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Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet
Qin, Chao1; He, Wei1; Zhu, Chunli2; Wu, Mengmeng1; Jin, Zhu1; Zhang, Qiang3; Wang, Guangji1; Yin, Lifang1
关键词Metformin hydrochloride Repaglinide Sandwiched osmotic pump tablets Pharmacokinetics Bioavailability In vivo-in vitro correlation
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2014-05-15
DOI10.1016/j.ijpharm.2014.03.002
466期:1-2页:276-285
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]IN-VIVO ; COMBINATION THERAPY ; BETA-CYCLODEXTRIN ; DELIVERY ; DRUG ; SYSTEM ; AGENT ; NIFEDIPINE ; PELLETS ; VITRO
英文摘要

The marketed compound tablet of metformin hydrochloride (MH) and repaglinide (RG) exhibits perfect multidrug therapeutic effect of type 2 diabetes. However, due to the short half life of the drugs, the tablet has to be administered 2 to 3 times a day, causing inconvenience to patient and fluctuations of plasma concentration. Here, a sandwiched osmotic pump tablet was developed to deliver the two drugs simultaneously at zero-order rate, in which MH and RG were loaded in different layers separated by a push layer. The osmotic pump tablet was prepared by a combination of three tableting procedure and film coating method. The factors including type and amount of propellant, osmotic active agents, amount of porogenic agent, coating weight, orifice diameter were optimized. The pharmacokinetic study was performed in beagle dogs, and the drug concentration in plasma samples was assayed by HPLC-MS/MS method. Simultaneous, controlled release of MH and RG in the first 12 and 8 h was achieved from the optimized formulation. A significantly decreased C-max, prolonged T-max and satisfactory bioavailability of the osmotic pump tablet were obtained, and a good in vivo-in vitro correlation of the two drugs was also established. In summary, the sandwiched osmotic pump tablet released the MH and RG simultaneously at zero-order rate, and exhibited significant sustained release effect in vivo and good in vivo-in vitro correlation. The designed controlled release system for MH and RG proposed a promising replacement for the marked compound product in the therapy of type 2 diabetes. (C) 2014 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000335441600031
项目编号2011ZX09202-101-24 ; 2012ZX09202101-008
资助机构National Ministry of Science and Technology the Twelfth Five-Year Plan ; Creation of Major New Drugs national major projects ; "333" High Level Talents Cultivation Project of Jiangsu Province
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61422
专题北京大学药学院
北京大学药学院_药剂学系
作者单位1.China Pharmaceut Univ, Sch Pharm, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
2.Nanjing Kang Bixin Pharmaceut Technol Co Ltd, Nanjing 210046, Jiangsu, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Qin, Chao,He, Wei,Zhu, Chunli,et al. Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2014,466(1-2):276-285.
APA Qin, Chao.,He, Wei.,Zhu, Chunli.,Wu, Mengmeng.,Jin, Zhu.,...&Yin, Lifang.(2014).Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet.INTERNATIONAL JOURNAL OF PHARMACEUTICS,466(1-2),276-285.
MLA Qin, Chao,et al."Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet".INTERNATIONAL JOURNAL OF PHARMACEUTICS 466.1-2(2014):276-285.
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