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Pharmaceutical salt formation guided by phase diagrams
Lam K.W.4; Xu J.4; Ng K.M.4; Wibowo C.1; Lin G.3; Luo K.Q.2
2010-12-15
Source PublicationIndustrial and Engineering Chemistry Research
ISSN08885885 15205045
Volume49Issue:24Pages:12503-12512
AbstractSalt 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. © 2010 American Chemical Society.
DOI10.1021/ie902080k
URLView the original
Language英語
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Cited Times [WOS]:6   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.ClearWaterBay Technology, Inc.
2.Nanyang Technological University
3.Chinese University of Hong Kong
4.Hong Kong University of Science and Technology
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GB/T 7714
Lam K.W.,Xu J.,Ng K.M.,et al. Pharmaceutical salt formation guided by phase diagrams[J]. Industrial and Engineering Chemistry Research,2010,49(24):12503-12512.
APA Lam K.W.,Xu J.,Ng K.M.,Wibowo C.,Lin G.,&Luo K.Q..(2010).Pharmaceutical salt formation guided by phase diagrams.Industrial and Engineering Chemistry Research,49(24),12503-12512.
MLA Lam K.W.,et al."Pharmaceutical salt formation guided by phase diagrams".Industrial and Engineering Chemistry Research 49.24(2010):12503-12512.
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