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Fasting and postprandial absorption of digoxin from a microencapsulated formulation

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Summary

The absorption of digoxin from a capsule preparation containing a large number of small, enteric-coated granules of the glycoside (Preparation CR) was compared in 10 volunteers with that from a rapidly dissolving tablet (Preparation L). Plasma and urine digoxin concentrations were measured by radioimmunoassay. In the fasting state, after a loading dose of digoxin (0.76 mg), peak plasma concentrations were significantly (p<0.001) lower after CR (2.0±0.5 nmol/l, mean±SD) than L (4.7±1.1 nmol/l). Peak concentrations after CR were significantly (p<0.001) delayed compared to L (3.3±0.6 h vs 1.1±0.4 h). Also, postprandial peak plasma concentrations at steady state, were significantly (p<0.01) lower after CR (1.0±0.3 nmol/l) than L (2.7±0.5 nmol/l), and the peak concentrations occurred later (3.9±1.7 h vs 1.4±0.9 h). The area under the plasma concentration-time curves was smaller (p<0.01) for CR (17.7±5.9 nmol·l−1·h) than for L (22.4±4.1 nmol·l−1·h), and so was the amount of drug excreted in urine (174±25 µg vs 190±31 µg; p<0.005). Thus, the absorption rate of digoxin from the enteric-coated formulation was markedly reduced but at the cost of a variable reduction in the amount absorbed.

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Bergdahl, B., Bogentoft, C., Jonsson, U.E. et al. Fasting and postprandial absorption of digoxin from a microencapsulated formulation. Eur J Clin Pharmacol 25, 207–210 (1983). https://doi.org/10.1007/BF00543792

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  • DOI: https://doi.org/10.1007/BF00543792

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