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.
ABSTRACT
Objective: Based on the advantages of representation of herb components group clustering by characteristic spectrum integrity, to study the in vitro dissolution behavior of Daidai Flavones Dropping Pills (DFDP), and to evaluate the synchronization release situation of group clustering. Methods: Rotating basket method and HPLC characteristic spectrum were employed to evaluate the group clustering dissolution and the release characteristics of DFDP in different dissolution media (pH 1.2 hydrochloric acid solution, pH 4.5 acetic acid-sodium acetate buffer, pH 6.8 phosphate buffer, and distilled water). The single exponential, logarithmic distribution and Weibull equation model were applied to fit the dissolution curves. Results: The similarity factor (f2) of the dissolution curves of nine common peak components in characteristic spectrum of DFDP was over 50; In addition the f2 of neohesperidin and naringin was 94.86, which indicated that the group clustering of DFDP had similar dissolution curves and synchronization release characteristics. Meanwhile the dissolution mechanism of group clustering of nine common peak activity composition was following the Weibull equation model. Conclusion: The established method is simple, rapid, and stable, which provides an experimental basic for in vitro analysis and quality evaluation of DFDP.
ABSTRACT
In order to explore the clinical hypolipidemic features of Daidai flavone extract, the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats were studied and compared. The study established the quantitative determination method of naringin and neohesperidin in plasma by UPLC-MS. Study compared the pharmacokinetics differences of naringin and noehesperidin in normal and hyperlipemia rats on the basis of establishment of hyperlipemia model. Results indicated that the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats showed significant differences. The C(max) of naringin and neohesperidin in hyperlipemia rats plasma after oral administration of Daidai flavone extract increased obviously, while t1/2, MRT and AUC0-24 h decreased, compared to normal rats. But t(max) showed no differences to that of normal rats. The results further proved Daidai flavone extract would have better hypolipidemic effect in the hyperlipemia pathological status. And the characteristic active ingredients naringin and noehesperidin were the material base of Daidai flavone extract to express the hypolipidemic effect.