盐酸罗哌卡因透皮凝胶剂的初步药效学研究  

Pharmacodynamic Study of Ropivacaine Hydrochloride Transdermal Gel

作　　者：马莉[1] 熊蕊 符旭东[2] 罗梦颖 徐莲[2] 

机构地区：[1]广州军区广州总医院,广州510010 [2]广州军区武汉总医院 [3]长江航运总医院,武汉脑科医院

出　　处：《中国药师》2016年第8期1459-1462,共4页China Pharmacist

基　　金：湖北省自然科学基金项目(编号:2013CFB430)

摘　　要：目的:初步评价盐酸罗哌卡因透皮凝胶剂的镇痛作用以及对皮肤的刺激性。方法:采用热板法和醋酸扭体法考察给药后不同时间点1%、3%和5%的盐酸罗哌卡因透皮凝胶对小鼠的镇痛作用。结果:1%、3%、5%的盐酸罗哌卡因透皮凝胶均能显著提高热板法小鼠的痛阈,显著抑制醋酸引起的小鼠疼痛扭体反应(P<0.01或P<0.05)。载药凝胶对小鼠的镇痛作用具有一定的量效关系,随着罗哌卡因浓度的增加,镇痛作用加强,镇痛持续时间延长,其中5%盐酸罗哌卡因透皮凝胶可持续镇痛24 h。不同浓度的盐酸罗哌卡因透皮凝胶剂对皮肤均无明显的刺激性。结论:5%的盐酸罗哌卡因透皮凝胶具有明显的镇痛作用且维持时间长,基本符合每天给药1次的设计要求。Objective： To evaluate the analgesic effect and skin irritation of ropivacaine hydrochloride（ RP-HCl） transdermal gel.Methods： The analgesic effects at different time points after the administration of 1%,3% and 5% RP-HCl transdermal gel in mice were investigated by the hot plate method and the writhing model induced by acetic acid. Results： The transdermal gel containing 1%,3% and 5% RP-HCl could significantly improve the pain valve of mice in the hot plate test and inhibit the writhing reaction induced by acetic acid（ P 〈0. 01 or P 〈0. 05）. RP-HCl transdermal gel showed certain analgesic effect in a dose-dependent manner. With the content increase of RP-HCl in the gel,the intensity and the duration of pain relief were both improved. 5% RP-HCl transdermal gel could prolong the analgesic effect to 24 h. RP-HCl transdermal gel showed no apparent skin irritation. Conclusion： 5% RP-HCl transdermal gel has a distinct analgesic effect for a long time with no obvious skin irritation,and it meets the design demand for the administration of once a day.

关 键 词：盐酸罗哌卡因 透皮凝胶 镇痛作用 皮肤刺激性 

分 类 号：R965.1[医药卫生—药理学]