OBJECTIVE To study on pharmacokinetics and metabolism of CA4 in SD rats with the oral administration CA4P.METHODS HPLC method was used for the detection of the concentration of CA4 in plasma.Column: AichromBond -1 ODS( 150 mm × 4.6 mm,5 μm);mobile phase: 0.05 mol·L -1 KH2PO4-methanol-acetonitrile( 50∶10∶40);flow rate: 1.0 mL·min -1; detection wavelength: 305 nm.After oral administration of CA4P at the dose of 20,50 and 90 mg·kg -1 in rats,the CA4 concentrations in plasma were detected.RESULTS There was good linearity in the range from 0.0155-7.7500 μg·mL -1( r = 0.9999).LOQ was 7.75 ng·mL -1; LOD was 0.3875 ng.The recovery was from 94.91%-99.85%;precision of intra-day and inter-day were 2.55%-4.87% and 5.06%-8.28%.After oral administration of CA4P in rats,the concentration-time curves of CA4 of two dosages were consistent with two-compartment model.The half lives were 48.74 min and 96.37 min; Vd were 131.39 and 450.19 L·kg -1; CL were 7.542 and 9.477 L·min -1·kg; AUC0 -t were 4.999 and 7.771 mg·L -1·min; bioavailability were 0.54% and 0.47% ,respectively.CONCLUSION The in dissolvable CA4 shows the poor absorption in body after oral administration of prodrug CA4P.It suggests that CA4 and CA4P are not applicable to oral administration directly.
OBJECTIVE To study the pharmacokinetics of active compound -combretastatin A4(CA4) which was produced by combretastatin A4 phosphate(CA4P) in rats.METHODS After iv administration of CA4P at the dose of 10,20 mg·kg-1 in rats,the concentrations of CA4 in blood serum at various time points were detected by HPLC method.Concentration-time curves were simulated by DAS program.RESULTS The concentration -time curves of CA4 of two groups were consistent with the two-compartment model.The main pharmacokinetic parameters of two groups were listed as follow:t1/2βwere 34.427±2.849 min and 30.076±3.107 min,Vd were 1.402±0.178 L·kg-1 and 1.568±0.131 L·kg-1,Cl were 0.061±0.003 L·min-1·kg-1 and 0.058±0.003 L·min-1·kg-1,AUC0-t were 132.393±3.144 mg·L-1·min and 291.872±15.555 mg·L-1·min,respectively.CONCLUSION After iv administration of CA4P,CA4 was rapidly metabolized and eliminated as two-compartment model in rats.
OBJECTIVE To study the pharmacokinetics of XY-02.METHODS Blood samples were collected at designed time points after iv administration of XY-02.The concentration of XY-02 was determined by HPLC.The HPLC system consisted of an ODS column(250 mm×4.6 mm,5 μm) and a mobile phase of methanol-0.1% acetic acid(50:50)with wavlength at 325 nm.RESULTS There was a good linearity in the range of 0.05-250 μg·ml-1.The quantitative limit was 0.017 μg·ml-1.The recoveries were 98.27%-99.50%.The precisions of intra-day and inter-day were 0.12%-0.60% and 0.48%-0.90%,respectively.After iv administration of XY-02 40,80,120 mg·kg-1,the half-life was 6.77,9.42,9.45 min;AUC(0-t) were 3908.04,5979.21,7635.33 mg·L-1·min-1,respectively.CONCULSION The pharmacokinetic process of XY-02 in rat serum fitted to a three-compartment model after iv of XY-02,and AUC increased along with the augment of dosage,fitted to linear dynamics(r=0.9959).
OBJECTIVE To find out the contents and distributing charaters of chlorogenic acid in tea from different enviroment and different kinds.To discuss the relationship between chlorogenic acid levels and producing processes.METHODSThe separation was performed on a Gemini C18 column(150 mm×4.6 mm,5 μm) with mobile phase of 0.1% H3PO4-acetonitril–triethylamine(92:8:0.1).The detection wavelength was 323 nm.RESULTSChlorogenic acid could be detected in all kinds of tea(0.01-0.40 mg·g-1).But the contents were different depending on the origin and producing processes.The contents of chlorogenic acid from high to low was:kuding teagreen teayellow teawhite teaflower teablue teablack teadark tea.In terms of producing area,tea from north area of the Yangtse river had the highest level,followed by the southern of Yangtse river southwest of Chinasouthern China.CONCLUSIONThe content of chlorogenic acid is diverse correlated with the place of produce as well as the producing technology of tea.