Efentakis Manuel, Buckton Graham
Centre for Materials Science, School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK.
Pharm Dev Technol. 2002 Jan;7(1):69-77. doi: 10.1081/pdt-120002232.
The extent of dissolution of theophylline from sodium alginate matrices has been studied in water and HCl. Surprisingly, it was observed that the dissolution rate was very fast for the low viscosity (LV) material in water and for the high viscosity (HV) in acid, whereas slow release was seen for LV in acid with very slow release for the HV in water. The extent of erosion and swelling of the matrices (with and without drug and with and without stirring) was determined from simple weighing experiments. Based on the extent of erosion and swelling, along with visual observations, it was concluded that the rapid release from LV in water was due to rapid and complete erosion of a weak gel layer. The rapid release of HV in HCl was due to an unexpected lamination of the tablet during swelling, which resulted in exposure of more of the tablet core, and caused increased erosion of the matrix. The slow release seen with the LV in HCl was due to the acid gel being tough and resistant to erosion. The very slow release observed with the HV in water was due to very substantial swelling, with the presence of near zero-order kinetics for this system being due to a balance of swelling and erosion, keeping the diffusion process at a constant rate. Furthermore, an anisotropic swelling behavior is indicated by the preferential expansion in the axial dimension relative to the radial dimension for both LV and HV alginates.
已在水和盐酸中研究了茶碱从海藻酸钠基质中的溶出程度。令人惊讶的是,观察到低粘度(LV)材料在水中以及高粘度(HV)材料在酸中的溶出速率非常快,而LV材料在酸中以及HV材料在水中的释放缓慢。通过简单的称重实验确定了基质(含药和不含药、搅拌和不搅拌)的侵蚀和溶胀程度。基于侵蚀和溶胀程度以及肉眼观察,得出结论:LV材料在水中的快速释放是由于弱凝胶层的快速且完全侵蚀。HV材料在盐酸中的快速释放是由于片剂在溶胀过程中意外分层,这导致更多片剂核心暴露,并导致基质侵蚀增加。LV材料在盐酸中的缓慢释放是由于酸性凝胶坚韧且抗侵蚀。HV材料在水中观察到的非常缓慢的释放是由于非常显著的溶胀,该系统存在接近零级动力学是由于溶胀和侵蚀的平衡,使扩散过程保持恒定速率。此外,LV和HV海藻酸盐在轴向尺寸相对于径向尺寸上的优先膨胀表明了各向异性的溶胀行为。