Abstract：
The solidification of deep eutectic solvent (DES) through wet impregnation techniques on inert solid carriers is an interesting approach that offers better processing attributes and excellent stability. Herein, DES of Fimasartan (FS) was developed to improve its solubility and bioavailability. The selected DES-FS was solidified by wet impregnation method employing Nesulin US2 and Aerosil 200. The SeDeM-SLA (solid-liquid adsorption) system was employed to investigate flow attributes of solidified DES-FS. Further, the selected solidified DES-FS (A) was characterized by Fourier transforms infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM). The DES comprising Choline Chloride (ChCl): Glycerol (Gly) (1:3) revealed maximum drug solubility (35.6 ± 2.2 mg/mL) and thus opted for solidification. Solidification through wet impregnation was employed using 1:0.5 ratios (DES-FS to carriers). The Index of Good Flow (IGF) value was calculated from the SeDeM-SLA expert system, which indicates the better flow characteristics of solidified DES-FS, particularly with Neusilin US2 [SDES-FS (A)]. The solid-state evaluation data of SDS-FS (A) suggested a transition of FS to an amorphous form, resulting in an increment in solubility and dissolution. A similar trend was reported in the in vivo pharmacokinetic study, which indicated a 2.9 folds increment in the oral bioavailability of FS. Furthermore, excellent stability, i.e., a shelf life of 28.44 months, reported by SDES-FS (A) in accelerated stability studies, suggests better formulation perspectives. In a nutshell, the present study evokes the potentiality of performing solidification through wet impregnation and successful implementation of the SeDeM-SLA expert model, which could find wide applications in pharmaceutical science.
摘要：
通过湿浸渍技术在惰性固体载体上固化低共熔溶剂（DES）是一种有趣的方法，可提供更好的加工属性和出色的稳定性。在这里，开发了Fimasartan（FS）的DES以提高其溶解度和生物利用度。所选择的DES-FS通过使用NesulinUS2和Aerosil200的湿浸渍法来固化。SeDeM-SLA（固液吸附）系统用于研究固化的DES-FS的流动属性。Further,选定的固化DES-FS（A）通过傅立叶变换红外光谱（FTIR）进行表征，粉末X射线衍射(PXRD),差示扫描量热法(DSC),扫描电子显微镜(SEM)。包含氯化胆碱(ChCl):甘油(Gly)(1:3)的DES显示最大药物溶解度(35.6±2.2mg/mL),因此选择固化。使用1:0.5比率(DES-FS与载体)通过湿浸渍进行固化。良好流量指数(IGF)值由SeDeM-SLA专家系统计算，这表明固化的DES-FS具有更好的流动特性，特别是使用NeusilinUS2[SDES-FS(A)]。SDS-FS（A）的固态评估数据表明FS转变为无定形形式，导致溶解度和溶出度增加。在体内药代动力学研究中报道了类似的趋势，这表明FS的口服生物利用度增加了2.9倍。此外，出色的稳定性，即，保质期为28.44个月，SDES-FS(A)在加速稳定性研究中报告，提出了更好的表述观点。简而言之，本研究唤起了通过湿浸渍和成功实施SeDeM-SLA专家模型进行固化的潜力，可以在药物科学中找到广泛的应用。
