Pharmacokinetics and Bioavailability in Vivo Rats of Daidai Flavonoids Lipid-Lowering Dropping Pills / 中国药学杂志

ABSTRACT

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 ρmax of neohesperidin in medicated serum is(1.68±0.02)extract and (5.54±0.09)dropping pillsmg·L-1, respectively; the ρmax of naringin is(1.50±0.05) extract and(4.83±0.10) dropping pillsmg·L-1, respectively; the ρmax and AUC0~∞ of Daidai fruit flavones lipid-lowering dropping pills were significantly higher than that of Daidai fruit flavonoids extraction(P<0.05), and MRT and t1/2 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.