포스포디에스테라제 Ⅲ의 저해물인 KR-30075의 흰쥐에서의 약물속도론 = Pharmacokinetics of KR-30075, A Potent Phosphodiesterase Ⅲ Inhibitor in Rats

다국어 초록 (Multilingual Abstract)

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 (4 ㎎/㎏) in the male at 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 1.0 ㎖/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 pharmacohinetic parameters of KR-30075 according to Minimum AIC Estimation.T_max was 1 hr, C_max was 0.789±0.31 ㎍/㎖ and elimination half T_(1/2) was 6.3l min after oral administration of 4 ㎎/㎏ KR-30075 to male rats.