Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 1 University Station, Campus Mail Code A1902, Austin, TX 78712, United States.
Int J Pharm. 2013 Aug 30;453(1):157-66. doi: 10.1016/j.ijpharm.2013.05.061. Epub 2013 Jun 7.
Poor water-solubility is a common characteristic of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate and bioavailability of these active ingredients belonging to BCS II and IV classifications. Over the last decade, nano-crystal delivery forms and amorphous solid dispersions have become well established in commercially available products and industry literature. This article is a comparative analysis of these two methodologies primarily for orally delivered medicaments. The thermodynamic and kinetic theories relative to these technologies are presented along with marketed product evaluations and a survey of commercial relevant scientific literature.
目前,水溶性差是药物开发管道中候选药物的一个共同特征。已经开发了各种工艺来提高这些属于 BCS II 和 IV 分类的活性成分的溶解度、溶解速率和生物利用度。在过去的十年中,纳米晶体递送形式和无定形固体分散体已在商业可获得的产品和行业文献中得到广泛应用。本文主要针对口服药物对这两种方法进行了比较分析。本文介绍了与这些技术相关的热力学和动力学理论,以及市售产品评估和商业相关科学文献调查。