制剂技术在提高BCSIV类药物生物利用度中的应用及此类药物体内外相关性研究现状

Recent Researches on the Application of Pharmaceutical Techniques in Improving the Bioavailability of BCS Class IV Drugs and In Vitro-In Vivo Correlation of This Class of Drugs

随着组合化学和高通量筛选在药物发现中的广泛应用,新候选药物不断涌现,其中不乏各种BCSIV类药物,而该类药物凸显的低溶解性/低渗透性极大地阻碍了其进一步的临床开发与应用。因此,如何有效提高该类药物生物利用度,已成为药剂学研究者长期以来广泛关注并致力于解决的课题。分类综述制剂技术在改善BCSIV类药物溶解性/渗透性方面的应用研究,并简介该类药物的体内外相关性研究进展。

As the combinatorial chemistry and the high throughput screening have been widely used in drug discovery, the proportion of BCS Class IV drugs in constantly emerging new drug candidates has significantly increased. The poorly solubility/poorly permeability of this class of drugs has become a barrier to their clinical development and application.Therefbre,how to improve their bioavailability based on solubility / permeability is the issue pharmacy researchers have given much attention to and made their attempt to solve for long. The recent researches on the application of pharmaceutical techniques in improving the solubility/permeability of＇ BCS Class IV drugs were classifiedly reviewed.The research progress in in vitro- in vivo correlation of this class of drugs was briefly introduced.