Absorption, Distribution and Excretion of OPB 2045 following a Single Subcutaneous Administration to Beagle Dogs
1998 Volume 13 Issue 1 Pages 8-12
Details
1998 Volume 13 Issue 1 Pages 8-12
The absorption, distribution and excretion of radioactivity were investigated in male beagle dogs following a single subcutaneous administration of 14C-labeled OPB-2045 at 1 mg/kg and the following results were obtained:
1. Blood concentrations of radioactivity reached maximum levels (Cmax) of 0.074μg eq. /ml at 30 min after dosing and then declined with half-lives of 29.5 hr and 58.6 hr as determined at 30 min to 12 hr and 12 hr to 168 hr, respectively, postdosing. The area under the concentration-time curve (AUC0→∞) was 5.40μg eq.·hr/ml. Serum concentrations of radioactivity reached Cmax of 0.084μg eq./ml at 30 min postdosing. The half-life of radioactivity in serum was 34.4 hr and 67.6 hr. AUC was 6.03μg eq.·hr/ml.
2. Radioactivity in blood cells during 30 min to 168 hr postdosing accounted for 28.3-46.5% of total radioactivity in the blood.
3. Radioactivity was highest in kidneys, followed by thyroid, pituitary gland, lungs, heart, liver and adrenal glands, showing 0.084-0.994μg eq./g, at 168 hr postdosing. 2.1% of the administered dose remained at the administration site.
4. Urinary and fecal excretion of radioactivity for 168 hr postdosing accounted for 59.4% and 23.5% of the administered doses, respectively.
