盐酸青藤碱单室单层渗透泵型控释片的制备及释放考察  

Preparation of Monolithic Sinomenine Hydrochloride Osmotic Pump Tablets and Dissolution Test

作　　者：辛伟[1] 张志宏[1] 白敏[1] 梁敏[1] 杨敏[1] 

机构地区：[1]石药集团中奇制药技术(石家庄)有限公司,石家庄050051

出　　处：《中国药学杂志》2011年第19期1500-1505,共6页Chinese Pharmaceutical Journal

基　　金：科技部"十一五"重大新药创制项目(2009zx09503-026);中国药物技术创新及产业化战略联盟;科技部"十一五"重大新药创制(2010ZX09401-402)

摘　　要：目的研制盐酸青藤碱单室渗透泵型控释片,并考察体外释药行为。方法采用湿法制粒制备片芯,包衣后激光打孔制备渗透泵片。考察不同辅料种类及用量、助溶剂及包衣增重等因素对药物释放的影响。考察优选处方在不同溶出条件下的释药行为。结果渗透泵片片芯采用质量百分比为60%的甘露醇-乳糖(2∶1)为渗透促进剂,10%酒石酸为酸性助溶剂;包衣膜采用醋酸纤维素为控释材料,聚乙二醇为增塑剂,包衣增重4%。所得控释片可体外控制释药16 h,药物释放曲线符合零级释药模型。结论所研制的盐酸青藤碱控释片释药过程达到了预期的控释目的。OBJECTIVE To develope monolithic sinomenine hydrochloride osmotic pump tablets and study the drug release behavior. METHODS Sinomenine hydrochloride and core excipients were mixed well, and granules were prepared using wet-granulatiun method. Then the granules were compressed into tablets and coated by pan coating. Orific, e was formed by laser. The intluence of difterent types and amount of excipients, solubilizers and coating amounts on drug release were studied. The dissolution of optimized fornmla- tion in dif%rent conditions was tested, and the drug release model was established. RESULTS The optimal core formulation consisted of 60% mannitol-lactose （ ratio was 2：1 ） as osmotic agent and 10% tartaric acid as solubilizer. Cellulose acetate was employed as coating material and PEG was used as plasticizer. The optimal coating amount was 4%. The drug was released from the tablets in a controlled manner in 16 b as expected. The release behavior of the drug was in accordance with zero-order model. CONCLUSION The monolithic sinomenine hydroehloride osmotic pump tablets have achieved desired controlled-release effect.

关 键 词：盐酸青藤碱 单室单层渗透泵片 控释 正交设计 

分 类 号：R944[医药卫生—药剂学]