生物利用度
化学
溶解度
山奈酚
磷脂
差示扫描量热法
色谱法
溶解
药代动力学
核化学
作者
Kexia Zhang,Lian‐Quan Gu,Jinpeng Chen,Yuanyuan Zhang,Jiang Yu,Longshan Zhao,Kaishun Bi,Xiaohui Chen
标识
DOI:10.1016/j.jpba.2015.05.017
摘要
As one of the dietary flavonoids, kaempferol (KP) has been well known to show strong anti-oxidative effect along with other biological properties. However, the oral bioavailability of KP is relatively low due to its poor solubility. In this study, we intended to increase the solubility and bioavailability of KP by preparing kaempferol-phospholipid complex (KP-PC). The KP-PC's physicochemical properties were characterized in terms of infrared spectroscopy (IR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), water/n-Octanol solubility and in vitro dissolution. KP-PC exhibited higher solubility and dissolution rate than KP, indicating a significant improvement in hydrophilicity. A UPLC-ESI-MS/MS method was developed and validated for the determination of KP in Sprague-Dawley (SD) rat plasma, so as to investigate the oral bioavailability of KP-PC versus KP. Results showed that Cmax and AUC(0-48 h) of KP from the complex (Cmax: 3.94 ± 0.83 μg/mL, AUC(0-48 h): 57.81 ± 9.43 mg/Lh) were higher than that of KP (Cmax: 1.43 ± 0.21 μg/mL, AUC(0-48 h): 13.65 ± 3.12 mg/Lh). This research indicated that phospholipid complex (PC) might be one of the suitable approachs to improve the oral bioavailability of KP and other poor-solubility flavonoids.
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