The process described herein proceeds to obtaining diclofenac choline from choline bicarbonate and diclofenac acid in mild conditions, using non-toxic solvent, with the same impurity profile deriving from diclofenac particle as for diclofenac sodium EP. | New approaches to the synthesis of diclofenac choline Current Chemistry Letters 6 2017 159 166 Contents lists available at GrowingScience Current Chemistry Letters homepage New approaches to the synthesis of diclofenac choline Elżbieta Dąbrowska-Maś and Wojciech Raś Synthesis Laboratory ICN Polfa Rzeszów . Przemysłowa 2 35-959 Rzeszow Poland CHRONICLE ABSTRACT Article history The process described herein proceeds to obtaining diclofenac choline from choline Received March 2 2017 bicarbonate and diclofenac acid in mild conditions using non-toxic solvent with the same Received in revised form impurity profile deriving from diclofenac particle as for diclofenac sodium EP. The substance June 20 2017 is also substantially free from impurities deriving from choline and free from inorganic by- Accepted June 21 2017 products what means that the quality may be accepted for use as an active substance in Available online medicine. June 22 2017 Keywords Diclofenac choline Anti-inflammatory agent Oromucosal solution Mouthwash solution 2017 Growing Science Ltd. All rights reserved. 1. Introduction Diclofenac as an active moiety of chemical name 2- 2 6-dichlorophenyl amino phenyl acetic acid belongs to the group of non-steroidal anti-inflammatory drugs NSAID and causes inhibition of prostaglandin synthesis. Diclofenac is used to reduce pain and inflammation and is administered mainly orally and topically but also in a form for injection. Diclofenac acid shows very poor water solubility what is the main problem in development of medicinal formulations of sufficient bioavailability. It causes that diclofenac is used in medicine mainly in the more soluble salt forms containing inorganic counterions as sodium and potassium. Diclofenac was firstly synthesized by Sallmann and Pfister in 19731 but further improvements2 and shortening of the synthesis process using PdI2 as the catalyst3 are known. New diclofenac derivatives of improved solubility are also .
