盐酸罗哌卡因透皮凝胶剂的处方优化  

Formula Optimization of Ropivacaine Hydrochloride Transdermal Gel

作　　者：熊蕊[1,2] 符旭东[1] 罗梦颖 徐莲[1,2] 

机构地区：[1]广州军区武汉总医院药剂科,武汉430070 [2]湖北中医药大学药学院

出　　处：《中国药师》2016年第4期660-664,共5页China Pharmacist

基　　金：湖北省自然科学基金项目(编号:2013CFB430)

摘　　要：目的:筛选盐酸罗哌卡因透皮凝胶剂的最佳处方。方法:以盐酸罗哌卡因凝胶的稳态透皮速率和24 h累积透皮率为考察指标,采用3因素3水平进行正交试验设计,并采用Design Expert 8.0.5.0软件对试验结果进行分析,确定最佳处方。结果:最佳处方的组成为:卡波姆2%,丙二醇10%,氮酮5%。以最佳处方制得的凝胶稳态透皮速率为0.695 1 mg·h^(-1)·cm^(-2),24 h累积透皮率为91.04%,与相同浓度的盐酸罗哌卡因药物溶液相比,24 h累积透皮率提高了22.79%。Design Expert 8.0.5.0软件对最佳处方的稳态透皮速率和24 h累积透皮率预测值良好。结论:该处方设计合理,性质良好,适合作为皮肤局部用药。Objective： To optimize the formula of ropivacaine hydrochloride transdermal gel. Methods： The steady transdermal rate and cumulative transdermal percentage in 24 h of ropivacaine hydrochloride gel were used as the indices,an orthogonal design was applied to select the optimal formula,and Design Expert 8.0.5.0 software was used to analyze the results. Results： The optimal formula contained 2% carbomer,10% propylene-glycol and 5% Azone. The steady transdermal rate of the optimal formula was 0.6951 mg·h^（-1）·cm^（-2）. The cumulative transdermal percentage in 24 h of the optimal formula was 91.04%,which was 22.79% higher than that of ropivacaine hydrochloride solution with the same concentration. Design Expert 8.0.5.0 software could predict the steady transdermal rate and cumulative transdermal percentage in 24 h of the optimal formula. Conclusion： The preparation design is reasonable,and the gel has promising properties,which is suitable for skin local application.

关 键 词：盐酸罗哌卡因 凝胶 正交设计 经皮给药 

分 类 号：R944.9[医药卫生—药剂学]