盐酸苯环壬酯透皮贴剂的制备及体外释放特性考察  

Study on the preparation of phencynonate hydrochloride transdermal patch and release character in vitro

作　　者：廖诗琴 刘辉[1,2] 赵静[1,3] 王彦辰[1,3] 郭真君 LIAO Shiqin;LIU Hui;ZHAO Jing;WANG Yanchen;s;GUO Zhenjun(Department of Pharmacy,Wuhan General Hospital of People＇s Liberation Army,Wuhan 430070,China;College of Pharmacy,Southern Medical University,Guangzhou 510515,China;College of Pharmacy,Hubei University of Chinese Medicine,Wuhan 430065,China)

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

出　　处：《沈阳药科大学学报》2018年第9期719-724,728,共7页Journal of Shenyang Pharmaceutical University

基　　金：国家"十二五"重大新药创制科技重大专项经费资助课题(2013ZX09J13109-05C)

摘　　要：目的制备盐酸苯环壬酯透皮贴剂并对其体外释放进行研究。方法以丙烯酸酯压敏胶Duro-Tak87-2677为基质材料,采用有机溶剂挥发法制备盐酸苯环壬酯透皮贴剂。基本制备工艺:搅拌速度为120 r·min^(-1),干燥温度为40℃、干燥时间为10 min,涂布厚度为0.40 mm;采用高效液相色谱法测定盐酸苯环壬酯透皮贴剂的体外释放度,色谱柱:Diamonsil C_(18)(250 mm×4.60 mm,5μm)柱,流动相:乙腈-水-磷酸-三乙胺(体积比240∶400∶1.1∶2.2);检测波长:220 nm;流速:1.0 mL·min^(-1);柱温:30℃;进样量:20μL。结果建立的体外释放度测定方法:采用浆碟法,以体积分数20%乙醇-生理盐水为释放介质,转速为50 r·min^(-1),该方法盐酸苯环壬酯在质量浓度0.2~6 mg·L^(-1)内线性良好。盐酸苯环壬酯透皮贴剂的释放行为符合Higuchi释放曲线,回归方程为Q=4.840 7t^(1/2)+8.686 1,R^2=0.970 4。结论盐酸苯环壬酯透皮贴剂制备工艺稳定,建立的释放度测定方法可用于盐酸苯环壬酯透皮贴剂的质量控制。Objective To prepare the phencynonate hydrochloride transdermal patch and study the release properties. Methods The phencynonate hydrochloride transderrnal patch was prepared by solvent evaporation method, and acrylic pressure sensitive adhesive of Duro-Tak87-2677 as a matrix. The basic preparation conditions were as follows：stirring speed at 120 r .min-1 ,drying at 40 ℃ for 10 rnin,the coating thickness of 0.40 mm. The release was determined by high performance liquid chromatography （HPLC）. The HPLC method was used with Diamonsil C18 chromatographic column （250 mm×4.60 mm,5 μm）,acetonitrile- water-phosphoric acid-triethylamine （ volume ratio 240： 400＂ 1.1＂ 2.2 ） as the mobile phase. The detective wavelength was 220 nm;flow rate was 1.0 mL · min-1, the column temperature was 30℃ and injection volume was 20 μL. Results The in vitro release percent of phencynonate hydrochloride transdermal patch was determined by pulp plate method, 20% ethanol physiological saline as the dissolution medium, and the rotation speed was 50 r · min - 1 Linearity was obtained over the concentration range of 0. 2 - 6 mg · L - 1. The release behavior of the transdermal patch was in accord with Higuchi equation, the regression equation was, Q = 4.840 7t1/2 ＋ 8. 686 1, the average recovery （ n = 9 ） was 0. 970 4. Conclusion The preparation process of phencynonate hydrochloride transdermal patch is stable. The drug release determining method is simple and reproducible, and it can be used for the quality control of phencynonate hydrochloride transdermal patch.

关 键 词：盐酸苯环壬酯 透皮贴剂 有机溶剂挥发法 释放度 HPLC 

分 类 号：R94[医药卫生—药剂学]