复方盐酸吡格列酮/盐酸二甲双胍控释片的制备及体外释放考察  

Preparation and in Vitro Evaluation of Compound Pioglitazone Hydrochloride and Metformin Hydrochloride Controlled Release Tablets

作　　者：张尧[1] 李永吉[1] 刘平[1] 武占楠[1] 尹莉芳[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009

出　　处：《药学与临床研究》2013年第3期221-223,共3页Pharmaceutical and Clinical Research

摘　　要：目的:盐酸吡格列酮(PG)和盐酸二甲双胍(MH)可联用治疗2型糖尿病,两者通过机理上的互补可增强对患者血糖的调控。本文通过将两者制成复方控释片达到联合用药,延长并控制药物释放的目的,并考察其体外释放特性。方法:以聚乙烯吡咯烷酮(PVPK30)、乳糖、MH作为片芯,通过湿法制粒压片,使用含醋酸纤维素、聚乙二醇(PEG400)、苯甲酸甲酯的包衣液进行包衣形成半透膜,并在片两面通过激光打孔机各打一小孔,进一步在控释片表面包PG的速释层,形成复方控释片。对片芯处方和控释层包衣液处方进行筛选,控制包衣膜厚度和释药孔径。结果:MH可达到24 h零级释放,PG快速释放。PEG400和苯甲酸甲酯用量,包衣膜厚度对MH释放有显著影响。结论:通过正交设计和单因素考察,可得到最优处方的复方控释制剂,零级释药和快速释药,并达到联合用药的目的。Objective：Pioglitazone hydrochloride（PG） and metformin hydrochloride（MH） can be used together to treat type2 diabetes and control the blood sugar of patients by complementation of the two drugs.The compound controlled release PG/MH tablets were developed to achieve combined medication and controlled release.The in vitro release was evaluated.Methods：PVPK30,lactose and MH were used to compress the tablet by wet granulation,and then coated with coating solution including cellulose acetate（CA）,PEG400 and benzoate.Delivery orifices were drilled by laser drill on both sides of the tablet.The compound controlled release PG/MH tablets were obtained by coating the tablet with coating solution containing PG.Formulations of tablet core and coating solution of controlled release layer,membrane thickness and diameter of delivery orifice were optimized by orthogonal design and single factor evaluation.Results：We can get a 24-hour zero order release MH layer and a rapid release PG layer.PEG400,benzoate and membrane thickness have significant influence on drug release.Conclusion：The optimized controlled release PG/MH tablets can achieve combined medication.

关 键 词：盐酸吡格列酮 盐酸二甲双胍 控释片 

分 类 号：TQ460.6[化学工程—制药化工] R927.11[医药卫生—药学]