中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 药物制剂研究中心
Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography

文献类型：期刊论文

作者Yin, Xianzhen2,6; Li, Haiyan6; Guo, Zhen6; Wu, Li5,6; Chen, Fangwei4,6; de Matas, Marcel3; Shao, Qun2; Xiao, Tiqiao1; York, Peter2; He, You1
刊名AAPS JOURNAL
出版日期2013-10
卷号15期号:4页码:1025-1034
关键词drug release kinetics gel-forming matrix tablet statistical modeling swelling and erosion synchrotron radiation X-ray computed microtomography
ISSN号1550-7416
DOI10.1208/s12248-013-9498-y
文献子类Article
英文摘要The hydration layer plays a key role in the controlled drug release of gel-forming matrix tablets. For poorly water-soluble drugs, matrix erosion is considered as the rate limiting step for drug release. However, few investigations have reported on the quantification of the relative importance of swelling and erosion in the release of poorly soluble drugs, and three-dimensional (3D) structures of the hydration layer are poorly understood. Here, we employed synchrotron radiation X-ray computed microtomography with 9-mu m resolution to investigate the hydration dynamics and to quantify the relative importance of swelling and erosion on felodipine release by a statistical model. The 3D structures of the hydration layer were revealed by the reconstructed 3D rendering of tablets. Twenty-three structural parameters related to the volume, the surface area (SA), and the specific surface area (SSA) for the hydration layer and the tablet core were calculated. Three dominating parameters, including SA and SSA of the hydration layer (SA (hydration layer) and SSA (hydration layer) ) and SA of the glassy core (SA (glassy core) ), were identified to establish the statistical model. The significance order of independent variables was SA (hydration layer) > SSA (hydration layer) > SA (glassy core) , which quantitatively indicated that the release of felodipine was dominated by a combination of erosion and swelling. The 3D reconstruction and structural parameter calculation methods in our study, which are not available from conventional methods, are efficient tools to quantify the relative importance of swelling and erosion in the controlled release of poorly soluble drugs from a structural point of view.
WOS关键词MATRIX TABLETS ; GEL-LAYER ; HYDROPHILIC MATRICES ; DISSOLUTION ; SOLUBILITY ; DIFFUSION ; TOMOGRAPHY
资助项目SSRF Key Program[Z12sr0040] ; Ministry of Science and Technology of China[S2010GR0920] ; Ministry of Science and Technology of China[2010ZX09401-402] ; Ministry of Science and Technology of China[2012ZX09301001-001] ; Chinese Academy of Sciences Visiting Professorship for Senior International Scientists[00000000] ; National Natural Science Foundation of China[81273453]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000325126300013
出版者SPRINGER
源URL[http://119.78.100.183/handle/2S10ELR8/277438]  
专题药物制剂研究中心
分子影像中心（筹）
通讯作者York, Peter
作者单位1.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai Synchrotron Radiat Facil, Shanghai 201204, Peoples R China
2.Univ Bradford, Inst Pharmaceut Innovat, Bradford BD7 1DP, W Yorkshire, England;
3.AstraZeneca, Formulat Sci, Pharmaceut Dev, Macclesfield, Cheshire, England;
4.Zhejiang Chinese Med Univ, Hangzhou 310053, Zhejiang, Peoples R China;
5.Anhui Univ Tradit Chinese Med, Hefei 230038, Anhui, Peoples R China;
6.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, Shanghai 201203, Peoples R China;
推荐引用方式
GB/T 7714		 Yin, Xianzhen,Li, Haiyan,Guo, Zhen,et al. Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography[J]. AAPS JOURNAL,2013,15(4):1025-1034.
APA Yin, Xianzhen.,Li, Haiyan.,Guo, Zhen.,Wu, Li.,Chen, Fangwei.,...&Zhang, Jiwen.(2013).Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography.AAPS JOURNAL,15(4),1025-1034.
MLA Yin, Xianzhen,et al."Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography".AAPS JOURNAL 15.4(2013):1025-1034.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。