The effect of food on the absorption of alpha-tocopheryl nicotinate in beagle dogs and human volunteers.

Abstract

The effect of food on absorption of d,1-alpha-tocopheryl nicotinate was studied in cross-over studies with eight beagle dogs and four human volunteers. When 100 mg of alpha-tocopheryl nicotinate in gelatin capsule was administered p.o. to beagle dogs in both a fasted state and after eating, the plasma peak level (Cmax) and area under the curve (AUC) of this ester in nonfasted state was five-fold higher than in fasted state, although the peak time (tmax) did not markedly differ between both conditions. Cmax and AUC after oral administration of 600 mg of alpha-tocopheryl nicotinate in human volunteers in nonfasted state was 32-fold and 29-fold higher, respectively, than during fasted state, without delay in tmax. The plasma levels of this ester following ingestion of 200 mg in fasted state were not detectable. A comparison of the 600-mg with 200-mg dose level during nonfasted state showed the former to be 1.8-fold higher in Cmax and 2.3-fold in AUC.