[The pharmacokinetics of an immunomodulator of the D-homo-8-azasteroid series].
The pharmacokinetic investigation and the study of metabolism of an immunostimulator of 8-azasteroid series were performed on a single-compartment model. The main pharmacokinetic parameters of the immunomodulator in mice were established using different routes of administration. The maximal accumulation of tritium-labeled 8-azasteroid was recorded in the kidneys, liver and lung. The character of distribution changes with time. The half-life period is in the range of from 0.69 to 1.4 hours at different routes of administration. The total clearance is 0.49 ml/min, the area under the pharmacokinetic curve--3.8-8.1 micrograms/h/ml. On the model of the monooxygenase cytochrome P-450-containing system of the liver microsomes there was confirmed the formation of two metabolites preliminarily isolated from the mouse urine. By the character of resorption, distribution, elimination this 8-azasteroid immunoactivator is close to the agents of glucocorticoid series.
Kuz'mitskiĭ
B B
BB
Stoma
O V
OV
Slepneva
L M
LM
Mashkovich
A E
AE
Nasek
V M
VM
D000276:Adjuvants, Immunologic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D001378:Azasteroids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D005260:Female; D006207:Half-Life; D006900:Hydroxylation; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008862:Microsomes, Liver / Q000201:enzymology; D013260:Steroids, Heterocyclic / Q000493:pharmacokinetics*; D013997:Time Factors; D014018:Tissue Distribution; D014316:Tritium
D000276:Adjuvants, Immunologic; D001378:Azasteroids; D013260:Steroids, Heterocyclic; D014316:Tritium; D003577:Cytochrome P-450 Enzyme System
Farmakokinetika immunomoduliatora riada D-gomo-8-azasteroidov.