Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part II: Pharmacokinetics in primates after repeated oral or single intravenous administration.
The pharmacokinetics of BM 113 (1-(benzhydryloxyethyl)piperidino-4-ethylacetate, CAS 115313-90-1; BM 113 maleate: CAS 115313-91-2) was studied using 3H-BM 113 in the Cynomolgus primate. Oral repeated administration of 0.75 mg/kg was performed on 8 days. 40 days after the oral treatment, a single intravenous administration of 0.4 mg/kg was done. Whatever the administration route, the radioactivity excretion was essentially urinary (about 60%) and most of the radioactivity was excreted within the first 24 h. The faecal elimination was low, about 10% of the administered dose. 40 days after the treatment, some radioactivity was already present in the urine. For this reason, the excretion balance ranged from 70 to 83% of the dose. The elimination half-life of 3H-BM 113 was long, about 80 h.
Duchêne
P
P
ADME Bioanalyses, Mougins, France.
Guidicelli
M D
MD
Tran
G
G
Ladure
P
P
Ollivier
R
R
Buzas
A
A
Merour
J Y
JY
Houin
G
G
D000284:Administration, Oral; D000818:Animals; D018926:Anti-Allergic Agents / Q000097:blood / Q000378:metabolism / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001711:Biotransformation; D005243:Feces / Q000737:chemistry; D006207:Half-Life; D007275:Injections, Intravenous; D008252:Macaca fascicularis; D010880:Piperidines / Q000378:metabolism / Q000493:pharmacokinetics*
D018926:Anti-Allergic Agents; D010880:Piperidines; C121324:BM 113