自制盐酸二甲双胍缓释片及原研药格华止XR体外释放一致性探究.docVIP

自制盐酸二甲双胍缓释片及原研药格华止XR体外释放一致性探究 　　摘 要 目的：比较自制盐酸二甲双胍缓释片与原研药格华止XR（Glucophage XR， 500 mg/片）的体外释放一致性。方法：使用羟丙甲纤维素和羧甲基纤维素钠为缓释材料，先将盐酸二甲双胍与羧甲基纤维素钠混匀，加入润湿剂80%乙醇溶液，制粒，过20目筛，干燥，整粒。再将干燥后的颗粒与羟丙甲纤维素等混匀，加入硬脂酸镁，压制成片。比较制得的盐酸二甲双胍亲水凝胶缓释骨架片与默克-雪兰诺公司生产的格华止XR的片剂性质，并分别采用使用pH介质的中国药典桨法和使用生物相关介质的美国药典往复筒法进行体外释放度的检测与比较。结果与结论：使用羟丙甲纤维素和羧甲基纤维素钠制备的盐酸二甲双胍缓释片与格华止XR的片剂物理性质和体外释放行为极其相似 关键词 盐酸二甲双胍缓释片 羟丙甲纤维素 羧甲基纤维素钠 亲水凝胶缓释骨架片 中图分类号：R927.11 文献标识码：A 文章编号：1006-1533（2017）05-0007-04 Study on in vitro drug release consistency between homemade metformin hydrochloride extended release tablet and its reference listed drug Glucophage XR YANG Jirong*， ZHU Ying （Department of Technique， Shanghai Colorcon Co. Ltd.， Shanghai 201108， China） ABSTRACT Objective： To compare the in-vitro drug release consistency between homemade metformin hydrochloride extended release tablet and its reference listed drug Glucophage XR （500 mg）. Methods： Metformin hydrochloride extended release tablets were manufactured by taking hydroxypropyl methylcellulose （HPMC， Methocel K100M） and sodium carboxymethyl cellulose （CMC-Na） as drug dissolution rate control polymers and 80% alcohol as a wet agent by granulation， screening and drying， then by blending the dried granule with HPMC and MCC-Na until uniform and finally by adding magnesium stearate and pressing tablets. The properties of tablets were compared between homemade metformin hydrochloride extended release tablet and Glucophage XR and the drug release profiles were also compared by paddle method in four different pH media and USP III method with bio-relative media. Results Conclusion： The in vitro drug release behavior of homemade metformin hydrochloride extended release tablet is very close to that of Glucophage XR. KEY WORDS metformin hydrochloride extended release tablet； hydroxypropyl methylcellulose； sodium carboxymethyl cellulose； hydrophilic matrix 盐酸二甲双胍是双胍类降血糖药物，是2型糖尿病的常用治疗药物，其缓释片的临床应用已趋普遍。盐酸二甲双胍在生物药剂学分类系统（biopharmaceutical classification system， BCS）中属Ⅲ类