IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina.
Área Técnica Farmacéutica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina.
Mater Sci Eng C Mater Biol Appl. 2018 Nov 1;92:694-702. doi: 10.1016/j.msec.2018.07.013. Epub 2018 Jul 10.
Succinyl-β-CD derivatives were obtained by green synthesis with degrees of substitution (DS) 1.3 and 2.9. The spray-drying technique was used to obtain albendazole (ABZ):succinyl-β-CD inclusion complexes. Phase solubility diagrams indicated that both succinyl-β-CD derivatives formed 1:1 molar ratio ABZ complexes, but the complex with DS 2.9 has a lower formation constant. The presence of stable inclusion complexes in aqueous solution was confirmed by NMR. For both complexes the aromatic moiety is encapsulated into the host cavity. In the solid-state, C and N NMR spectral differences between ABZ and ABZ included in spray-dried systems showed that strong structural changes occurred in the systems. At least two different ABZ amorphous species were identified based on DS. ABZ species were stable over more than six months based on spectral data. Finally, the influence of DS in the number and type of the inclusion complexes was elucidated.
琥珀酰-β-CD 衍生物通过绿色合成得到，取代度（DS）分别为 1.3 和 2.9。喷雾干燥技术用于获得阿苯达唑（ABZ）：琥珀酰-β-CD 包合物。相溶解度图表明，两种琥珀酰-β-CD 衍生物均形成 1:1 摩尔比的 ABZ 配合物，但 DS 为 2.9 的配合物具有较低的形成常数。NMR 证实了在水溶液中存在稳定的包合物。对于这两种配合物，芳环部分都被包裹在主体空腔内。在固态下，ABZ 与喷雾干燥体系中包含的 ABZ 的 C 和 N 核磁共振光谱差异表明，体系中发生了强烈的结构变化。基于 DS，至少鉴定出两种不同的 ABZ 无定形物质。基于光谱数据，ABZ 物质在超过六个月的时间内保持稳定。最后，阐明了 DS 对包含配合物的数量和类型的影响。
