具有区分力的甲磺酸地拉韦啶片体外溶出度方法研究  

Development of Discriminatory Dissolution Methods for Delavirdine Mesylate Tablets

作　　者：方婷 王东凯[2] 魏斌斌[1] 孙婷[2] FANG Ting;WANG Dong-kai;WEI Bin-bin;SUN Ting(School of Pharmacy,China Medical University,Shenyang 110122,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]中国医科大学药学院,沈阳110122 [2]沈阳药科大学药学院,沈阳110016

出　　处：《中国药学杂志》2021年第11期929-935,共7页Chinese Pharmaceutical Journal

摘　　要：目的建立并验证具有区分力的甲磺酸地拉韦啶片(100 mg)体外溶出方法,为仿制药的开发提供参考。方法建立了测定甲磺酸地拉韦啶片HPLC的体外溶出度方法,通过原料药的溶解性以及原研药品和自制制剂在pH 1.2、pH 4.5[4 mg·mL-1十二烷基硫酸钠(SDS)]、pH 6.0(4 mg·mL-1 SDS)和水(4 mg·mL-1 SDS)中的溶出行为,采用相似因子(f2)法评价溶出行为的相似性,筛选出具有区分力的溶出方法。结果自制制剂B与原研药品在4种介质中溶出行为相似(f2均大于50),自制制剂A、C、D在4种介质中均存在f2小于50的情况。结论采用桨法50 r·min-1在pH 4.5(0.4%SDS)、pH 6.0(0.4%SDS)和水(0.4%SDS)中测定本品溶出度具有一定区分力。OBJECTIVE To establish and validate the discriminating dissolution methods of delavirdine mesylate tablets(100 mg)in vitro,which provided reference for the development of generic drugs.METHODS High performance liquid chromatography(HPLC)was used to establish the methods for the determination of the dissolution of delavirdine mesylate tablets.The solubility of delavirdine mesylate in different pH solutions were measured.The dissolution curves of RESCRIPTOR®(100 mg)and self-made tablets were determined in pH 1.2,pH 4.5(4 mg·mL-1 SDS),pH 6.0(4 mg·mL-1 SDS)and water(4 mg·mL-1 SDS)four media,f2 similarity factor method was used to evaluate the similarity of dissolution curves.RESULTS The dissolution curves were similar between self-made tablet B and brand-name drugs in four different media(f2 were greater than 50),while the f2 of self-made tablet A,C,D in four media were not all greater than 50.CONCLUSION The discriminatory dissolution methods of delavirdine mesylate dispersible tablets are determined by paddle method,50 r·min-1 rotation speed,the medium are pH 4.5 acetate buffer(4 mg·mL-1 SDS),pH 6.0 phosphate buffer(4 mg·mL-1 SDS)and water(4 mg·mL-1 SDS).

关 键 词：甲磺酸地拉韦啶片 原研药品 自制制剂 溶出度 区分力 相似因子法 

分 类 号：R944[医药卫生—药剂学]