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In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier
Yin, Li-Fang1,2; Huang, Shi-Jing2,3; Zhu, Chun-Li2; Zhang, Shu-Hui2; Zhang, Qiang1; Chen, Xi-Jing2; Liu, Qing-Wang2
关键词Repaglinide solid dispersion polyvinylpyrrolidone dissolution absorption pharmacokinetics
刊名DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
2012-11-01
DOI10.3109/03639045.2011.652635
38期:11页:1371-1380
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]POLYETHYLENE-GLYCOL 6000 ; PHYSICOCHEMICAL CHARACTERIZATION ; GASTROINTESTINAL ABSORPTION ; MOLECULAR DISPERSIONS ; HYDROPHILIC CARRIERS ; DISSOLUTION RATE ; DRUG-RELEASE ; ENHANCEMENT ; INDOMETHACIN ; SOLUBILITY
英文摘要

In order to improve the dissolution and absorption of the water insoluble drug repaglinide, a solid dispersion was developed by solvent method using polyvinylpyrrolidone K30 (PVP K30) as the hydrophilic carrier for the first time. Studies indicated that both solubility and the dissolution rate of repaglinide were significantly increased in the solid dispersion system compared with that of repaglinide raw material or physical mixtures. The repaglinide solid dispersions with PVP K30 solid state was characterized by polarizing microscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FT-IR). DSC and XRD studies indicated that repaglinide existed in an amorphous form in the solid dispersion. FT-IR analysis demonstrated the presence of intermolecular hydrogen bonding between repaglinide and PVP K30 in the solid dispersion. In the in situ gastrointestinal perfusion experiment, solid dispersion was shown to remarkably enhance the absorption of repaglinide in stomach and all segments of intestine. In vivo pharmacokinetic study in rats showed that immediate and complete release of repaglinide from the solid dispersion resulted in rapid absorption that significantly increased the bioavailability and the maximum plasma concentration over repaglinide raw material. These results demonstrated PVP K30 was an appropriate carrier for solid dispersion of repaglinide, with increased dissolution and oral absorption.

语种英语
WOS记录号WOS:000309453100011
项目编号NECT-08-0846 ; 2009ZX09310-004 ; 2009CB90300
资助机构Ministry of Education of the People&prime ; s Republic of China ; Ministry of Science and Technology of the People&prime ; s Republic of China ; National Basic Research Program of China
引用统计
被引频次:14[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/62074
专题北京大学药学院
北京大学临床肿瘤学院_肿瘤放疗科
作者单位1.Third Peoples Hosp Chengdu, Chengdu, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
3.China Pharmaceut Univ, Sch Pharm, Nanjing, Jiangsu, Peoples R China
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GB/T 7714
Yin, Li-Fang,Huang, Shi-Jing,Zhu, Chun-Li,et al. In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier[J]. DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,2012,38(11):1371-1380.
APA Yin, Li-Fang.,Huang, Shi-Jing.,Zhu, Chun-Li.,Zhang, Shu-Hui.,Zhang, Qiang.,...&Liu, Qing-Wang.(2012).In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier.DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY,38(11),1371-1380.
MLA Yin, Li-Fang,et al."In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier".DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY 38.11(2012):1371-1380.
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