Sun Yongda
Key Laboratory for Green Chemical Technology, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072, China.
Curr Pharm Des. 2014;20(3):349-68. doi: 10.2174/13816128113199990404.
Supercritical fluid particle design (SCF PD) offers a number of routes to improve solubility and dissolution rate for enhancing the bioavailability of poorly water-soluble drugs, which can be adopted through an in-depth knowledge of SCF PD processes and the molecular properties of active pharmaceutical ingredients (API) and drug delivery system (DDS). Combining with research experiences in our laboratory, this review focuses on the most recent development of different routes (nano-micron particles, polymorphic particles, composite particles and bio-drug particles) to improve solubility and dissolution rate of poorly water-soluble drugs, covering the fundamental concept of SCF and the principle of SCF PD processes which are typically used to control particle size, shape, morphology and particle form and hence enable notable improvement in the dissolution rate of the poorly water-soluble drugs. The progress of the industrialization of SCF PD processes in pharmaceutical manufacturing environment with scaled-up plant under current good manufacturing process (GMP) specification is also considered in this review.
超临界流体颗粒设计(SCF PD)提供了多种提高溶解度和溶出速率的途径,以增强难溶性药物的生物利用度,这可以通过深入了解SCF PD过程以及活性药物成分(API)和药物递送系统(DDS)的分子特性来实现。结合我们实验室的研究经验,本综述重点关注不同途径(纳米-微米颗粒、多晶型颗粒、复合颗粒和生物药物颗粒)在提高难溶性药物溶解度和溶出速率方面的最新进展,涵盖超临界流体的基本概念以及SCF PD过程的原理,这些过程通常用于控制粒径、形状、形态和颗粒形式,从而显著提高难溶性药物的溶出速率。本综述还考虑了在当前良好生产规范(GMP)下,在制药生产环境中使用放大装置进行SCF PD过程工业化的进展。