盐酸利多卡因凝胶剂处方优化及稳定性考察

Optimization of Lidocaine Hydrochloride Gel Formula and study on its stability

目的:考察多种渗透促进剂对盐酸利多卡因凝胶经皮渗透的影响,并从中筛选其最佳处方组成。方法:采用离体皮肤渗透实验,以渗透速率为指标,均匀设计优化处方工艺,考察不同渗透促进剂对羧甲基纤维素钠(CMC-Na)基质的凝胶剂中利多卡因的经皮渗透效果。结果:含1.5%月桂氮(?)酮,4%聚乙二醇-400,2%泊洛沙姆和25%丙二醇(PG)的盐酸利多卡因凝胶剂具有最佳的经皮渗透速率,且处方稳定,对皮肤无刺激性。结论:渗透促进剂对盐酸利多卡因经皮渗透有显著的促进作用。

Objective: To study the influence of several different permeation enhancers on transdermal permeation of lidocaine hydrochloride gel to obtain an optimal prescription. Methods: The uniform design was used to optimize the carboxymethylcellulose sodium (CMC-Na) gel formula with the permeation rate constant as the indexes in vitro Results: The gel preparation was composed of 1.5% Azone, 4% polyethylene glycol (PEG) 400, 2% Pluronic F68 and 25% propylene glycol (PG) showed the most significant permeation effect. The gel also showed a good stability and no skin irritation. Conclusion: Lidocaine was significantly absorbed across skin from gel comprised of permeation enhancers.