Kesisoglou Filippos, Panmai Santipharp, Wu Yunhui
Department of Pharmaceutical Research, Merck & Co., Inc., West Point, PA, USA.
Adv Drug Deliv Rev. 2007 Jul 30;59(7):631-44. doi: 10.1016/j.addr.2007.05.003. Epub 2007 May 25.
Poor aqueous solubility represents a major hurdle in achieving adequate oral bioavailability for a large percentage of drug compounds in drug development nowadays. Nanosizing refers to the reduction of the active pharmaceutical ingredient (API) particle size down to the sub-micron range, with the final particle size typically being 100-200 nm. The reduction of particle size leads to a significant increase in the dissolution rate of the API, which in turn can lead to substantial increases in bioavailability. This review describes the principles behind nanosizing, the production and characterization of nanoformulations as well as the current experience with utilization of such formulations in vivo.
如今，在药物研发中，对于很大比例的药物化合物而言，水溶性差是实现足够口服生物利用度的主要障碍。纳米化是指将活性药物成分（API）的粒径减小至亚微米范围，最终粒径通常为100 - 200纳米。粒径的减小导致API溶解速率显著提高，进而可大幅提高生物利用度。本文综述了纳米化背后的原理、纳米制剂的生产与表征，以及此类制剂在体内应用的当前经验。
