期刊
ADVANCED DRUG DELIVERY REVIEWS
卷 64, 期 6, 页码 480-495出版社
ELSEVIER
DOI: 10.1016/j.addr.2011.10.009
关键词
Poorly soluble drug; Dissolution; Bioavailability; Supersaturation; Crystal form; Self-emulsifying formulation; Solid dispersion; Amorphous; Nanosuspension
New chemical entities are required to possess physicochemical characteristics that result in acceptable oral absorption. However, many promising candidates need physicochemical modification or application of special formulation technology. This review discusses strategies for overcoming physicochemical problems during the development at the preformulation and formulation stages with emphasis on overcoming the most typical problem, low solubility. Solubility of active pharmaceutical ingredients can be improved by employing metastable states, salt forms, or cocrystals. Since the usefulness of salt forms is well recognized, it is the normal strategy to select the most suitable salt form through extensive screening in the current developmental study. Promising formulation technologies used to overcome the low solubility problem include liquid-filled capsules, self-emulsifying formulations, solid dispersions, and nanosuspensions. Current knowledge for each formulation is discussed from both theoretical and practical viewpoints, and their advantages and disadvantages are presented. (C) 2012 Elsevier B.V. All rights reserved.
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