固体分散体在提高难溶性药物口服生物利用度中的应用-药学与临床研究.doc

固体分散体在提高难溶性药物口服生物利用度中的应用 董雅芬, 胡 滨，杨秋娅，娄月芬* （上海市第一人民医院分院药剂科，上海200081） 摘要：固体分散体在提高难溶性药物溶出度和口服生物利用度中的应用引起了药学工作者的关注，本文综述了固体分散体常用载体、常用的溶剂、提高难溶性药物溶出速率的机制和制备方法以及其他替代的方法，以期为难溶性药物制备为固体分散体提供参考。 关键词：固体分散体；难溶性药物；生物利用度 Application of Solid Dispersion to Improve Poorly Water-Soluble Drugs Bioavailability DONG Ya-fen1, HU Bin2, YANG Qiu-ya2, LOU Yue-fen* Department of Pharmacy, Branch Court of Shanghai First Peoples Hospital, Shanghai 200081, China ABSTRACT Solid dispersion have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of poorly water-soluble drugs. This article reviews solid dispersion commonly used carriers and solvents, mechanisms of solid dispersion improving drugs release rate, various preparation techniques and other alternative strategies. Aslo this review is to provide the reference for poorly water-soluble drugs to prepare solid dispersion. KEY WORDS:Solid dispersion; Poorly water-soluble drugs; Bioavailability 由于高通量筛选技术在药物开发中的广泛应用，涌现了很多分子量较大，结构复杂的化合物，在这些化合物中约40%是水难溶性的 ADDIN EN.CITE EndNoteCiteAuthorGiri TK/AuthorYear 2010/YearRecNum605/RecNumDisplayText[1]/DisplayTextrecordrec-number605/rec-numberforeign-keyskey app=EN db-id=00pxdap9gx0fwmes5535eafxx02zvfzdp9d0605/key/foreign-keysref-type name=Journal Article17/ref-typecontributorsauthorsauthorGiri TK, Alexander A., Tripathi DK/author/authors/contributorstitlestitlePhysicochemical classi?cation and formulation development of solid dispersion of poorly water soluble drugs: an updated review/titlesecondary-titleInt. J. Pharm. Biol. Arch. /secondary-title/titlesperiodicalfull-titleInt. J. Pharm. Biol. Arch./full-title/periodicalpagesstyle face=normal font=default size=100%309/stylestyle face=normal font=default charset=134 size=100%–324/style/pagesvolume1/volumedatesyear 2010/year/datesurls/urls/record/Cite/EndNote[ \o Giri TK, 2010 #6051]。在口服给药中，胃肠道的生理状况复杂，药物吸收的速度和程度受到诸多因素的影响，尤其对于水溶性差的药物，该类药物在胃肠道的溶解度很差，溶出速率低导致生物利用度较低 ADDIN EN.CITE EndN