1.219%和1.794%;供试药中丙胺卡因经猪皮1和2 h的透皮率分别为0.096%和0.439%,对应贮留率分别为0.982%和1.564%;供试药中两药1和2 h的透皮率和贮留率与对照药比较无显著性差异（P〉0.05）。结论：供试药复方利多卡因乳膏的皮肤透皮率和贮留率与对照药Emla乳膏是一致的。Objective： To compare the consistency in skin permeation and retention of compound lidocaine cream with control cream. Methods： The concentrations of lidocaine and prilocaine in samples were quantified by HPLC. The in vitro penetration experiments of compound lidocaine cream were performed using Bama miniature pig skin and modified Franz’s cell. Results： A good linear relationship was observed between peak area and concentration of lidocaine and prilocaine over a range of 0. 3 ~ 6. 0 μg·m L-1. The recovery and precision of two drugs met method system suitability requirements. The extents of 1 h and 2 h percutaneous absorption of lidocaine through pig skin from test compound cream were 0. 113% and 0. 519%,and the respective retention rates in skin were1. 219% and 1. 794%. The extents of 1 h and 2 h percutaneous absorption of prilocaine through pig skin from test compound cream were 0. 096% and 0. 439%,and the respective retention rates in skin were 0. 982% and1. 564%. There were no significant difference（ P 〉 0. 05） in 1 h and 2 h percutaneous absorption and retention rate of the two drugs between test and control compound creams. Conclusion： The skin penetration and skin retention of lidocaine and prilocaine from test compound lidocaine cream are consistent with thoof control Emlacream.

关 键 词：复方利多卡因乳膏 丙胺卡因 透皮率 贮留率 体外渗透试验 

分 类 号：R944.21[医药卫生—药剂学]