Phase 1 Trial of Single Dose of Sustained Release Capsule of Urapidil (BKU), in Healthy Volunteers
1983 Volume 14 Issue 3 Pages 529-544
Details
1983 Volume 14 Issue 3 Pages 529-544
The sustained-release capsule of urapidil (BKU), a new antihypertensive currently on the West German market as Ebrantil®, was studied in a phase 1 trial with doses ranging 15-90mg (1/ (2-3) times the German dosage), and the results obtained were as follows:
1. Orthostatic disorders, side effects on the central nervous system and vasodilative symptoms and gastrointestinal disorders were found dose-dependently. These mild symptoms were occurred mostly 4 hr after administration in related with the plasma levels and thereafter disappeared.
2. Blood pressure was lowered at the dose of 60mg in the standing position and 90mg in supine, sitting and standing position. No other drug-related changes were observed in heart rate, electrocardiogram and laboratory findings.
3. In pharmacokinetic studies, the present results were in agreement with thoseobtained with German volunteers, and detectable racial differences were not observed. In a total of 18 cases, T1/2 and maximum plasma concentration time (Tmax) were 3.2±0.3hr (mean± S.E.) and 3.8±0.2hr, respectively. Maximum plasma concentration (Cmax) and AUC were dose-dependent. Recoveries in 24 hrurine were11.8±1.8% to 18.3±3.1% for the unchanged, 20.8±4.3% to 30.8±1.8% for hydroxylated metabolite and 2.2±0.4% to 2.9±0.6% for N-demethylated metabolite.
