Otto H. York Department of Chemical, Biological and Pharmaceutical Engineering, New Jersey Institute of Technology, Newark NJ 07102, USA.
Pharmaceutics. 2011 Aug 11;3(3):485-96. doi: 10.3390/pharmaceutics3030485.
The dynamic performances of two different controlled-release systems were analyzed. In a reservoir-type drug-delivery patch, the transdermal flux is influenced by the properties of the membrane. A constant thermodynamic drug activity is preserved in the donor compartment. Monolithic matrices are among the most inexpensive systems used to direct drug delivery. In these structures, the active pharmaceutical ingredients are encapsulated within a polymeric material. Despite the popularity of these two devices, to tailor the properties of the polymer and additives to specific transient behaviors can be challenging and time-consuming. The heuristic approaches often considered to select the vehicle formulation provide limited insight into key permeation mechanisms making it difficult to predict the device performance. In this contribution, a method to calculate the flux response time in a system consisting of a reservoir and a polymeric membrane was proposed and confirmed. Nearly 8.60 h passed before the metoprolol delivery rate reached ninety-eight percent of its final value. An expression was derived for the time it took to transport the active pharmaceutical ingredient out of the polymer. Ninety-eight percent of alpha-tocopherol acetate was released in 461.4 h following application to the skin. The effective time constant can be computed to help develop optimum design strategies.
分析了两种不同控释系统的动态性能。在储库型给药贴片中，透皮通量受膜的性质影响。在供药室内保持药物的恒定热力学活性。整体式基质是用于控制药物释放的最廉价系统之一。在这些结构中，将活性药物成分封装在聚合物材料内。尽管这两种装置很受欢迎，但要根据特定的瞬变行为来调整聚合物和添加剂的特性可能具有挑战性和耗时。通常考虑的启发式方法来选择载体配方只能提供对关键渗透机制的有限了解，从而难以预测装置性能。在本研究中，提出并验证了一种计算由储库和聚合物膜组成的系统通量响应时间的方法。美托洛尔的递送速率达到最终值的 98%需要近 8.60 小时。推导出了活性药物成分从聚合物中运出所需的时间的表达式。在应用于皮肤后 461.4 小时，98%的醋酸生育酚释放。可以计算有效时间常数以帮助制定最佳设计策略。
