盐酸罗哌卡因透皮凝胶剂的初步药效学研究 |
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引用本文: | 马莉熊蕊符旭东罗梦颖徐莲. 盐酸罗哌卡因透皮凝胶剂的初步药效学研究[J]. 中国药师, 2016, 0(8): 1459-1462 |
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作者姓名: | 马莉熊蕊符旭东罗梦颖徐莲 |
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作者单位: | 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 |
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基金项目: | 湖北省自然科学基金项目(编号:2013CFB430) |
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摘 要: | 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。
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关 键 词: | 盐酸罗哌卡因;透皮凝胶;镇痛作用;皮肤刺激性 |
收稿时间: | 2016-03-01 |
修稿时间: | 2016-04-18 |
Pharmacodynamic Study of Ropivacaine Hydrochloride Transdermal Gel |
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Abstract: | 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. |
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Keywords: | Ropivacaine hydrochloride Transdermal gel Analgesic effect Skin irritation |
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