琥珀酸美托洛尔缓释微丸片的制备  

Preparation of metoprolol succinate sustained-release pellet tablets

作　　者：陆步实[1] 花春剑 李春海[2] 孙磊[1] 

机构地区：[1]南京工业大学江苏省药物研究所,江苏南京211800 [2]南京工业大学药学院,江苏南京210009

出　　处：《南京工业大学学报（自然科学版）》2016年第1期117-122,共6页Journal of Nanjing Tech University(Natural Science Edition)

摘　　要：利用流化床包衣法制备琥珀酸美托洛尔缓释微丸,并与适宜辅料混合压制成片剂;利用正交试验考察载药微丸粒径、乳糖用量、SiO_2用量和包衣质量增加率4个关键因素对释放度的影响;利用单因素实验法考察微晶纤维素（MCC）用量、交联聚维酮（PVPP）用量和压力对释放的影响。结果表明：最优条件为载药微丸粒径0.5~0.6mm、乳糖用量5.0%、SiO_2用量10%、包衣质量增加率25%、MCC（粒径0.18 mm）用量44%、PVPP用量15%和压力70 N。与参比制剂比较,自研制剂在pH=1.2盐酸溶液、pH=4.5磷酸盐缓冲液、pH=6.8磷酸盐缓冲液和水4种介质中的释放曲线相似因子（f_2）均大于50。说明白研制剂在4种不同介质中的释放曲线和参比制剂一致,两者均属于non-Fick释放。Metoprolol succinate sustained-release pellets were prepared by fluid bed coating technology, and the sustained-release tablets were prepared by compression of sustained-release pellets with suitable excipients.The influence of four key factors, such as the drug pellets size, the content of lactose, silicon dioxide （SiO2 ）, and the coating level, was investigated for drug release by design of experiments. The influence of microcrystalline cellulose （ MCC ） content, crosslinking polyvingypyrrolidone （ PVPP ） content and pressure was investigated for drug release by single factor experiments. Results showed that the most suitable conditions were drug pellet sizes of 0. 5-0. 6 mm, lactose content of 5.0%, SiO2 content of 10%, coating level of 25% ,MCC （size 0. 18 mm） content of 44% ,PVPP content of 15% ,and tablet pressure of 70 N.Compared with reference preparation 0c2 factors of release curves for self-prepared preparations in the four kinds of different mediums （ pH = 1.2 hydrochloric acid solution, pH = 4. 5 and 6. 8 phosphate buffer solution, and water） were greater than 50.The release curves of self-prepared preparations were consistent with reference preparation ones, and they all belonged to non-Fick release.

关 键 词：琥珀酸美托洛尔 缓释微丸 正交试验 

分 类 号：R944.4[医药卫生—药剂学]