以多孔辅料为载体的固体分散体改善难溶性药物溶出度的研究进展

Research Progress of Solid Dispersion of Porous Material as Carrier to Improve the Dissolution Rate of Poorly Water-Soluble Drugs

溶解性是制约生物药剂学分类系统(BCS)Ⅱ类药物成药性与临床应用的关键。将药物制备成固体分散体是一种提高溶出度的有效方法。随着多孔辅料的不断研发与涌现,其独特的结构优势,使得其作为载体制备固体分散体成为药剂学研究的热点。基于此,笔者阐释了多孔辅料的概念与特点,总结了孔径大小、孔有序性及表面基团对释药性能的影响,介绍了以多孔辅料为载体的固体分散体的制备方法,归纳了常用的多孔辅料的分类、特点及应用,以期推动多孔辅料在难溶性药物中的应用,提高药物的生物利用度。

Drug solubility is the key factor that restricts the forming and clinical application of drugs in class II of the biopharma- ceutics classification system （BCS）. At present, making drugs into solid dispersion is an effective method to improve the dissolution rate. And with the research and development of mesoporous materials, using porous materials as the carrier to prepare solid dispersion becomes a hot research topic in recent years because of their unique structure advantages. Therefore, this paper elaborates the concept and characteristics of porous materials, summarizes the effects of pore size and ordered and surface groups on drug release properties, introduces the preparation method of solid dispersions with porous materials as the carrier, and finally summarizes the classification, characteristics and applications of the common porous materials in order to promote the application of porous materials in the pharma- ceutical preparation of poorly water-soluble drugs and improve their bioavailability.