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  • Title: [Pharmacokinetics of AR-L 115 BS in rhesus monkeys (author's transl)].
    Author: Mierau J.
    Journal: Arzneimittelforschung; 1981; 31(1a):221-5. PubMed ID: 7195226.
    Abstract:
    Pharmacokinetic studies of the cardiotonic agent 2-[(2-methoxy-4-methylsulfinyl)phenyl]-1H-imidazo[4,5-b]pyridine (AR-L 115 BS) in rhesus monkeys following oral and intravenous administration of the 14C-labelled compound were performed. 1. Following oral administration the blood- and plasma level maximum was reached between 1 and 3 h with an average maximum concentration of 8% (whole blood) and 4% (plasma) of the administered dose. 3 h after reaching the maximum concentration the blood and plasma level had fallen to half the maximum concentration. The substance was absorbed completely. 2. Following i.v. injection the elimination of radioactivity from blood and plasma, resp., showed a two-phase course with elimination half-lives of t1/2 alpha = 75 min and t1/2 beta = 12 h. 3. Within 120 h following oral and i.v. administration, 95% and 91%, resp., of the administered radioactivity were excreted. Following both ways of administration a relatively rapid renal excretion occurred. 4. The distribution pattern of the urine metabolites showed a complete biotransformation of the initial compound. In all urinary fractions two main metabolites occurred. Because of the identical metabolite pattern a different metabolic behaviour following oral and i.v. administration can be excluded.
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