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A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate
Jia, Zengrong1,2; Lin, Ping1; Xiang, Yu1; Wang, Xueqing1; Wang, Jiancheng1; Zhang, Xuan1; Zhang, Qiang1
关键词Fenofibrate Oral bioavailability Nanomatrix Silica Polymethylacrylate
刊名EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
2011-09-01
DOI10.1016/j.ejpb.2011.05.009
79期:1页:126-134
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]WATER-SOLUBLE DRUGS ; ORDERED MESOPOROUS SILICA ; LIPID NANOPARTICLES ; AMORPHOUS INDOMETHACIN ; SOLID DISPERSION ; DELIVERY-SYSTEM ; CYCLOSPORINE-A ; ITRACONAZOLE ; FORMULATION ; SOLUBILITY
英文摘要

A novel solid particle system with a nanomatrix structure and without surfactant for the oral delivery of insoluble drugs was prepared. This used a combination of pH-sensitive polymethylacrylate and nano-porous silica, in order to improve the drug absorption using only pharmaceutical excipients and a relative simple process. The in vitro drug dissolution and in vivo oral bioavailability of this formulation, using fenofibrate as the model drug, were compared with other reference formulations such as a suspension, micronized formulation or self microemulsion drug delivery system (SMEDDS). The supersaturation stabilizing effect of different polymers was evaluated and the physicochemical characterization of the optimal formulation was conducted by SEM, TEM, surface area analysis, DSC, and XRD. The optimized formulation prepared with polymethylacrylate (Eudragit (R) L100-55) and silica (Sylysia (R) 350) markedly improved the drug dissolution compared with other reference preparations and displayed a comparative oral bioavailability to the SMEDDS. Fenofibrate existed in a molecular or amorphous state in the nanomatrix, and this state was maintained for up to 1 year, without obvious changes in drug release and absorption. In conclusion, the nanomatrix formulation described here is a promising system to enhance the oral bioavailability of water-insoluble drugs. (C) 2011 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000295427600017
项目编号2009CB930300 ; 2009ZX09310-001
资助机构National Basic Research Program of China ; Ministry of Science and Technology
引用统计
被引频次:44[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/400002259/62046
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.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang, Peoples R China
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Jia, Zengrong,Lin, Ping,Xiang, Yu,et al. A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate[J]. EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,2011,79(1):126-134.
APA Jia, Zengrong.,Lin, Ping.,Xiang, Yu.,Wang, Xueqing.,Wang, Jiancheng.,...&Zhang, Qiang.(2011).A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate.EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS,79(1),126-134.
MLA Jia, Zengrong,et al."A novel nanomatrix system consisted of colloidal silica and pH-sensitive polymethylacrylate improves the oral bioavailability of fenofibrate".EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS 79.1(2011):126-134.
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