目的 建立UPLC-MS同时测定大鼠血浆中玳玳果黄酮降脂滴丸药效组分新橙皮苷和柚皮苷的定量分析方法,比较玳玳果黄酮降脂滴丸与玳玳果总黄酮降脂提取物在大鼠体内的药动学特性。方法 采用UPLC-MS联用分析技术,测定大鼠血药浓度及拟合药-时曲线;大鼠分别灌胃给药玳玳果总黄酮降脂提取物、玳玳果黄酮降脂滴丸,分析比较其体内药动学过程,考察玳玳果黄酮降脂滴丸口服生物利用度的改善情况。结果 药动学试验结果表明,含药血浆中新橙皮苷的ρ_max分别为(1.68±0.02)_提取物和(5.54±0.09)_滴丸mg·L^-1,柚皮苷的ρ_max分别为(1.50±0.05)_提取物和(4.83±0.10)_滴丸mg·L^-1,玳玳果黄酮降脂滴丸的ρ_max、AUC_0-∞显著高于玳玳果总黄酮降脂提取物(P＜0.05);滴丸的MRT、t_1/2相比于玳玳果总黄酮降脂提取物明显缩短;以玳玳果总黄酮降脂提取物为参比,滴丸中新橙皮苷和柚皮苷的相对生物利用度分别提高了278.52%和258.59%。结论 玳玳果黄酮降脂滴丸明显改善了玳玳果总黄酮降脂提取物中药效成分新橙皮苷和柚皮苷的口服生物利用度。

OBJECTIVE To establish an UPLC-MS method for simultaneously determining the contents medical components of neohespiridin and naringin in rat plasma, meanwhile to investigate the pharmacokinetics for Daidai flavonoids lipid-lowering dropping pills and Daidai flavones extraction were compared in rats. METHODS We are established an UPLC-MS method to simultaneously determine the content of effective components(neohesperidin and naringin) of Daidai fruit flavones lipid-lowering dropping pills in rat plasma, measured blood drug concentration in rats, fitted medicine curve, analyzed and compared the pharmacokinetic process in vivo of Daidai fruit flavones lipid-lowering dropping pills and Daidai fruit flavonoids extracts, to evaluate the oral bioavailability improvement of Daidai fruit flavones lipid-lowering dropping pills. RESULTS The pharmacokinetics experimental results of rat gastric drug delivery with Daidai fruit flavonoids extract compared with that of rat with Daidai fruit flavones lipid-lowering dropping pills showed that the ρ_max of neohesperidin in medicated serum is(1.68±0.02) _extract and(5.54±0.09) _{dropping pills}mg·L^-1, respectively; the ρ_max of naringin is(1.50±0.05) _extract and(4.83±0.10) _{dropping pills}mg·L^-1, respectively; the ρ_max and AUC_0~∞ of Daidai fruit flavones lipid-lowering dropping pills were significantly higher than that of Daidai fruit flavonoids extraction(P<0.05), and MRT and t_1/2 of Daidai fruit flavones lipid-lowering dropping pills were significantly shorter than that of Daidai fruit flavonoids extracts.With Daidai fruit flavonoids extract as reference, the relative bioavailability of neohesperidin and naringin in dropping pills were 278.52% and 258.59%, respectively. CONCLUSION Daidai flavones dropping pill can significantly improve the medical components of neohespiridin and naringin oral bioavailability of Daidai flavones extraction.