Garnero Claudia, Chattah Ana Karina, Longhi Marcela
Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA) CONICET-UNC and Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina.
Facultad de Matemática, Astronomía y Física and IFEG (CONICET), Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina.
J Pharm Biomed Anal. 2014 Jul;95:139-45. doi: 10.1016/j.jpba.2014.02.017. Epub 2014 Mar 3.
In this work, complexes of β-cyclodextrin and the two solid forms of furosemide were prepared and characterized for their potential pharmaceutical applications, with the interactions between the two compounds being studied in the solution and solid states. The solubility studies revealed different behaviors of the polymorphs. In particular, it was observed that the binary complex significantly increased the solubility of furosemide form I in the gastric simulated fluid, which resulted in a rise in the bioavailability of this formulation after oral administration. In addition, results using ssNMR, FT-IR, DSC, TGA, SEM and XRPD provided evidence of the formation of complexes after utilizing kneading and freeze-drying methods. A comparison with previous developed complexes that used maltodextrin as the ligand was performed. Our results suggest that these novel supramolecular complexes showed promise to be used in drug delivery systems with an application in pharmaceutical formulations.
在本研究中,制备了β-环糊精与两种固体形式速尿的复合物,并对其潜在的药物应用进行了表征,同时研究了两种化合物在溶液和固态下的相互作用。溶解度研究揭示了多晶型物的不同行为。特别地,观察到二元复合物显著提高了速尿晶型I在模拟胃液中的溶解度,这导致口服给药后该制剂的生物利用度提高。此外,使用固体核磁共振、傅里叶变换红外光谱、差示扫描量热法、热重分析法、扫描电子显微镜和X射线粉末衍射的结果提供了采用捏合和冷冻干燥方法后形成复合物的证据。与先前开发的以麦芽糊精为配体的复合物进行了比较。我们的结果表明,这些新型超分子复合物有望用于药物递送系统,并应用于药物制剂中。