Rabinow Barrett E
Strategic Technical Development, Baxter Healthcare Corporation, Baxter Technology Park, Round Lake, Illinois 60073, USA.
Nat Rev Drug Discov. 2004 Sep;3(9):785-96. doi: 10.1038/nrd1494.
A surprisingly large proportion of new drug candidates emerging from drug discovery programmes are water insoluble, and therefore poorly bioavailable, leading to abandoned development efforts. These so-called 'brickdust' candidates can now be rescued by formulating them into crystalline nanosuspensions. In the process of overcoming issues involving solubility, additional pharmacokinetic benefits of the drugs so formulated have come to be appreciated. As such, insolubility issues of the past have provoked a paradigm change, which now offers novel solutions for innovative drugs of the future.
从药物研发项目中涌现出的新候选药物中，有相当大比例的药物是水不溶性的，因此生物利用度差，导致研发工作被放弃。这些所谓的“砖粉”候选药物现在可以通过将它们制成结晶纳米混悬液来挽救。在克服溶解性问题的过程中，人们逐渐认识到如此制备的药物还具有额外的药代动力学优势。因此，过去的溶解性问题引发了一种范式转变，现在为未来的创新药物提供了新的解决方案。
