Team Nanovectors for Targeted Therapy and Molecular Imaging (VICT), Chemical and Biological Technologies for Health Unit (UTCBS), CNRS UMR8258, INSERM U1022, Paris Descartes University, Sorbonne-Paris-Cité, Chimie ParisTech, PSL Research University, School of Pharmacy, 4 avenue de l'Observatoire, 75006, Paris, France.
ChemMedChem. 2019 Jan 8;14(1):8-23. doi: 10.1002/cmdc.201800612. Epub 2018 Dec 27.
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.
活性主要成分的固体制剂筛选是药物开发的一个挑战，因为超过 80%的上市药物是以固体制剂的形式配制的。需要对药物的各种固体制剂进行广泛而全面的研究，以促进其向临床转化。因此，必须考虑到体外和体内稳定性、靶向性、溶解度、溶出率和生物利用度等因素，选择最合适的固体制剂。在这篇综述中，涵盖了固体制剂筛选技术，包括多晶型物、溶剂化物、盐、共晶和无定形颗粒等固体形式的差异。此外，还讨论了固体药物的粒径减小，深入了解了药物纳米晶体制剂的出现。本文还提供了文献和市场上报道的最小纳米晶体的概述，以及它们的应用和给药途径。
