THE EFFECT OF FOOD ON THE ABSORPTION OF ALPHA-TOCOPHERYL NICOTINATE IN BEAGLE DOGS AND HUMAN VOLUNTEERS

  • 1 January 1981
    • journal article
    • research article
    • Vol. 19  (5) , 216-219
Abstract
D,1-.alpha.-Tocopheryl nicotinate is a peripheral vasodilator that has been widely used in Japan for improving blood circulation impediment following coronary insufficiency and cerebral apoplexia. The effect of food on absorption of d,1-.alpha.-tocopheryl nicotinate was studied in cross-over studies with 8 beagle dogs and 4 human volunteers. When 100 mg of .alpha.-tocopheryl nicotinate in gelatin capsule was administered p.o. [per os] 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 5-fold higher than in fasted state, but 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 the 200 mg dose level during nonfasted state showed the former to be 1.8-fold higher in Cmax and 2.3-fold in AUC.

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