The plasma concentration and urinary excretion of 15 (R)-15-methylprostaglandin E2 (Arbaprostil, CU-83) and its 15 (S)-15-methyl epimer (CU-83 (S)) were studied in healthymale volunteers after a single oral administration of CU-83.
Maximum plasma concentrations of CU-83 following the administration at doses of 20, 40 and 60μg were 127.4, 152.8 and 164.2pg/ml, respectively, from 0.6 to 0.9hr. On theother hand, maximum plasma concentration of CU-83 (S) following the administration was7.4 pg/ml at 1.1hr in the case of 20μg dose, 17.7pg/ml at 1.0 hr in 40μg and 44.1pg/mlat 1.0hr in 60μg.
Urinary excretion half-lives of CU-83 and CU-83 (S) were 1.2-1. 6hr and 3. 2-5.2hr, respectively. Of the administered dose, 1. 45-1. 65% as CU-83 and 0.98-1.62% as CU-83 (S) were excreted in urine until 24 hr after administration.
