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目的:建立Beagle犬血浆中灯盏乙素的定量分析方法,测定灯盏乙素在Beagle犬体内血药浓度经时过程,评价灯盏花素磷脂复合物自微乳的药代动力学及相对生物利用度。方法:单剂量分别灌胃给予Beagle犬灯盏花素磷脂复合物自微乳及灯盏花素片,采用HPLC测定血浆中灯盏乙素的浓度,流动相甲醇-0.2%磷酸水(45∶55),检测波长335 nm。运用DAS2.1.1软件程序拟合药物浓度-时间曲线,计算药动学参数和生物利用度。结果:灯盏花素磷脂复合物自微乳、灯盏花素片灌胃Beagle犬后灯盏乙素药-时曲线均符合二室模型,主要药代动力学参数Tmax分别为190 min和160 min,Cmax分别为78.98mg·L-1和33.63 mg·L-1,AUC0-t分别为18 674.619 mg·L-1·min和9 132.475 mg·L-1·min;相对生物利用度204.49%。结论:灯盏花素磷脂复合物自微乳较灯盏花素片能显著提高灯盏乙素在Beagle犬体内的生物利用度,为灯盏花素口服制剂的开发提供新方向。
OBJECTIVE: To establish a quantitative method for the determination of scutellarin in Beagle dog plasma and to determine the pharmacokinetics and relative bioavailability of scutellarin-phospholipid complex self-microemulsion . Methods: Beagle dog was treated with single dose of Breviscapine phospholipid composite self-microemulsion and breviscapine tablets by HPLC. The concentration of scutellarin in plasma was determined by HPLC. The mobile phase consisted of methanol -0.2% phosphoric acid (45:55) Detection wavelength of 335 nm. DAS2.1.1 software program was used to fit the drug concentration-time curve to calculate pharmacokinetic parameters and bioavailability. Results: The scutellarin-time curve of breviscapine phospholipid composite self-microemulsion and breviscapine tablet intragastric administration was consistent with two-compartment model. The main pharmacokinetic parameters Tmax were 190 min and 160 min, Cmax Respectively, 78.98 mg · L-1 and 33.63 mg · L-1, respectively. The AUC0-t was 18 674.619 mg · L-1 · min and 9 132.475 mg · L-1 · min respectively. The relative bioavailability was 204.49%. Conclusion: Breviscapine phospholipid composite self-microemulsion compared to breviscapine tablets can significantly improve the bioavailability of scutellarin in Beagle dogs and provide a new direction for the development of breviscapine oral formulations.