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目的:比较研究亳菊总黄酮原料及其纳米乳制剂中主要活性成分木犀草素、芹菜素在大鼠体内的药动学特征。方法:取大鼠40只,随机分成亳菊总黄酮原料组(TF组)、亳菊总黄酮纳米乳组(TF-NE组),各组动物均灌胃给予400 mg·kg-1药物,采用高效液相色谱法(HPLC)测定灌服不同制剂大鼠血浆中木犀草素、芹菜素的血药浓度。采用3P97药动学软件,以二室开放模型计算药动学参数。结果:TF组血浆木犀草素Cmax为(0.68±0.08)μg·ml-1,tmax为(1.58±0.14)h,t1/2α为(1.62±0.75)h,t1/2β为(5.93±1.64)h,AUC0-∞为(5.53±0.61)μg·h·ml-1。芹菜素Cmax为(0.53±0.08)μg·ml-1,tmax为(2.24±0.48)h,t1/2α为(1.72±0.53)h,t1/2β为(5.82±1.36)h,AUC0-∞为(5.94±1.28)μg·h·ml-1。TF-NE组中木犀草素Cmax为(0.74±0.36)μg·ml-1,tmax为(3.61±2.04)h,t1/2α为(2.29±1.44)h,t1/2β为(6.87±3.39)h,AUC0-∞为(16.62±2.44)μg·h·ml-1。芹菜素Cmax为(1.12±0.34)μg·ml-1,tmax为(4.73±1.40)h,t1/2α为(3.27±0.41)h,t1/2β为(7.70±3.26)h,AUC0-∞为(19.17±4.45)μg·h·ml-1,与亳菊总黄酮比,二者的F相对分别为313%和318%。结论:与亳菊总黄酮原料相比,纳米乳制剂明显延长了芹菜素(延长了2.3 h)和木犀草素(延长2.0h)的达峰时间,显著增加二者的AUC0-∞水平和相对生物利用度,说明纳米乳制剂能延缓亳菊总黄酮的吸收,显著提高其生物利用度。
OBJECTIVE: To compare the pharmacokinetics of luteolin and apigenin, the main active components in the raw materials of Bo-ping flavonoids and their nanoemulsion preparations. Methods: Forty rats were randomly divided into three groups: the animals in the group of the TF group and the other groups, The plasma concentrations of luteolin and apigenin in different preparations of rats were determined by high performance liquid chromatography (HPLC). Using 3P97 pharmacokinetics software, pharmacokinetic parameters were calculated in a two-compartment open model. Results: The plasma luteolin Cmax in TF group was (0.68 ± 0.08) μg · ml-1, the tmax was (1.58 ± 0.14) h, the t1 / 2α was (1.62 ± 0.75) h and the t1 / 2β was (5.93 ± 1.64) h, AUC0-∞ was (5.53 ± 0.61) μg · h · ml-1. Apigenin Cmax was (0.53 ± 0.08) μg · ml-1, tmax was (2.24 ± 0.48) h, t1 / 2α was (1.72 ± 0.53) h, t1 / 2β was (5.82 ± 1.36) h and AUC0-∞ was (5.94 ± 1.28) μg · h · ml-1. The Cmax of luteolin in TF-NE group was (0.74 ± 0.36) μg · ml-1, the tmax was 3.61 ± 2.04 h, the t1 / 2α was (2.29 ± 1.44) h, and the t1 / 2β was (6.87 ± 3.39) h, AUC0-∞ was (16.62 ± 2.44) μg · h · ml-1. The Cmax of apigenin was (1.12 ± 0.34) μg · ml-1, the tmax was (4.73 ± 1.40) h, the t1 / 2α was (3.27 ± 0.41) h and the t1 / 2β was (7.70 ± 3.26) (19.17 ± 4.45) μg · h · ml-1, respectively. Compared with the content of total flavonoids in Bo-jiang, the F of the two strains were 313% and 318% respectively. Conclusion: Compared with the content of total flavonoids in Boju, the nanoemulsion significantly prolongs the peak time of apigenin (prolonged 2.3 h) and luteolin (prolonged 2.0 h), significantly increases the AUC0-∞ level and relative Bioavailability, indicating that nanoemulsion can delay the absorption of the content of total flavonoids in Bo-ge, and significantly improve its bioavailability.