Solubility and dissolution profile assessment in drug discovery.
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.
Sugano
Kiyohiko
K
Global Research & Development, Nagoya Laboratories, Pharmaceutical R&D, Pfizer Inc., Aichi, Japan. Kiyohiko.Sugano@pfizer.com
Okazaki
Arimichi
A
Sugimoto
Shohei
S
Tavornvipas
Sumitra
S
Omura
Atsushi
A
Mano
Takashi
T
D000465:Algorithms; D001647:Bile Acids and Salts / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003198:Computer Simulation; D004058:Diffusion; D015195:Drug Design; D004345:Drug Industry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012995:Solubility; D013816:Thermodynamics