Pharmacokinetics of a chemoprotective agent, 2-(allylthio)pyrazine, after intravenous administration to rabbits.
The pharmacokinetics of 2-(allylthio)pyrazine (2-AP) were evaluated after intravenous administrations of the drug to rabbits. The reason for the multiple peaks in the plasma concentration of 2-AP after intravenous administration of the drug to rabbits were also investigated. After intravenous administration of 2-AP, 10, 20, and 50 mg/kg, to rabbits, the pharmacokinetic parameters of 2-AP, such as the total area under the plasma concentration-time curve from time 0 to 12 h (261, 672, and 1190 micrograms min/ml), the total body clearance (38.3, 42.0, 44.6 ml/min/kg), and the percentages of intravenous dose of 2-AP excreted in 24 h as unchanged drug (0.0306, 0.0252, and 0.0492%), were independent of the dose ranges studied. Since the amount of 2-AP excreted in 12-h bile as unchanged drug after intravenous administration of 2-AP, 20 mg/kg, was only 0.0241 +/- 0.00156%, and some of 2-AP excreted in gastrointestinal tract as unchanged drug was reabsorbed, the reason for the appearance of multiple peaks after intravenous administration of 2-AP could be at least partly due to gastrointestinal excretion of the drug.
Han
K S
KS
College of Pharmacy, Seoul National University, South Korea.
Woo
S J
SJ
Koo
C H
CH
Lee
M G
MG
D000818:Animals; D019540:Area Under Curve; D001646:Bile / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D007262:Infusions, Intravenous; D008297:Male; D011719:Pyrazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011817:Rabbits
C104935:2-(allylthio)pyrazine; D004791:Enzyme Inhibitors; D011719:Pyrazines