Fronts movement as a useful tool for hydrophilic matrix release mechanism elucidation
Fronts movement as a useful tool for hydrophilic matrix release mechanism elucidation
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DOI：
10.1016/s0378-5173(00)00407-5
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发表时间：
2000-07-20
影响因子：
5.8
通讯作者：
Jiménez-Castellanos, MR
中科院分区：
文献类型：
--
作者：
Ferrero, C;Muñoz-Ruiz, A;Jiménez-Castellanos, MR
本研究的目的是修改科隆博等人提出的前沿移动方法，以便将其应用于无色药物和亲水性非溶胀性基质。以茶碱为模型药物，羧甲基纤维素钠（NaCMC）或新型接枝共聚物--羟丙基纤维素甲基丙烯酸甲酯（HCMMAL）为高分子载体，制备了茶碱骨架片。从整个片剂进行药物释放实验。还使用由通过四个不锈钢螺钉连接的两个Plexiglass（R）盘组成的特殊装置来评价径向药物释放和前沿运动。释放动力学通过Higuchi，Korsmeyer和Peppas方程确定，并与前沿运动数据相关。药物释放和前沿运动动力学分析揭示了两种基质不同的释放机制。药物从NaCMC基质中的释放主要由室温下的释放控制，而药物通过多孔网络的扩散调节药物从HCMMAL基质中的释放。暴露于溶出介质的表面减少导致药物释放速率降低，但释放机制没有本质上改变。前沿运动被证明是一个有用的工具，为基质释放机制的解释。对HCMMAL矩阵中观察到的不同波前提出了一个新的命名。(C)2000 Elsevier Science B. V.保留所有权利。
The purpose of this study was to modify the fronts movement method proposed by Colombo et al. in order to apply it to uncoloured drugs and hydrophilic non-swellable matrices. Matrix tablets were prepared using theophylline as a model chug and sodium carboxymethylcellulose (NaCMC) or a new graft copolymer, hydroxypropylcellulose methylmethacrylate dried by lyophilization (HCMMAL), as polymer carriers. Drug release experiments were performed from the whole tablets. Radial drug release and fronts movement were also evaluated using special devices consisting of two Plexiglass (R) discs joined by means of four stainless steel screws. Release kinetics were determined by means of Higuchi, Korsmeyer and Peppas equations and were related to the fronts movement data. The analysis of drug release and fronts movement kinetics revealed a different release mechanism for both matrices. Drug release from NaCMC matrices was mostly controlled by rt laxation, whereas drug diffusion through the porous network regulated drug release from HCMMAL matrices. A reduction in the surface exposed to the dissolution medium led to a decrease in the drug release rate, bat the release mechanism was not essentially modified. Fronts movement was shown as a useful tool for matrix release mechanism elucidation. A new denomination for the different fronts observed in HCMMAL matrices was proposed. (C) 2000 Elsevier Science B.V. All rights reserved.