Effects Of Levocetirizine And Levofloxacin On Plasma Concentration Of Aminophylline In SD Rat

Objective:To investigate the effect of the elected two groups of chiral drug Levocetirizine and Levofloxacin on serum concentration of Aminophylline in SD rat,and investigate the effect of the two groups of racemate of chiral drug Cetirizine and ofloxacin on plasma concentration of Aminophylline by HPLC methods. To observe the significant difference of pharmacokinetics(PK) of the two groups compare with the plasma concentration of taking aminophylline alone.Methods: HPLC methods with UV detection were developed to study the pharmacokinetics of aminophylline in SD rats . The chromatography condition were: Hypersil-C18 column ( 250mm×4.6mm,5um) ;Water–methanol(85:15) as mobile phase at 1.0 mL·min-1; Detection wavelength was 275 nm at 35°.Serum concentrations of aminophylline were determined at different times and analysed the difference of pharmacokinetics(PK) after establish three dose of aminophylline(APL,APL+LCZ or LOFX,APL+ CZ or OFX).Results:In the chromatography condition, the rentention time of Aminophylline were 6.9～7.56min.The extraction recoveries of plasma were 68.04%~70.77% and recovery methodology were 92.48%~95% . The RSD of precision were 1.92%~3.28%.The pharmacokinetics of Aminophylline conforms to a one-compartment model , and showed the first order kinetics of distribution and elimination process in SD rats. To compare taking Aminophylline alone with taking Aminophylline and Levofloxacin,the total body chearance(CL) ,elimination half-life(T1/2) , take initial blood concentration(Co) and Elimination rate (Ke) have significant difference. The area under the curve (AUC) and apparent volume of distribution(V( c )) have difference. There were no difference of taking Aminophylline with Levofloxacin or Ofloxacin compared with take it alone.Conclusion: The plasma concentration of aminophylline was raised after take it with levocetirizine or cetirizine, at the same time, the greater inhibitory action of metabolism of taking aminophylline with cetirizine than levocetirizine. No effect of levofloxacin or floxacin on serum concentration of aminophylline.