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[1]陆步实,花春剑,李春海,等.琥珀酸美托洛尔缓释微丸片的制备[J].南京工业大学学报(自然科学版),2016,38(01):117-122.[doi:10.3969/j.issn.1671-7627.2016.01.019]
 LU Bushi,HUA Chunjian,LI Chunhai,et al.Preparation of metoprolol succinate sustained-release pellet tablets[J].Journal of NANJING TECH UNIVERSITY(NATURAL SCIENCE EDITION),2016,38(01):117-122.[doi:10.3969/j.issn.1671-7627.2016.01.019]
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琥珀酸美托洛尔缓释微丸片的制备()
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《南京工业大学学报(自然科学版)》[ISSN:1671-7627/CN:32-1670/N]

卷:
38
期数:
2016年01期
页码:
117-122
栏目:
出版日期:
2016-01-10

文章信息/Info

Title:
Preparation of metoprolol succinate sustained-release pellet tablets
文章编号:
1671-7627(2016)01-0117-06
作者:
陆步实1花春剑2李春海2孙磊1
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
Author(s):
LU Bushi1HUA Chunjian2LI Chunhai2SUN Lei1
1.Jiangsu Provincial,Institute of Materia Medica,Nanjing Tech University,Nanjing 211800,China; 2.College of Pharmaceutical Sciences,Nanjing Tech University,Nanjing 210009,China
关键词:
琥珀酸美托洛尔 缓释微丸 正交试验
Keywords:
metoprolol succinate sustained-release pellets orthogonal experiments
分类号:
R944.4
DOI:
10.3969/j.issn.1671-7627.2016.01.019
文献标志码:
A
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、SiO2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0.5~0.6 mm、乳糖用量5.0%、SiO2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(f2)均大于50。说明自研制剂在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。
Abstract:
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,f2 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.

参考文献/References:

[1] 刘雪茹.β受体阻滞剂临床应用[J].河北医药,2011,33(6):921.
[2] 张红梅,袁月玲.缓控释制剂的研究进展和临床应用中存在的问题[J].中国医学创新,2012,9(14):151.
[3] 冯中,李晓燕,吴燕红,等.心血管药物缓控释制剂的研究进展[J].时珍国医国药,2008,19(11):2664.
[4] PIERCY D A,QUARTERMAN C P,KENDALL M J,et al.Plasma levels and negative chronotropic effect of metoprolol following single doses of a conventional and sustained release formulation [J].Eur j clin pharmacol,1979,15(11):97.
[5] 国家药典委员会.中华人民共和国药典[M].二部.北京:化学工业出版社,2010:附录87.
[6] 刘会芳,赵燕燕,杜光玲,等.正交试验优选洛伐他汀胶囊处方工艺[J].中国药房,2008,19(31):2435.
[7] 徐自生.正交实验法在教育科研中的应用简介[J].上海教育科研,1987(3):44.
[8] 刘清飞,罗国安,王义明.缓控释制剂释放度相似性评价方法的应用进展[J].中国药学杂志,2006,41(15):1121.
[9] 陆彬.药物新剂型与新技术[M].北京:人民卫生出版社,1998:31.

备注/Memo

备注/Memo:
收稿日期:2014-11-21
作者简介:陆步实(1972—),男,江苏南京人,研究员,主要研究方向为药物新制剂,E-mail:Bushi89@163.com.
引用本文:陆步实,花春剑,李春海,等.琥珀酸美托洛尔缓释微丸片的制备[J].南京工业大学学报(自然科学版),2016,38(1):117-122..
更新日期/Last Update: 2016-01-20