Lopes Carla M, Lobo José Manuel Sousa, Pinto João F, Costa Paulo
Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha 164, 4050-047 Porto, Portugal.
Int J Pharm. 2006 Oct 12;323(1-2):93-100. doi: 10.1016/j.ijpharm.2006.05.063. Epub 2006 Jun 6.
Compressed mini-tablets systems are presented as a biphasic delivery system designed for zero-order sustained drug release. The outer layer that fills the void spaces between the mini-tablets was formulated to release the drug in a very short time (fast release), while the mini-tablets provided a prolonged release. Different composition (HPMC or EC) and number (10 or 21) of mini-tablets were used to obtain different drug release rates. The in vitro performance of these systems showed the desired biphasic behaviour: the drug contained in the fast releasing phase (powder enrobing the mini-tablets) dissolved within the first 2 min, whereas the drug contained in the mini-tablets was released at different rates, depending up on formulation. Based on the release kinetic parameters calculated, it can be concluded that mini-tablets containing HPMC were particularly suitable approaching to zero-order (constant) release over 8h time periods.
压缩微片系统是一种双相给药系统,设计用于零级持续药物释放。填充微片之间空隙的外层被设计成在很短时间内释放药物(快速释放),而微片则提供延长释放。使用不同组成(羟丙甲纤维素或乙基纤维素)和数量(10片或21片)的微片来获得不同的药物释放速率。这些系统的体外性能显示出所需的双相行为:快速释放阶段(包裹微片的粉末)中含有的药物在前2分钟内溶解,而微片中含有的药物则根据制剂以不同速率释放。根据计算出的释放动力学参数,可以得出结论,含有羟丙甲纤维素的微片在8小时时间段内特别适合接近零级(恒定)释放。