目的 制备木犀草素（Lut）固体分散体（Lut-SD）和木犀草素磷脂复合物固体分散体（Lut-PC-SD），并比较2种固体分散体对口服吸收生物利用度的影响。方法 以PVP K30为载体，溶剂挥发法分别制备Lut-SD和Lut-PC-SD。粉末X衍射（XRPD）分析Lut在2种固体分散体体中存在状态，并对溶解度及溶出度改善情况进行考察。SD大鼠分别ig给予Lut、Lut-SD和Lut-PC-SD，预定时间点取血。以香叶木素为内标，HPLC法测定并计算血浆样品中Lut的血药浓度，计算主要药动学参数。结果 XRPD分析结果显示，Lut在Lut-SD和Lut-PC-SD呈均以无定形状态存在。Lut-SD和Lut-PC-SD分别将Lut溶解度由（61.09±0.09）μg/mL提高至（365.33±0.38）μg/mL和（401.14±0.19）μg/mL，且体外溶出度均得到提高。药动学研究结果显示，与原料药相比，Lut-SD的生物利用度提高至150.10%，Lut-PC-SD提高至204.52%。结论 Lut-SD和Lut-PC-SD均可显著提高Lut口服吸收生物利用度，且Lut-PC-SD的效果更佳。

Objective To prepare luteolin solid dispersions (Lut-SD) and luteolin phospholipids complex solid dispersions (Lut-PC-SD), and compare the effects of two kinds of solid dispersions on the bioavailability in vivo. Methods PVP K30 was employed as carrier, and solvent evaporation method was used to prepare Lut-SD and Lut-PC-SD. Their existential state of luteolin in solid dispersions was analyzed by X-ray power diffraction (XRPD). The solubility and dissolution rate were also studied. SD rats in each group were administered intragastrically with Lut, Lut-SD, and Lut-PC-SD, respectively. Their blood samples were collected at different time intervals. Diosmetin was used as internal standard, the concentration of Lut in blood was analyzed by HPLC, and the main pharmacokinetic parameters were obtained. Results The results of XRPD indicated that Lut showed an amorphous state in Lut-SD and Lut-PC-SD. The solubility of Lut was enhanced from (61.09 ±0.09) μg/mL to (365.33 ±0.38) μg/mL and (401.14 ±0.19) μg/mL by Lut-SD and Lut-PC-SD, repectively. The dissolution of Lut was also improved greatly by the two kinds of solid dispersions. Compared to Lut, the bioavailability of Lut-SD and Lut-PC-SD was enhanced to 150.10% and 204.52%, repectively. Conclusion Lut-SD and Lut-PC-SD both could enhance the bioavailability of Lut in SD rats notably. In addition, Lut-PC-SD could give a better effect.

国家科技重大专项（2018ZX09201009-002-009）