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State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation
ChemMedChem ( IF 3.4 ) Pub Date : 2018-12-27 , DOI: 10.1002/cmdc.201800612
Brice Martin Couillaud 1 , Philippe Espeau 1 , Nathalie Mignet 1 , Yohann Corvis 1
Affiliation  

The solid‐form screening of active principal ingredients is a challenge for pharmaceutical drug development, as more than 80 % of marketed drugs are formulated in the solid form. A broad and comprehensive study of the various solid forms of drugs is needed to enhance their translation into the clinic. Therefore, the most suitable solid form must be taken into consideration regarding ex vivo and in vivo stability, targeting, solubility, dissolution rate, and bioavailability. In this review, techniques of solid‐form screening are covered, including differences in solid forms such as polymorphs, solvates, salts, co‐crystals, and amorphous particles. Moreover, solid drug size reduction is also discussed, with insight into the emergence of drug nanocrystal formulations. An overview of the smallest nanocrystals reported in the literature and on the market is also provided, along with their applications and routes of administration.

中文翻译:

药物固体形式的最新技术:从晶体性能问题到纳米晶体配方

活性主要成分的固体形式筛选对于药物开发是一个挑战,因为超过80%的市售药物都是以固体形式配制的。需要对各种固体形式的药物进行广泛而全面的研究,以增强其向临床的转化。因此,关于离体和体内稳定性,靶向性,溶解性,溶解速率和生物利用度,必须考虑最合适的固体形式。在这篇综述中,涵盖了固体形式的筛选技术,包括固体形式的差异,例如多晶型物,溶剂化物,盐,共晶体和无定形颗粒。此外,还讨论了固体药物尺寸的减小,并深入了解了药物纳米晶体制剂的出现。
更新日期:2018-12-27
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