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新药开发中药物的盐型选择
引用本文:张大平,陆伟根. 新药开发中药物的盐型选择[J]. 中国医药工业杂志, 2011, 42(8)
作者姓名:张大平  陆伟根
作者单位:中国医药工业研究总院上海医药工业研究院,上海,200437
摘    要:成盐是改善弱酸性及弱碱性药物的溶解度和提高药物生物利用度的重要手段.因此,为药物筛选合适的反离子是药品研发过程的关键步骤.本文探讨了筛选反离子时需考虑的因素和成盐对药物的溶解度和溶出速率的影响.

关 键 词:成盐  溶解度  pH-溶解度关系  反离子  盐型筛选  综述

Salt Screening in Drug Development Process
ZHANG Daping,LU Weigen. Salt Screening in Drug Development Process[J]. , 2011, 42(8)
Authors:ZHANG Daping  LU Weigen
Affiliation:ZHANG Daping,LU Weigen~* (Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 20043 7)
Abstract:Salt formation is frequently employed to improve the solubility and bioavailability of weakly acidic and basic drugs.Therefore,choosing me appropriate counterion is the key step in the drug development process.In this paper,the protocol of screening salts and the effects on solubility and dissolution rate after salt formation are discussed.
Keywords:salt formation  solubility  pH-solubility profile  counterion  salt screening  review  
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