Sugano Kiyohiko, Okazaki Arimichi, Sugimoto Shohei, Tavornvipas Sumitra, Omura Atsushi, Mano Takashi
Global Research & Development, Nagoya Laboratories, Pharmaceutical R&D, Pfizer Inc., Aichi, Japan.
Drug Metab Pharmacokinet. 2007 Aug;22(4):225-54. doi: 10.2133/dmpk.22.225.
The purposes of the review are to: a) Provide a comprehensible introduction of the-state-of-the-art sciences of solubility and dissolution, b) introduce typical technologies to assess solubility and dissolution, and c) propose the best practice strategy. The theories of solubility and dissolution required in drug discovery were reviewed especially from the view point of oral absorption. The physiological conditions in the gastrointestinal fluid in humans and animals were then briefly summarized. Technologies to assess solubility and dissolution in drug discovery were then introduced. Recently, these technologies have been improved by the laboratory automation and computational technologies. Finally, the strategies to apply these technologies for a drug discovery project were discussed.
a）对溶解度和溶出度的最新科学知识进行易懂的介绍；b）介绍评估溶解度和溶出度的典型技术；c）提出最佳实践策略。特别从口服吸收的角度回顾了药物发现中所需的溶解度和溶出度理论。然后简要总结了人和动物胃肠道液中的生理条件。接着介绍了药物发现中评估溶解度和溶出度的技术。最近，这些技术已通过实验室自动化和计算技术得到改进。最后，讨论了将这些技术应用于药物发现项目的策略。
