Box-Behnken设计-响应面法优化盐酸苯环壬酯透皮贴剂的处方  

Optimization of Phencynonate Hydrochloride Transdermal Patch Formulation by Box-Behnken Design-response Surface Methodology

作　　者：廖诗琴 刘辉[1,2] 赵静[2,3] 王彦辰[2,3] 郭真君 LIAO Shiqin;LIU Hui;ZHAO Jing;WANG Yanchen;GUO Zhenjun(College of Pharmacy,Southern Medical University,Guangzhou 510515,China;Dept.of Pharmacy,Wuhan General Hospital of PLA,Wuhan 430070,China;College of Pharmacy,Hubei University of TCM,Wuhan 430065,China)

机构地区：[1]南方医科大学药学院,广州510515 [2]中国人民解放军武汉总医院药剂科,武汉430070 [3]湖北中医药大学药学院,武汉430065

出　　处：《中国药房》2018年第7期897-901,共5页China Pharmacy

基　　金：国家"十二五"重大新药创制科技重大专项经费资助项目(No.2013ZX09J13109-05C)

摘　　要：目的:优化盐酸苯环壬酯透皮贴剂的处方。方法:采用有机溶剂挥发法制备盐酸苯环壬酯透皮贴剂。以48 h的累积透皮量为指标,采用单因素试验和Box-Behnken设计-响应面法优化处方中投药量、透皮吸收促进剂氮酮用量、压敏胶用量,并对最优处方所制贴剂的外观和黏附力进行评价。结果:最优处方为投药量263 mg、氮酮165 mg、压敏胶1.94 g、甲醇1.6 g,所制贴剂的48h累积透皮量为(119.48±2.95)μg/cm^2(n=5),与预测值的相对误差为2.48%;其表面平整光洁、切口光滑,黏附力较好。结论:成功制得盐酸苯环壬酯透皮贴剂,其累积透皮量达到预期标准。OBJECTIVE:To optimize the formulation of Phencynonate hydrochloride transdermal patch.METHODS:Phencynonate hydrochloride transdermal patch was prepared by solvent evaporation method.Using 48 h accumulative transdermal volume as index,single factor test and Box-Behnken design-response surface methodology were used to optimize drug dosage,the amount of transdermal enhancers azone and pressure-sensitive adhesive,and evaluate the appearance,adhesion of the formulation prepared by the best prescription.RESULTS:The optimized formulation was as follows as 263 mg drug dosage,165 mg azone,1.94 g pressure-sensitive adhesive and 1.6 g methanol.48 h accumulative transdermal volume of prepared patch was(119.48±2.95)μg/cm2(n=5),related error of which to predicted value was 2.48%.The prepared patch showed smooth surface and incision,good adhesiveness.CONCLUSIONS:Phencynonate hydrochloride transdermal patch is prepared successfully,its accumulative transdermal volume is in agreement with predicted standard.

关 键 词：盐酸苯环壬酯 透皮贴剂 累积透皮量 Box-Behnken设计-响应面法 处方优化 

分 类 号：R943[医药卫生—药剂学]