Estudio del efecto de β-ciclodextrina sobre la estabilidad de Norfloxacina forma C

C. GARNERO; A. CHATTAH; L. FABIETTI; M. LONGHI

Cordoba

Congreso; 3a Reunión Internacional de Ciencias Farmacéuticas; 2014

Universidad Nacional de Córdoba

The polymorphism, the ability of a molecule to exist in several different conformations, affects the chemical and physical properties of an active pharmaceutical ingredient (API), which have a significant impact on pharmaceutical profile. A strategy developed to improve solubility, stability, and bioavailability of API is the formation of complexes with cyclodextrins (CDS). Norfloxacin (NOR) is a synthetic broad antibacterial fluoroquinolone that exists in several solid forms. In this study NOR form C was select as API model. Preliminary reports showed that supramolecular systems with -cyclodextrin (-CD) as ligand were developed to optimize physicochemical properties of API. In this study, the effect of novel supramolecular systems on chemical and physical stability of NOR C in solid state was investigated. The stability of NOR C, the NOR C:-CD system, obtained by kneading method, and their physical mixture was evaluated under accelerated storage conditions (at 40°C and 75% relative humidity). The solid samples were stored in closed glass vials exposed to daylight over a 6 month period into a stability chamber. The samples at predetermined intervals were monitored. The chemical stability was studied by high performance liquid chromatography (HPLC), while solid state nuclear magnetic resonance (ssNMR) and powder X-ray diffraction (PXRD) were used to evaluate the physical stability and possible phase transformations. Moreover, the hygroscopicity was determined. Our results revealed that NOR C and the physical mixture suffered the chemical degradation process. While, the amount of NOR C remains constant in the NOR C:-CD system, indicating that the interaction between -CD and NOR C increase the stability of the polymorph. Furthermore, it was observed absence of polymorphic transformations indicating that the samples maintains its physical stability. In conclusion, the NOR C:-CD system constitute an alternative tool to improve physicochemical properties of this polymorph, with potential application for the preparation of pharmaceutical dosage products.