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Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat
Wang, Xue-qing1; Fan, Jie-ming1; Liu, Ya-ou2; Zhao, Bo1; Jia, Zeng-rong1; Zhang, Qiang1
关键词Nanomatrix Ph-sensitive Nanoparticles Suspension Oral Bioavailability Sorafenib
刊名INTERNATIONAL JOURNAL OF PHARMACEUTICS
2011-10-31
DOI10.1016/j.ijpharm.2011.08.003
419期:1-2页:339-346
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]PH-SENSITIVE NANOPARTICLES ; WATER-SOLUBLE DRUGS ; CYCLOSPORINE-A ; SOLID DISPERSIONS ; SILICA PARTICLES ; DELIVERY ; ITRACONAZOLE ; FORMULATION ; ABSORPTION ; STABILITY
英文摘要

Sorafenib is slightly absorbed in the gastrointestinal tract due to its poor solubility in water. To improve its absorption, a novel nanoparticulate formulation-nanomatrix was used in the study. The nanomatrix was a system prepared from a porous material Sylysia (R) 350 and a pH sensitive polymer Eudragit (R). The formulations were optimized by orthogonal design (L(9)(3(4))) and their bioavailability were evaluated in rat, comparing to pH-sensitive Eudragit nanoparticles and suspension of sorafenib. In the formulations, the ratio of sorafenib to Eudragit (R) S100 was found to be more important determinant of the sorafenib bioavailability than the ratio of sorafenib to Sylysia (R) 350. As for the bioavailability, the AUC(0-36h) of sorafenib nanomatrix was 13-33 times to that of sorafenib suspension, but only 16.8% to 40.8% that of Eudragit (R) 5100 nanoparticles. This may be resulted from the different drug dispersion degree, release character and bioadhension activity. However, because all the materials used in the nanomatrix formulation are commonly adjuvant, safe, easy to get and cheap, above all, the nanomatrix formulation can solve the stability and scaling up problems in the nanoparticles, it had potential to develop into a product in the future. (C) 2011 Elsevier B.V. All rights reserved.

语种英语
WOS记录号WOS:000296307000044
项目编号2009CB930300 ; 2009ZX09310-001
资助机构National Basic Research Program of China ; State Key Projects
引用统计
被引频次:46[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/400002259/53743
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, Hosp 1, Dept Pharm, Beijing 100034, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Wang, Xue-qing,Fan, Jie-ming,Liu, Ya-ou,et al. Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2011,419(1-2):339-346.
APA Wang, Xue-qing,Fan, Jie-ming,Liu, Ya-ou,Zhao, Bo,Jia, Zeng-rong,&Zhang, Qiang.(2011).Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat.INTERNATIONAL JOURNAL OF PHARMACEUTICS,419(1-2),339-346.
MLA Wang, Xue-qing,et al."Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat".INTERNATIONAL JOURNAL OF PHARMACEUTICS 419.1-2(2011):339-346.
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