[Pharmacokinetics and bioavailability of the myotonolytic N-(hydroxy-2-ethyl)-cinnamide (author's transl)]

The bioavailability, the absorption and elimination rate (biological half-life) as well as the volume of distribution for different routes of application were tested for the myotonolytic N-(hydroxy-2-ethyl)-cinnamide (LCB-29). 60 mg were administered i.v., 400 mg p.o. and 400 mg or 7 X 200 mg as ointment. For the i.v. and oral application the serum levels as well as the urine levels were determined. The amount of LCB-20 which may have been present in the urine after the ointment application was below the limit of detection. Serum concentrations were determined 10 times within 24 h after each application. Based on these values an absolute bioavailabiltiy for the LCB-29-ointment could be estimated at 1% in an application on 200 cm2 skin. This proved that the absorption of LCN-29 as ointment is very low compared to that in the oral application (absolute bioavailability 30%). The half-life was determined to be quite similar for all 3 routes of application: approximately 1 h. The absorption rate decreased by the factor 1.7 when LCB-29 was administered cutaneously instead of orally.