盐酸罗哌卡因透皮凝胶剂的初步药效学研究

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。

Pharmacodynamic Study of Ropivacaine Hydrochloride Transdermal Gel

ABSTRACT 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 24h. 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.