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学科主题: 药学
题名:
Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: Preparation, characterization and evaluation in vivo
作者: Yang, Meiyan1; He, Shaolong1,2; Fan, Yunzhou3; Wang, Yuli1; Ge, Zhenzhong4; Shan, Li1; Gong, Wei1; Huang, Xiaoli1,2; Tong, Youzhi5; Gao, Chunsheng1
关键词: Solid dispersion ; Microenvironmental pH ; Acidifier ; Poorly water soluble drug ; Bioavailability
刊名: INTERNATIONAL JOURNAL OF PHARMACEUTICS
发表日期: 2014-11-20
DOI: 10.1016/j.ijpharm.2014.08.047
卷: 475, 期:1-2, 页:97-109
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]: EXTENDED-RELEASE FORMULATIONS ; ORAL BIOAVAILABILITY ; DELIVERY SYSTEMS ; SOLUBILITY PARAMETERS ; MATRIX TABLETS ; PARTICLE-SIZE ; DOSAGE FORMS ; MODULATION ; MECHANISM ; TELMISARTAN
英文摘要:

The aim of the present work was to design a pH-modified solid dispersion (pH(M)-SD) that can improve the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug. To select the appropriate acidifiers, a solubility test was carried out first. Solid dispersions (SDs) containing GT0918 and polyvinylpyrrolidone (PVP) were prepared using a solvent evaporation method and were characterized using dissolution studies in different media. The solid states of the SDs were investigated using scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transformed infrared spectroscopy (FTIR). The in vivo pharmacokinetics of the pHM-SDs tablets were also studied in beagle dogs compared to the conventional tablets. The optimized pH(M)-SD (GT0918/PVP/citric acid, 1: 2: 2 weight ratio) exhibited a significant improvement in the dissolution behavior compared to both the physical mixture and the binary SDs. Solid-state characterization revealed that the amorphous formation of GT0918 in the SDs and the strong H-bonding were only found in the pH(M)-SDs containing citric acid. Furthermore, the GT0918-loaded pH(M)-SD tablets showed a higher AUC and a lower t(max) compared to the conventional tablets. Accordingly, the pH(M)-SD might be an efficient route for enhancing the dissolution and bioavailability of poorly water-soluble GT0918. a 2014 Elsevier B. V. All rights reserved.

语种: 英语
所属项目编号: 2012ZX09301003-001-009 ; 2011ZX09102-001-05
项目资助者: National Key Technologies R &amp ; D Program for New Drugs ; State Key Laboratory of Antitoxic Drugs and Toxicology
WOS记录号: WOS:000345299500010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53924
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Henan Univ, Pharmaceut Coll, Kaifeng 475004, Peoples R China
2.Suzhou Kintor Pharmaceut Inc, Suzhou 215123, Peoples R China
3.Beijing Inst Pharmacol & Toxicol, Dept Pharmaceut, Beijing 100850, Peoples R China
4.Cent S Univ, Sch Pharm, Changsha 410013, Hunan, Peoples R China
5.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China

Recommended Citation:
Yang, Meiyan,He, Shaolong,Fan, Yunzhou,et al. Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: Preparation, characterization and evaluation in vivo[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2014,475(1-2):97-109.
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