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学科主题: 药学
题名:
Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat
作者: 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
发表日期: 2011-10-31
DOI: 10.1016/j.ijpharm.2011.08.003
卷: 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
所属项目编号: 2009CB930300 ; 2009ZX09310-001
项目资助者: National Basic Research Program of China ; State Key Projects
WOS记录号: WOS:000296307000044
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53743
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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