Pharmacokinetics and tissue distribution of 2-methoxyestradiol intravenous emulsion in mouse

Aim:To investigate the pharmacokinetics and tissue distribution characteristics of 2-methoxyestradiol(2-ME)intravenous emulsion in mouse.Methods:After the plasma and tissue homogenate were precipitated,the 2-ME concentrations were determined by RP-HPLC.Pharmacokinetics and tissue distribution characteristics were analized using 3P97.Results:Concentration-time curve of 2-ME intravenous emulsion and 2-ME control solution were described by two-compartment model.Compared with those of 2-ME control solution,the elimination half-life of emulsion was prolong,AUC increased,the clearance rate decreased significantly,the average drug retention time was 16.6 fold,and the targeting parameters in the lung,liver,and spleen were greater.Conclusion:2-ME intravenous emulsion has a sustained-release characteristic and tissue targeting efficient in lung,liver,and spleen.