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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 197-202 
    ISSN: 1432-1041
    Keywords: digoxin ; hydrolysis metabolites ; enteric coating ; dihydrodigoxin ; liquid chromatography ; RIA ; urine ; plasma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A capsule preparation containing small, enteric-coated granules of digoxin was developed to prevent acid hydrolysis of the drug in the stomach and to diminish the variation in plasma glycoside concentration during the intervals between doses. The absorption and metabolism of tritiated digoxin after a single oral loading dose of this formulation (Formulation C) were compared to those after ingestion of a digoxin solution (Formulation S) by 8 healthy men. Drug concentrations were measured by radioimmunoassay (RIA) and liquid chromatography (LC). The percentage of the digoxin dose excreted in the urine during 72 h, as measured by RIA, was significantly lower after the capsule (20.5±2.0% vs 36.2±3.0% after S, mean±SEM) but total urinary radioactivity after the two treatments was similar (C 35.3±5.2 and S 41.2±2.6%; p〉0.05). The discrepancy was mainly due to significantly greater excretion of dihydrodigoxin after the capsule ( $$\bar m$$ 12.8%, range 0–28.6% of the dose) than after the digoxin solution ( $$\bar m$$ 5.4%, range 0–14.5%). Dihydrodigoxin was not measured by the RIA. The recovery of hydrolysis metabolites (LC) was greater during the first 24 h after S (2.3±0.6% vs 0.9±0.3% after C; p〈0.05). The peak plasma concentration of digoxin (RIA) was significantly reduced and delayed after intake of C (2.5±0.4 nmol/l at 3.8±0.3 h vs. 8.3±0.8 nmol/l at 0.9±0.1 h after S), and so was the shortening of electromechanical systole at 1.5 h, 2.5 h, and 3 h. Thus, the enteric-coated digoxin preparation delayed the absorption and reduced the hydrolysis of the glycoside, but it also carried the drawback of reducing digoxin availability, mainly because of increased metabolism to dihydrodigoxin.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 17 (1980), S. 443-447 
    ISSN: 1432-1041
    Keywords: digoxin ; enteric coating ; absorption ; radioimmunoassay ; urinary digoxin ; plasma digoxin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of digoxin from two capsule preparations containing a large number of small, enteric-coated granules of the glycoside (0.38 mg) was compared with that of the same amount from ultrarapidly dissolving commercial tablets. Eight volunteers were studied during steady state conditions. Digoxin concentrations in plasma and urine were measured by radioimmunoassay. Peak plasma concentrations of digoxin were significantly (p〈0.01) delayed after taking the capsules (2.6±1 h and 2.6±0.9 h, mean±SD) as compared to the tablets (1.3±0.7 h). The peak concentrations produced by the capsules were 3.1±1.0 and 2.6±1.1 nmol/l; only the latter was significantly (p〈0.05) lower than after the tablets (3.4±1.0 nmol/l). Areas under the plasma concentration-time curves during a 24 h dosage interval were similar for the three preparations, and so was the 24 h urinary excretion of digoxin, which averaged 60–63% of the daily dose. Thus, this particular enteric coating of digoxin delayed absorption without reducing the amount absorbed.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 207-210 
    ISSN: 1432-1041
    Keywords: digoxin ; absorption ; enteric coating ; radioimmunoassay ; urinary digoxin ; plasma digoxin ; dissolution rate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: 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.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Anaesthesia 38 (1983), S. 0 
    ISSN: 1365-2044
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Twenty patients undergoing microlaryngoscopy were anaesthetised with thiopentone and nitrous oxide. Half of the patients received 1.0–1.5 mg of fentanyl during anaesthesia, the effect of which was antagonised by naloxone 0.4 mg intravenously and 0.4 mg subcutaneously. The other patients served as controls and received saline instead of fentanyl and naloxone. Fentanyl markedly reduced mean arterial pressure and the heart rate-systolic arterial pressure product during microlaryngoscopy. Conversely, there were significant increases in these measurements after naloxone had been given. However, there were no significant differences between patients given fentanyl with naloxone, and those given saline, in respect of arterial pressure, heart rate or dysrhythmia during recovery. No patient vomited, or appeared nauseated when observed afterwards in the operating room. One patient vomited several hours after naloxone.
    Type of Medium: Electronic Resource
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