Pharmaceutical Salt Formation Guided by Phase Diagrams
Publication in refereed journal

香港中文大學研究人員

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替代計量分析
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其它資訊
摘要Salt formation is frequently employed to Improve the solubility and bioavailability of pharmaceutical compounds Solid liquid equilibrium (SLE) phase diagram that serves as the foundation for designing crystallization-based separation is introduced to facilitate the recovery of the desired salt form Two poorly water-soluble drugs, each with two ionizable groups, were selected to demonstrate this phase diagram-guided approach The first is pemetrexed with confirmed monosodium and disodium salt forms The second drug is the orally administered dapsone for which no known salt form has been established Dihydrochloric salt of dapsone was successfully formed alongside the experimental phase diagram Its solubility was found to be 80 times higher than that of the parent drug Caco-2 cell assays showed that the intestinal permeability of the dihydrochloric salt was as good as that of the parent drug, thus confirming the usefulness of the salt form
著者Lam KW, Xu JJ, Ng KM, Wibowo C, Lin G, Luo KQ
期刊名稱Industrial && Engineering Chemistry Research
出版年份2010
月份12
日期15
卷號49
期次24
出版社AMER CHEMICAL SOC
頁次12503 - 12512
國際標準期刊號0888-5885
語言英式英語
Web of Science 學科類別Engineering; Engineering, Chemical; ENGINEERING, CHEMICAL

上次更新時間 2021-19-01 於 01:11