Polymorphism in a new ciprofloxacin saccharinate: X-Ray, FTIR and solid state NMR characterization

C. B. ROMAÑUK; Y. GARRO LINCK; A. K. CHATTAH; G. A. MONTI; R. BAGGIO; M. T. GARLAND; S. L. CUFFINI

Estancia San PEdro, Brasil

Congreso; LAPOLC 09; 2009

Polymorphism has been recognized as an important element of drug development.1 The fluoroquinolone Ciprofloxacin (CIP) is a widely prescribed broad-spectrum oral antibiotic available in more than 100 countries and has been approved for the treatment of several types of infections2. Saccharin (SAC) is one of the best known and most widely used artificial sweetening agents.  Also, it has been proposed that it could be used to improve organoleptic properties of drugs. New pharmaceutical derivatives of fluoroquinolones with SAC having sweet taste, have been recently reported.3 In the present work we characterize the CIP-SAC form II (Fig 1 and 2), which is compared with the previously reported form I.3 CIP-SAC (II) was successfully obtained as a single-crystal. To characterize and distinguish both polymorphic forms we used solid state techniques: powder X-ray diffraction, single-crystal X-ray diffraction, Infrared and Solid State NMR (13C-CPMAS).