期刊
AAPS JOURNAL
卷 15, 期 4, 页码 1025-1034出版社
SPRINGER
DOI: 10.1208/s12248-013-9498-y
关键词
drug release kinetics; gel-forming matrix tablet; statistical modeling; swelling and erosion; synchrotron radiation X-ray computed microtomography
资金
- SSRF Key Program [Z12sr0040]
- Ministry of Science and Technology of China [S2010GR0920, 2010ZX09401-402, 2012ZX09301001-001]
- Chinese Academy of Sciences Visiting Professorship for Senior International Scientists
- National Natural Science Foundation of China [81273453]
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.
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