[Comparative studies on the bioavailability of nicergoline from two different steady-state preparations]. / Vergleichende Untersuchungen zur Bioverfügbarkeit von Nicergolin aus zwei unterschiedlichen Darreichungsformen im Steady State.

ABSTRACT

Comparative Studies on the Bioavailability of Nicergoline from Two Different Preparations in Steady State The bioavailability of nicergoline (CAS 27848-84-6) in a new 30 mg tablet and a 10 mg dragee formulation (Sermion) was evaluated under steady state conditions in 18 healthy male volunteers between the age of 21 and 37 years. During the run-in phase, the volunteers received on 7 consecutive days 30 mg nicergoline either 1 x 30 mg/d tablet (test substance) or 3 x 10 mg dragees (reference). On day 8, after intake of 1 x 30 mg in a 24 h interval or 1 x 10 mg in a 8 h interval respectively, the plasma concentrations of the nicergoline metabolite 10-methoxy-6-methyl-ergoline-8 beta-methanol (MDL) were measured. The area under the plasma concentrations in the 24 h interval after administering the 30 mg tablet was not 3 times greater as to be expected; it was by a factor of 4 significantly greater than the area under the curve of the 10 mg dragee in the 8 h interval. Therefore, nicergoline has a higher availability in the 30 mg tablet than in the 10 mg dragee form. Both formulations were equally well tolerated.