PMID: 11427358Jun 28, 2001Paper

Comparison of the physicochemical properties of the N-(2-hydroxyethyl) pyrrolidine, diethylamine and sodium salt forms of diclofenac

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

Abstract

Non steroidal anti-inflammatory agents (NSAIDs) such as diclofenac have very low aqueous solubilities and consequently salt formation may be used to enhance solubility and dissolution rate. In this study, we examined the physicochemical properties of three diclofenac salts, diclofenac sodium (DNa), diclofenac N-(2-hydroxyethyl)pyrrolidine (DHEP) and diclofenac diethylamine (DDEA), and their different solid state forms to determine the influence of salt form on solubility, dissolution rate and membrane transport. The equilibrium solubility of DDEA at 25 degrees C was determined as 33 mM, lower than the solubilities of DHEP (273 mM) and DNa (66 mM) previously reported (Ledwidge and Corrigan, 1998). In addition to the dihydrate form of DHEP previously characterised, monohydrate forms of DHEP and DDEA were identified. Intrinsic dissolution rate studies were used to determine the solubility ratios of the hydrated and anhydrous forms. The monohydrate form of DHEP was found to be 1.8 times less soluble than the anhydrate, whereas DDEA anhydrate was approximately 1.7 times as soluble as the monohydrate form. On investigation of the pH-solubility profile (25 degrees C) of DDEA, appreciable supersaturation (76 mM) relative to the theoret...Continue Reading

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Citations

May 10, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Margit HornofAndreas Bernkop-Schnürch
Sep 5, 2001·International Journal of Pharmaceutics·K M O'Connor, O I Corrigan
Jul 30, 2010·International Journal of Clinical Practice·B H McCarberg, C E Argoff
Jan 12, 2012·Journal of Pharmaceutical Sciences·Adamo FiniRita Morigi
Feb 9, 2007·Journal of Pharmaceutical Sciences·Paola MinghettiAdamo Fini
Feb 24, 2011·Journal of Pharmaceutical Sciences·Sateesh Kumar SathigariR Jayachandra Babu
Apr 28, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Susan W LarsenClaus Larsen
Apr 26, 2005·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Adamo FiniAntonio M Rabasco
Nov 4, 2004·Drug Development and Industrial Pharmacy·Beom Soo ShinSun Dong Yoo
Nov 29, 2011·Drug Development and Industrial Pharmacy·S E DavidB R Conway
Apr 7, 2015·International Journal of Pharmaceutics·E AhnfeltH Lennernäs
Aug 16, 2006·Drug Development and Industrial Pharmacy·M A El-MassikN A Daabis
Mar 29, 2005·Journal of Pharmaceutical Sciences·Cristina CavallariAdamo Fini
Oct 4, 2005·Journal of Pharmaceutical Sciences·Adamo FiniJosefa Alvarez-Fuentes
May 27, 2009·Drug Development and Industrial Pharmacy·Ligang ZhaoZhonggui He
Jun 19, 2019·International Journal of Environmental Health Research·Mariela A AgotegarayVerónica L Lassalle
Jun 5, 2014·Archives of Pharmacal Research·Roshan PradhanJong Oh Kim
Dec 7, 2007·Journal of Medicinal Chemistry·G Steffen PaulekuhnChristoph Saal

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