新型固体分散体技术改善水难溶药物溶解度的研究进展  

Recent Progress on the Solubility Improvement for Poorly Water-Soluble Drugs by Forming Solid Dispersions with Novel Carriers and Advanced Techniques

作　　者：刘文利[1] 魏振平[1] 

机构地区：[1]天津大学化工学院,天津300072

出　　处：《中国药学杂志》2016年第22期1901-1906,共6页Chinese Pharmaceutical Journal

基　　金：天津市自然科学基金资助项目(14JCYBJC29100)

摘　　要：通过改善水难溶药物的溶解度来提高其溶出速率以及口服后的吸收和生物利用度,是开发此类药物的口服制剂所面临的一大挑战。相对于其他制剂技术,用固体分散技术改善水难溶药物的溶解度,简便易行而更有优势也更受到关注。在简要介绍固体分散体的特点基础上,笔者重点对近年来固体分散体制备中所用的新型载体材料和制备方法进行综述。介绍了两亲性聚合物:聚乙二醇羟基硬脂酸酯、聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物、2-甲基丙烯酰乙氧基磷酰胆碱单体与甲基丙烯酸丁酯单体嵌段共聚物;还有无机材料:硅酸铝镁、介孔二氧化硅微粒和介孔碳酸镁,以及新型制备方法:超临界流体技术、高速静电纺丝和微环境pH修饰技术。To improve the in vitro dissolution and in vivo absorption as well as the bioavailability after oral administration by increas- ing the solubility with the formation of solid dispersion remains a great challenge for the oral dosage form design of poorly water-soluble drugs. Compared with the other pharmaceutical techniques in improving the solubility for poorly water-soluble drugs, priorities are usu- ally given to solid dispersion for its manufacturing convenience. Following the characteristics introduction, we were focused this review on the novel carriers and advanced techniques used for preparing solid dispersions. Amphiphilic polymers used as novel solid dispersion carriers are Solutol HS 15, Soluplus and poly [ MPC-co-BMA]. Inorganic materials like magnesium aluminum metasilicat, mesoporous silica microparticle and mesoporous magnesium carbonate are introduced together with the advanced solid dispersing techniques such as supereritical fluid technology, high speed electro-spinning and microenvironmental pH modified technology.

关 键 词：水难溶药物 固体分散体 溶解度 体外溶出度 新型载体材料 新型制备方法 

分 类 号：R944[医药卫生—药剂学]