Salt Formation During Cogrinding of Enrofloxacin with Saccharin.

ROMAÑUK CAROLINA BEATRIZ; MANZO RUBEN HILARIO; OLIVERA MARIA EUGENIA

Tandil, Buenos Aires

Encuentro; 40a Reunión Anual de la Sociedad Argentina de Farmacología Experimental; 2008

Sociedad Argentina de Farmacología Experimental (SAFE)

Fluoroquinolone saccharinate salts (P-060105581) are pharmaceutical alternatives of fluoroquinolones presenting sweet taste to improve its palatability. The necessity of high amounts of hot water limits the convenience of the preparation method.  The purpose of this work was to investigate the mechanism of salt formation during cogrinding of solid reactants. Enrofloxacin saccharinate salt was used as a model compound. Cogrinding in a ball mill of anhydrous solid reactants was studied. Coground samples were analyzed by FTIR, XRPD, DSC-TGA at regular intervals from 0-8 hs and compared with enrofloxacin saccharinate obtained from solution method to establish amount and kind of interactions. The extent of salt formation during cogrindng was quantified by DSC and indicates the quick formation of the salt with a faster rate in the early stages of the process with not less than 45% of the salt formed after 30 min.  The reaction was completed after 6 hs. The solid obtained is a polymorph of that obtained from solution.  This method yields enrofloxacin saccharinate in a faster and cheaper way since solvents or boiling are not needed and the synthesis is completed in a unique step.