RESUMO
OBJECTIVE:To establish a HPLC-fluorescence detection method for the determiniation of the serum concentration of metoprolol.METHODS:The determination was performed on Symmetry C18 column,and the mobile phase consisted of acetonitrile-water-triethylamine -phosphoric acid(110∶390∶2.5∶1.6) at a flow rate of 0.8 mL?min-1.The excitation wavelength was 265 nm and the emission wavelength 298 nm,and the sample size was 20 ?L.RESULTS:Good linearity was obtained for metoprolol over the range of 2.0～100.0 ?g?L-1 with correlation coefficient r=0.999 6.At low,medium and high concentrations,the average recoveries of metoprolol were 99.73%,98.21% and 99.38%,respectively.The intra-day RSD were 2.89%,2.36% and 1.32%,respectively,and the inter-day RSD were 3.73%,3.03% and 2.25% respectively.The lowest detectable limit was 1.0 ?g?L-1.CONCLUSION:This method is precise,accurate,specific,simple yet with high recovery,and it is applicable for clinical monitoring of blood concentration and pharmacokinetic study.
RESUMO
OBJECTIVE:To evaluate the human body pharmacokinetics and bioequiavailability of two kinds of oral single dose of hydrochloric itraconazole capsules.METHODS:A randomized,crossover study of20healthy volunteers receiving sin-gle oral dose of200mg itraconazole was conducted with in vivo blood concentrations determined by HPLC-fluorescence de-tection.RESULTS:The pharmacokinetic parameters for the testing itraconazole and the reference itraconazole were as fol-lows,t 1/2 were(29.3?5.62)h and(29.3?5.81)h,respectively;C max were(81.4?60.0)?g/L and(77.8?45.2)?g/L,respec-tively;t max were(3.9?0.70)h and(4.2?0.70)h,respectively;AUC 0～72 were(1199.4?649.6)(?g?h)/L and(1174.3?701.9)(?g?h)/L,respectively;AUC 0～∞ were(1414.0?815.2)(?g?h)/L and(1386.1?735.8)(?g?h)/L,respectively.there were no significant differences in main pharmacokinetics parameters between2preparations,except in t max from analysis of variance and one-side&two-sides t-tests.The relative bioavailability of trial itraconazole capsule was(105.3?23.4)%.CONCLUSION:These two kinds of itraconazole capsules are bioequivalent.
