Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina.
Unidad de Investigación y Desarrollo en Tecnología Farmacéutica-UNITEFA (CONICET-UNC), Córdoba, Argentina.
AAPS PharmSciTech. 2018 Apr;19(3):1468-1476. doi: 10.1208/s12249-018-0952-0. Epub 2018 Feb 20.
Albendazole, an effective broad-spectrum anthelmintic agent, showed unpredictable therapeutic response caused by poor water solubility and slow dissolution rate. Then, novel binary and multicomponent supramolecular systems of two different solid forms of albendazole (I and II) with maltodextrin alone or with glutamic acid were studied as an alternative to improve the oral bioavailability of albendazole. The interactions and effects on the properties of albendazole were studied in solution and solid state. The solid systems were characterized using Raman and Fourier transform-infrared spectroscopy, thermal analysis, powder X-ray diffraction, and scanning electron microscopy. The solubility measurements, performed in aqueous and simulated gastric fluid, showed that albendazole (form II) was the most soluble form, while its supramolecular systems showed the highest solubility in simulated gastric fluid. On the other hand, the dissolution profiles of binary and multicomponent systems in simulated gastric fluid displayed pronounced increments of the dissolved drug and a faster dissolution rate compared to those of free albendazole forms. Thus, these supramolecular structures constitute an interesting alternative to improve the physicochemical properties of albendazole, with potential application for the preparation of pharmaceutical oral formulations.
阿苯达唑是一种有效的广谱驱虫药，但由于其水溶性差和溶解速度慢，导致治疗效果难以预测。因此，研究了两种不同固体形式（I 型和 II 型）的阿苯达唑与麦芽糊精或谷氨酸的新型二元和多组分超分子系统，以提高阿苯达唑的口服生物利用度。在溶液和固体状态下研究了它们之间的相互作用和对阿苯达唑性质的影响。采用拉曼和傅里叶变换红外光谱、热分析、粉末 X 射线衍射和扫描电子显微镜对固体系统进行了表征。在水相和模拟胃液中的溶解度测量表明，阿苯达唑（II 型）是最易溶解的形式，而其超分子系统在模拟胃液中的溶解度最高。另一方面，在模拟胃液中，二元和多组分系统的溶出曲线显示出药物溶解量的显著增加和更快的溶解速率，与游离阿苯达唑形式相比有所提高。因此，这些超分子结构为改善阿苯达唑的物理化学性质提供了一种有趣的选择，可能适用于制备口服药物制剂。
