Polymer particle erosion controlling drug release. I. Factors influencing drug release and characterization of the release mechanism

被引:109
作者
Zuleger, S [1 ]
Lippold, BC [1 ]
机构
[1] Univ Dusseldorf, Inst Pharmazeut Technol, D-40225 Dusseldorf, Germany
关键词
controlled drug delivery; hydrocolloid tablets; methyl hydroxyethyl cellulose (MHEC); polymer particle erosion; zero-order release; hydrodynamic stress;
D O I
10.1016/S0378-5173(01)00596-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The present study deals with controlled drug delivery from hydrocolloid tablets by polymer particle erosion. The influence of excipients and formulation factors on the dissolution behaviour of the methyl hydroxyethyl cellulose (MHEC)-tablets is investigated. Linear drug release with low susceptibility to hydrodynamic stress is obtained. The use of drugs with higher solubility leads to a slight acceleration of the release due to the contribution of diffusion to the release process. Higher drug loading and consequently lower polymer content expedites dissolution as well as changes in the tablets' geometry resulting in enlarged release surfaces. Furthermore, alterations of the composition of the dissolution medium affect drug release. However, neither viscosity grade nor the particle size of the polymer or compaction pressure has a marked impact on the dissolution. Investigations to clarify the mechanism of polymer particle erosion include erosion studies and the comparison of different batches of MHEC, of products from different manufacturers and of fibrous trial products. There is evidence that the insoluble fibres within the water soluble MHEC are responsible for the occurrence of polymer particle erosion by disturbing swelling and formation of a thick coherent gel layer and thus, causing erosion of the hydrocolloid tablet with synchronous drug release. (C) 2001 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:139 / 152
页数:14
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