PMID: 11913718Mar 27, 2002Paper

Pharmacokinetics, stability, and blood partition of DA-8159, a new phosphodiesterase V inhibitor

Research Communications in Molecular Pathology and Pharmacology
H J ShimM G Lee

Abstract

The pharmacokinetics of DA-8159, a new phosphodiesterase V inhibitor, after 1 min intravenous, 30 mg/kg, and oral, 30 mg/kg, administration of the drug to rats, the stability of DA-8159 in various pH solutions ranging from 1 to 13, and human and rat plasma and urine, and the blood partition of DA-8159 between plasma and blood cells of rabbit were evaluated. After intravenous administration, DA-8159 was eliminated fast with the mean total body clearance of 126 ml/min/kg, and was almost completely metabolized in rats; 5.98% of intravenous dose of DA-8159 were excreted unchanged in 24-hr urine. The extent of absolute oral bioavailibility of DA-8159 was approximately 25%. The apparent volume of distribution at steady state was considerably large, 15048 ml/kg, suggesting that DA-8159 has a good affinity to rat tissues. DA-8159 was relatively stable in various pH solutions, and human and rat plasma and urine for up to 48 h incubation in a water-bath shaker kept at 37 degrees C and at a rate of 50 oscillations per min. DA-8159 reached equilibrium fast (within 30 sec mixing manually) between plasma and blood cells of rabbit blood and the plasma-to-blood cell concentration ratios were independent of initial blood concentrations of DA-81...Continue Reading

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