盐酸二甲双胍缓释片仿制药处方开发与体外溶出效果评价  

Generic Drug Formulation Development of Metformin Hydrochloride Extended-Release Tablets and in Vitro Dissolution Evaluation

作　　者：尹朋朋 许俊博 刘茜英 肖慧 王丽伟 YIN Pengpeng;XU Junbo;LIU Qianying;XIAO Hui;WANG Liwei(China Resources Double-Crane Pharmaceutical Co.,Ltd.,Beijing,China 100102)

机构地区：[1]华润双鹤药业股份有限公司,北京100102

出　　处：《中国药业》2025年第3期38-42,共5页China Pharmaceuticals

摘　　要：目的开发盐酸二甲双胍缓释片仿制药处方,并评价其体外溶出效果。方法根据二甲双胍的本身理化性质和渗透泵缓释片处方设计要求,以片芯处方中聚维酮K30的比例、十二烷基硫酸钠的比例、缓释层包衣增重为考察指标,以累计释放度为评价指标,筛选盐酸二甲双胍缓释片处方。结果筛选出的处方为,片芯中聚维酮K30、十二烷基硫酸钠的比例分别为5.0%,2.0%,缓释层包衣增重为14%~16%。自研制剂与参比制剂在pH 1.0盐酸溶液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液、水中的溶出曲线相似因子(f_(2))均超过70,12 h时的累计溶出度均超过90%。结论筛选出的盐酸二甲双胍缓释片处方符合质量要求,自研制剂与参比制剂的体外溶出效果基本一致。Objective To develop the formulation of the generic drug Metformin Hydrochloride Extended-Release Tablets,and to evaluate the in virto dissolution.Methods Based on the physical and chemical properties of metformin and the design requirements of the osmotic pump extended-release tablet prescription,the proportion of polyvinylpyrrolidone K30,sodium dodecyl sulfate,and the weight gain of the sustained-release layer coating in the tablet core prescription were taken as the evaluation indexes,and the cumulative release rate was taken as the evaluation index to screen the prescription of Metformin Hydrochloride Extended-Release Tablets.Results The selected prescription was as follows:the proportion of polyvinylpyrrolidone K30 and sodium dodecyl sulfate in the core was 5.0% and 2.0%,respectively,and the weight gain of the extended-release layer coating was in the range of 14%-16%.The similarity factor(f_(2))of the dissolution curves of the self-developed formulation and the reference prescription in pH 1.0 hydrochloric acid solution,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution,and water all exceeded 70,and the cumulative dissolution rate within 12 h exceeded 90%.Conclusion The selected prescription of Metformin Hydrochloride Extended-Release Tablets can meet the quality requirements,and the in vitro dissolution effect of the self-developed prescription is similar to that of the reference prescription.

关 键 词：盐酸二甲双胍缓释片 渗透泵 处方开发 体外溶出效果 

分 类 号：R917[医药卫生—药物分析学] R977.15[医药卫生—药学]