COMPARISON OF BIOAVAILABILITY OF DIGOXIN IN CAPSULE, TABLET, AND SOLUTION TAKEN ORALLY WITH INTRAVENOUS DIGOXIN

  • 1 January 1976
    • journal article
    • research article
    • Vol. 16  (10) , 461-467
Abstract
Six healthy volunteers were given 5 single-dose treatments of 0.40 mg digoxin either i.v., in liquid form, in conventional tablet form (dissolution rate 76% in 1-h) or in new capsule preparations containing 0.05, 0.10 or 0.20 mg digoxin/capsule. Serum levels, area under the concentration-time curve, and daily urinary digoxin excretion were measured for 6 days. Higher serum digoxin levels were seen after ingestion of the capsules than after the tablets, with peak levels for the former being 2.2-2.8 times higher than after tablet digoxin. Bioavailability was assessed further by comparing the area under a 6 h concentration-time curve, and again the capsules gave a consistently higher value than the tablets. The absorption of 0.40 mg digoxin from any of the capsule preparations was much greater than 0.50 mg digoxin in commercially available tablets. The 6-day cumulative urinary digoxin excretion was also greater for the capsules than for the 0.20-mg tablets. In comparison with i.v. digoxin, tablets provide 75% maximum bioavailability, whereas the capsule preparations of digoxin improve the bioavailability of digoxin and the 0.20-mg digoxin capsule is absorbed better than 0.25-mg digoxin tablet.

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