目的: 对川乌凝胶贴膏初粘力、剥离度最优范围及适宜载药量进行分析。方法: 随机选购市售8 种不同生产厂家、不同品质等级的凝胶贴膏, 从感观、初粘力、持粘力、剥离度4 个方面进行质量再评价;以单因素实验与混料设计实验对川乌凝胶贴膏的基质处方配比进行筛选, 分别制备川乌提取物载药量120、240、480、960 mg 的凝胶贴膏;以48 只昆明清洁级小鼠为研究对象, 随机分为6 组, 每组各8 只, 分别给予空白凝胶贴膏（模型组）、吲哚美辛凝胶贴膏（阳性组）以及120（实验A 组）、240（实验B 组）、480（实验C 组）、960 mg（实验D 组）的川乌凝胶贴膏给药, 通过小鼠醋酸扭体实验评价最优川乌载药量。结果: 8 个品牌的凝胶贴膏质量再评价的差异较大, 整体来看, 初粘力、持粘力与剥离度越大, 凝胶贴膏的揭贴性等感观评价越差;根据试验结果凝胶贴膏的最优配方为: 聚丙烯酸钠3%, 羧甲基纤维素钠1. 5%, 硅藻土4%, 甘油25%。通过小鼠醋酸扭体实验可见, 每贴川乌凝胶贴膏载药量为480、960 mg 时, 小鼠扭体潜伏期越短, 扭体次数越小, 镇痛率越高, 综合考虑到安全性等因素, 认为载药量为480 mg 的川乌凝胶贴膏更加适宜应用于临床。结论: 川乌凝胶贴膏的制备在保证镇痛、抗炎效果的同时, 还应该充分考虑到其外观、追随性、揭帖性、安全性等特征, 将其初粘力、剥离度、载药量控制在适宜范围内, 以促进其在临床的高效、合理应用。
Objective: To analyze the optimum range of initial adhesive force, stripping degree and suitable drug loading of Sichuan Wu gel patch. Methods: Eight kinds of gel patch from different manufacturers and grades of quality were randomLy selected for quality reevaluation from four aspects: perception, initial adhesion, adhesion and peel. Single factor experiment and mixing the material design experiment was conducted to screen the base 240 mg, 480 mg and 960 mg were prepared respectively;48 Kunming clean-grade mice were used as the research subjects were randomLy divided into 6 groups, 8 in each group, and were given blank gel patch（model group）, indomethacin gel patch（positive group）and 120 mg（experiment A）and 240 mg（experiment B）Group）, 480 mg （experiment C）, 960 mg(experiment D） of Chuanwu gel patch, and the optimal dose of Chuanwu was evaluated by the mouse acetic acid writhing experiment. Results: The re-evaluation of the quality of the gel patch of the eight brands was quite different. Overall, the greater the initial adhesion, the holding force and the peeling degree, the worse the sensory evaluation of the gel patch;according to the test results, the optimal formula of the gel patch is: sodium polyacrylate 3%, sodium carboxymethyl cellulose 1. 5%, diatomaceous earth 4%, glycerin 25%. It could be seen from the mouse acetic acid writhing experiment that when the drug loading of each chuanwu gel patch was 480 mg and 960 mg, the shorter the incubation period of the mouse writhing, the smaller the number of writhing, the higher the analgesic rate, taking into account safety and other factors, it was believed that Chuanwu gel patch with a drug loading of 480 mg was more suitable for clinical application. Conclusion: The preparation of Chuanwu gel patch should not only ensure its analgesic and anti-inflammatory effects, but also give full consideration to its appearance, follow-up, placardability, safety and other characteristics, and control its initial adhesion, peeling degree, and drug loading within an appropriate range to promote its efficient and reasonable application in the clinic.
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