微粉化技术提高水不溶性药物溶解度

药物的微粉化可以改善颗粒的润湿性,进而提高水不溶性药物的溶解度和溶解速率。目前普遍采用的药物微粒化技术主要包括机械研磨、超临界流体过程、低温喷淋和溶剂蒸发沉积过程。本文介绍了这些微粉化制备技术的基本原理以及该类技术的应用进展。

Enhancement Dissolution of Poorly Water Soluble Drug by Micronization

It has been reported that about 40% of active compounds being developed by the pharmaceutical industry are poorly water soluble. A limiting factor in the oral bioavailability of poorly water soluble compounds is their inadequate dissolution rates. Increasing the dissolution rate of poorly water soluble active pharmaceutical ingredients (APIs) has become a major challenge in pharmaceutical formulation development. Micronizing processes could enhance the wetting and dissolution properties of poorly water soluble APIs. The micronizing processes involve mechanical micronization, supercritical fluid process, cryogenic spray process and solvent evaporation processes. The principles of the processes and their applications are introduced in this paper.