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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 transdermal gel. Methods: The analgesic effect of 1%, 3% and 5% transdermal ropivacaine HCl hydrochloride solution to mice at different time points was investigated by hot plate method and acetic acid writhing method. Results: 1%, 3%, 5% ropivacaine hydrochloride transdermal gel can significantly increase the pain threshold of hot plate method mice, and significantly inhibit acetic acid induced writhing reaction in mice (P <0.01 or P <0.05). The drug-loaded gel has a dose-effect relationship with the analgesic effect of mice. With the increase of ropivacaine concentration, the analgesic effect is enhanced and the analgesic duration is prolonged. The transdermal coagulation of 5% ropivacaine hydrochloride Adhesive sustained analgesia 24 h. Different concentrations of ropivacaine hydrochloride transdermal gel on the skin no significant irritation. Conclusion: 5% ropivacaine hydrochloride transdermal gel has obvious analgesic effect and maintains for a long time, which is basically in line with the design requirements of once-daily administration.