INTEQUI   20941
INSTITUTO DE INVESTIGACIONES EN TECNOLOGIA QUIMICA
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
PREPARATION OF CO-AMORPHOUS FAMOTIDINE ? NAPROXEN SYSTEM BY MECHANICAL ACTIVATION: PHYSICAL CHARACTERIZATION AND SOLUBILITY ENHANCEMENT
Autor/es:
M.G.RUSSO; G.E. NARDA; Y. A. DAVILA; ELENA V. BRUSAU; C. ALMANDOZ
Lugar:
Rosario- Santa Fe
Reunión:
Congreso; 4ta. Reunión Internacional de Ciencias Farmacéuticas; 2016
Resumen:
Preparation of co-amorphous Famotidine ? Naproxen system by mechanical activation: physical characterization and solubility enhancementDávila, Y.a,b; Russo, M.a; Almandoz, C b.; Brusau, E.a; Narda, G.ae-mail: yadavila@unsl.edu.araINTEQUI (CONICET-UNSL). Química Inorgánica and bQuímica Física. FQBF, Universidad Nacional de San Luis, San Luis, 5700.The 84% of 50 most sold drugs is orally administered and thus requires significant absorption and appropriate delivery[1]. A strategy when dealing with poorly water soluble drugs, consists in converting them in amorphous that present improved solubility and dissolution rate compared to their crystalline counterparts, but are physically unstable. The stabilization is commonly achieved by combination with an inert carrier and recently, through the development of binary amorphous systems; the interactions between the co-amorphous partners seem to be responsible of the improved behavior[2].This work presents the physicochemical characterization of a famotidine (class IV) ? naproxen (class II) co-amorphous 1:1 mixture prepared by cryo-milling. Such system was selected with the aim to increase the dissolution of both drugs and relieve the well-known gastrointestinal side effects of the NSAID. The XRD patterns agree with thermal analysis measurements, consistent with an amorphous phase. A DSC signal at 73.3 ºC is assigned to a glass transition and no further events are observed until decomposition. A heterosynthon involving the guanidinium group of famotidine and the carboxylic one of naproxen is proposed according to the FTIR bands shifting. In addition, solubility of naproxen and famotidine increases significantly in relation to the pure drugs, the values being 1.35 and 1.94 mg mL-1, respectively. The results are compared with those obtained by quench-cooling and speed-vacuum techniques[3].Keywords: co-amorphous; naproxen; famotidine.[1] S. Dengale et al. Eur. J. Pharm. Sci. 62 (2014) 57[2] N. Chieng et al. Eur. J. Pharm. Biopharm. 71 (2009) 47.[3] Y. Dávila et al. VI Congreso Iberoamericano de Ciencias Farmacéuticas (2015).