Box-Behnken设计-响应面法优化盐酸苯环壬酯透皮贴剂的处方

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48 h累积透皮量为(119.48±2.95)μg/cm2(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)μ g/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.