CONICET | Buscador de Institutos y Recursos Humanos

Fluoroquinolone Saccharinates (FQ-SACs, P-060105581) are new salts of FQs regarded as pharmaceutical alternatives. They have demonstrated an improvement in their organoleptic properties when evaluated in animals and humans. The aim of this work was to study aqueous solubility and pH compatibility of the saccharinate salts of the FQs norfloxacin, ciprofloxacin and enrofloxacin in order to establish their utility as pharmaceutical alternatives. Solubility studies were comparatively conducted at 25 ºC in water and also at pH values embracing intestinal range (from 4 to 8) and compared to FQs. From 10 to 120 % of the SAC, present in aqueous saturated solutions of FQ-SACs, was neutralized with NaOH. Solid phase in equilibrium was characterized by FTIR to determine the controlling solubility species. FQ-SACs are 5-20 times more soluble in water than their respective FQ precursor and yield saturated solutions whose pH is higher than that of the respective hydrochlorides (4.3-4.6). Solubility of FQ-SACs decrease with pH increase, following the same pattern observed with the precursors. However, close to neutrality, were minimum solubility is observed, norfloxacin and ciprofloxacin salts are more soluble than expected. This behavior can be explained by ionic pair formation and may occur at intestinal pHs in which the FQs are absorbed. The increase observed in the solubility allows enlarging formulation possibilities and might have an impact in the in vivo amount of drug dissolved at intestinal level.

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