포스포디에스테라제 III의 저해물인 KR-30075의 흰쥐에서의 약물속도론

Pharmacokinetics of KR-30075, A Potent Phosphodiesterase III Inhibitor in Rats

A procedure for the determination of KR-30075 and its metabolites in plasma and urine by high performance liquid chromatography is described. For the study of pharmacokinetic properties of KR-30075, a new PDE III inhibitor, the plasma concentration and urinary excretion after an oral administration of KR-30075 (4mg/kg) in the male rat (Sprague Dawley) were determined by high performance liquid chromatography. The best extraction efficiency of KR-30075 and KR-30072 is obtained with ethyl ether adjusted to pH 4.0. Retention times of both KR-30072 and KR-30075 were within 5 min and resolution was complete at the flow rate of 1.0ml/min. The sensitivity and specificity of this HPLC assay appears to be satisfactory for the pharmacokinetic study of KR-30075 and its metabolites. One-compartment open model with first-order absorption was applied to evaluate the pharmacokinetic parameters of KR-30075 according to Minimum AIC Estimation. Tmax was 1 hr, Cmax was 0.789 +/- 0.31 mcg/ml and elimination half T1/2 was 6.31 min after oral administration of 4mg/kg KR-30075 to male rats.