[The pharmacokinetics of Z-2-amino-5-chlorobenzophenoneamidinohydrazone in the rat].
Model-independent and model-dependent pharmacokinetic parameters were determined from the course of total radioactivity in blood following single i.v., p.o. and i.p. administration of two different doses of Z-2-amino-5-chloro-14C-benzophenoneamidinohydrazone (14C-1). Following i.v. administration of 14C-1 the total radioactivity in blood exhibits dose-dependent pharmacokinetics. After i.v. administration of 1,4.10(-6) mol.kg-1 14C-1 the terminal half-life has been found with 7 h, whereas this value is 32 h after administration of 4,4.10(-5) mol.kg-1 to female rats and 18 h after administration of 3,1.10(-5) mol.kg-1 to male rats. The apparent volume of distribution increases when the dose is increased. Following p.o. administration of 1,4.10(-6) mol.kg-1 and 4,1.10(-4) mol.kg-1 14C-1 the extent of absorption amounts to 21 and 59%, respectively. This effect of dose is related to the dose-dependent prolongation of gastrointestinal passage. After i.p. administration of 14C-1 the rate and extent of drug absorption is high. The time course of total radioactivity in blood is similar to that after i.v. administration.
Schieweck
A
A
Fachbereich Pharmazie, Humboldt-Universität zu Berlin.
offchert
H H
HH
Morgenroth
U
U
Joram
U
U
D000284:Administration, Oral; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001577:Benzophenones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001711:Biotransformation; D005260:Female; D006207:Half-Life; D006835:Hydrazones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D008297:Male; D008954:Models, Biological; D051381:Rats; D017208:Rats, Wistar
D000889:Anti-Arrhythmia Agents; D001577:Benzophenones; D006835:Hydrazones; C080444:(Z)-2-amino-5-chlorobenzophenonamidinohydrazone acetate
Untersuchungen zur Pharmakokinetik von Z-2-Amino-5-chlorbenzophenonamidinonhydrazon an der Ratte.