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Pharmaceutical salt formation guided by phase diagrams / Ka W. Lam in Industrial & engineering chemistry research, Vol. 49 N° 24 (Décembre 2010) 

Public ISBD [article]  in Industrial & engineering chemistry research > Vol. 49 N° 24 (Décembre 2010) . - pp. 12503-12512 Titre : Pharmaceutical salt formation guided by phase diagrams Type de document : texte imprimé Auteurs : Ka W. Lam, Auteur ; Jinjie Xu, Auteur ; Ka M. Ng, Auteur Année de publication : 2011 Article en page(s) : pp. 12503-12512 Note générale : Chimie industrielle Langues : Anglais (eng) Mots-clés : Phase  diagram Résumé : 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. DEWEY : 660 ISSN : 0888-5885 En ligne : http://cat.inist.fr/?aModele=afficheN&cpsidt=23692005 [article] Pharmaceutical salt formation guided by phase diagrams [texte imprimé] / Ka W. Lam, Auteur ; Jinjie Xu, Auteur ; Ka M. Ng, Auteur . - 2011 . - pp. 12503-12512. Chimie industrielle Langues : Anglais (eng) in Industrial & engineering chemistry research > Vol. 49 N° 24 (Décembre 2010) . - pp. 12503-12512 Mots-clés : Phase  diagram Résumé : 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. DEWEY : 660 ISSN : 0888-5885 En ligne : http://cat.inist.fr/?aModele=afficheN&cpsidt=23692005