This study explores the molecular association between 4-(thiophen-2-yl)-1-(4-(4-(trifluoromethyl)phenyl)piperazin-1-yl)butan-1-one (RTC1), an antidiabetic compound recently reported by our research group with challenging aqueous solubility, and 2-hydroxypropyl-β-cyclodextrin (HPBCD). The formation of a RTC1/HPBCD complex resulted in improved solubility. A phase-solubility diagram was used to determine the complex stability constant and stoichiometric ratio. 2D ¹H NMR spectroscopy was utilized to study the molecular interaction between RTC1 and HPBCD in the complex. Differential scanning calorimetry and scanning electron microscopy was also employed to confirm complex formation. In vitro biological evaluation, using a glucose uptake assay, showed that the homogeneous RTC1/HPBCD complex solution showed the same activity to that of RTC1 alone, with no reduction in activity due to the presence of HPBCD.

这项研究探讨了最近报道的一种抗糖尿病化合物4-（噻吩-2-基）-1-（4-（4-（三氟甲基）苯基）哌嗪-1-基）丁-1-酮（RTC1）之间的分子缔合是由我们的研究小组提出的，它具有极富挑战性的水溶性和2-羟丙基-β-环糊精（HPBCD）。RTC1 / HPBCD复合物的形成导致溶解度提高。使用相溶解度图确定复数稳定常数和化学计量比。2D ¹利用1 H NMR光谱研究复合物中RTC1和HPBCD之间的分子相互作用。差示扫描量热法和扫描电子显微镜也被用来确认复合物的形成。使用葡萄糖摄取测定法进行的体外生物学评估显示，均匀的RTC1 / HPBCD复合溶液显示出与单独的RTC1相同的活性，并且由于HPBCD的存在，活性没有降低。