Ferrero C, Muñoz-Ruiz A, Jiménez-Castellanos M R
Departmento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/Tramontana s.n. 41012, Sevilla, Spain.
Int J Pharm. 2000 Jul 20;202(1-2):21-8. doi: 10.1016/s0378-5173(00)00407-5.
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 drug 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 relaxation, 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, but 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.
本研究的目的是对科伦坡等人提出的前沿运动方法进行改进,以便将其应用于无色药物和亲水性非膨胀性基质。以茶碱为模型药物,以羧甲基纤维素钠(NaCMC)或一种新型接枝共聚物——冻干的羟丙基纤维素甲基丙烯酸甲酯(HCMMAL)为聚合物载体,制备了基质片剂。对整片片剂进行了药物释放实验。还使用由四个不锈钢螺丝连接的两个有机玻璃圆盘组成的特殊装置评估了径向药物释放和前沿运动。通过Higuchi、Korsmeyer和Peppas方程确定释放动力学,并将其与前沿运动数据相关联。药物释放和前沿运动动力学分析表明,两种基质的释放机制不同。NaCMC基质中的药物释放主要受松弛控制,而药物通过多孔网络的扩散调节了HCMMAL基质中的药物释放。暴露于溶解介质的表面积减小导致药物释放速率降低,但释放机制没有本质改变。前沿运动被证明是阐明基质释放机制的有用工具。提出了在HCMMAL基质中观察到的不同前沿的新命名。