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Preparation of ursolic acid?phospholipid complex by solvent-assisted grinding method to improve dissolution and oral bioavailability

机译:通过溶剂辅助研磨方法制备熊磷脂络合物,改善溶出和口服生物利用度

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摘要

To improve the aqueous solubility and the oral bioavailability of a poorly water-soluble biologically active pentacyclic triterpenoid, ursolic acid (UA), ursolic acid?phospholipid complex (UA?PC) was prepared using solvent-assisted grinding method which is green and simple. The phospholipid complex was characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscope (SEM), and transmission electron microscope (TEM), which confirmed the formation of the phospholipid complex. Specifically, compared with free UA, the formulation demonstrated over 276-fold higher aqueous solubility of UA and exhibited faster dissolution rate and higher cumulative dissolution percentages. Finally, the oral bioavailability of the prepared UA?PC was evaluated using Sprague-Dawley (SD) rats. Compared with free UA, the UA?PC exhibited considerable enhancement in the bioavailability with an increase in C-max (183.80 vs 68.26??g/l) and AUC (0?24?h) (878.0 vs 212.1??g?h/l), which was consistent with the in vitro results. This enhancement was attributed to the improvement of solubility and dissolution in vitro. Therefore, the method of solvent-assisted grinding appears to be an efficient approach for the preparation of UA?PC, and the prepared UA?PC showed a promising potential to overcome the limitation of poor oral bioavailability associated with low water solubility.
机译:为了改善水溶性的水溶性和口服生物活性五胞苷三萜类化合物,使用溶剂辅助研磨方法制备铜酸(UA),熊胆酸α磷脂酸(UAβPC)。磷脂复合物的特征在于差示扫描量热法(DSC),粉末X射线衍射(PXRD),扫描电子显微镜(SEM)和透射电子显微镜(TEM),其证实了磷脂复合物的形成。具体地,与游离UA相比,该配方在uA的含量较高的含水溶解度上显示出超过276倍,并且表现出更快的溶解速率和更高的累积溶解百分比。最后,使用Sprague-Dawley(SD)大鼠评估制备的UA的口腔生物利用度。与免费的UA相比,UA?PC随着C-MAX的增加而增加了生物利用度的大量增强(183.80 Vs 68.26 ?? G / L)和AUC(0?24?H)(878.0 Vs 212.1 ?? g?h / l),与体外结果一致。这种增强归因于体外改善溶解度和溶解。因此,溶剂辅助研磨的方法似乎是制备UAαPC的有效方法,并且制备的UA?PC显示出克服与低水溶性低相关的口服生物利用度的限制的有希望的潜力。

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