Kesisoglou Filippos, Wu Yunhui
Department of Pharmaceutical Research, Merck Research Laboratories, Merck & Co., Inc., WP75B-210, 770 Sumneytown Pike, P.O. Box 4, West Point, Pennsylvania 19486-0004, USA.
AAPS J. 2008 Dec;10(4):516-25. doi: 10.1208/s12248-008-9061-4. Epub 2008 Nov 6.
Selection of API phase is one of the first decision points in the formulation development process. Subsequent to phase selection, the focus shifts to the API physical properties such as particle size. Oftentimes, such properties are closely monitored throughout the drug development, as they can have a direct impact on the formulation bioperformance. The purpose of this mini-review was to describe the potential for application of absorption modeling in understanding the effect of API properties on bioavailability. Examples are provided to demonstrate how absorption modeling can be applied both early on to set the formulation strategy as well as during the development process to help with setting of specifications around the API. Limitations of the existing models and areas of possible expansion of such tools are also discussed.
原料药阶段的选择是制剂研发过程中的首要决策点之一。在阶段选择之后，重点转向原料药的物理性质，如粒径。通常，这些性质在整个药物研发过程中都受到密切监测，因为它们会对制剂的生物性能产生直接影响。本小型综述的目的是描述吸收建模在理解原料药性质对生物利用度影响方面的应用潜力。文中提供了示例，以说明吸收建模如何既能在早期应用于制定制剂策略，又能在研发过程中用于帮助设定原料药的质量标准。同时也讨论了现有模型的局限性以及此类工具可能的扩展领域。
