PMID: 11532579Sep 5, 2001Paper

Preparation and characterisation of a range of diclofenac salts

International Journal of Pharmaceutics
K M O'Connor, O I Corrigan

Abstract

Physicochemical properties of diclofenac salts prepared using eight different counterions and including five novel salts, obtained with the bases 2-amino-2-methyl-1,3-propanediol, 2-amino-2-methylpropanol, tert-butylamine, benzylamine and deanol, were compared. Four of the bases used to prepare these salts were related in their chemical structure, differing only in the number of hydroxy groups. Characterisation techniques included X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, thermomicroscopy, Karl Fischer titration, FT-IR spectroscopy and elemental analysis. In the case of salts prepared from 2-amino-2-methylpropanol and benzylamine, two polymorphic forms of each salt were identified. For the 2-amino-2-methyl-1,3-propanediol salt, a pseudopolymorphic form was identified. The aqueous solubilities of the salts studied ranged from 3.95 mM (tris(hydroxymethyl)aminomethane salt) to 446 mM (deanol salt), corresponding to a 113-fold difference in solubility. The solubility of diclofenac deanol was higher than the solubilities for diclofenac salts reported earlier. Correlation was found between the inverse of the salt melting point and the logarithm of salt solubility. A log-log relationship was obs...Continue Reading

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Citations

Apr 15, 2004·International Journal of Pharmaceutics·Vimon Tantishaiyakul
May 10, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Margit HornofAndreas Bernkop-Schnürch
Apr 6, 2007·Chemical & Pharmaceutical Bulletin·Jahanbakhsh Ghasemi, Saadi Saaidpour
Sep 13, 2002·Journal of Pharmaceutical Sciences·Karen M O'Connor, Owen I Corrigan
Oct 4, 2005·Journal of Pharmaceutical Sciences·Adamo FiniJosefa Alvarez-Fuentes
Jan 12, 2012·Journal of Pharmaceutical Sciences·Adamo FiniRita Morigi
Jun 6, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Ekarat JantratidJennifer B Dressman
Dec 7, 2007·Drug Discovery Today·Lokesh KumarArvind K Bansal
May 4, 2007·International Journal of Pharmaceutics·Henry R CostantinoSteven C Quay
Jun 23, 2005·The Journal of Pharmacy and Pharmacology·Majella E LaneOwen I Corrigan
Mar 3, 2012·Drug Development and Industrial Pharmacy·Benjamin M CollmanAnthony C Blackburn
Nov 29, 2011·Drug Development and Industrial Pharmacy·S E DavidB R Conway
Jun 21, 2013·Drug Development and Industrial Pharmacy·Vineet Kumar RaiShubhini A Saraf
Sep 24, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Atsushi KambayashiJennifer Dressman
Nov 3, 2010·The Journal of Pharmacy and Pharmacology·Sarah E DavidBarbara R Conway
Jun 20, 2007·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Sontaya LimmatvapiratManee Luangtana-Anan
Nov 3, 2009·Drug Development and Industrial Pharmacy·Grzegorz Garbacz, Werner Weitschies
Mar 15, 2018·Physical Chemistry Chemical Physics : PCCP·Mariana KozlowskaAnna Kaczmarek-Kedziera
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter

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