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  • 1
    ISSN: 1573-904X
    Keywords: etintidine ; high-performance liquid chromatography (HPLC) ; solid extraction ; determination of etintidine in plasma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract This paper describes a new, rapid solid extraction method for the determination of etintidine in plasma. The method employs a semiautomatic sample preparation system. Plasma samples and the internal standard (cimetidine) were applied onto octyl-bonded silica extraction columns. The extraction columns were then subjected to Tris buffer and water wash and were subsequently loaded onto an automatic sample injection system. The contents of the extraction columns were eluted on-line with a mobile phase of acetonitrile:methanol:0.1% ammonium hydroxide (85:10:5, by volume) onto a silica analytical column and detected by UV absorption at 229 nm. The chromatographic condition separates etintidine from some of its metabolites and other endogenous components in plasma. The detection limit for etintidine was 0.02–0.05 µg/ml when 0.2 ml of plasma was used. This method has been used for the determination of plasma etintidine levels in humans and mice after oral administration of etintidine and was found to be suitable for pharmacokinetic/bioavailability studies of etintidine in humans and animals. The method can also be used for the quantitative determination of cimetidine and certain metabolites of etintidine.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1573-8744
    Keywords: etintidine ; propranolol ; 4-hydroxypropranolol ; interaction ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Etintidine HCl is a potent H2 -blocker. The effect of clinical doses of etintidine on the disposition of a single oral dose of propranolol was investigated in 12 normal subjects. This was a double-blind, two-way crossover study. Each subject received etintidine (400 mg) or placebo twice a day with meals for 4 days on two occasions (separated by 4 days). On each occasion, the subjects were fasted overnight on Day 3 and were given an oral dose of Inderal® (40 mg propranolol hydrochloride) 30 min following the administration of the morning dose of etintidine or placebo on Day 4. Blood samples were collected prior to and up to 24 hr following the administration of propranolol. The plasma samples were analyzed for propranolol and 4-hydroxypropranolol by HPLC. Comparison of the pharmacokinetic parameters of propranolol between etintidine and the placebo groups indicates that etintidine significantly increased the AUC0−∞,values (573.5 vs. 146.4 ng·hr/ml, p=0.0001)and prolonged the elimination half-life (4.61 vs. 2.33 hr) of propranolol. Statistical evaluation of the pharmacokinetic parameters of 4-hydroxypropanolol indicates that etintidine also increased the AUC0−24 values (43.8 vs. 16.4 ng·hr/ml, p=0.0028) and prolonged the elimination half-life (4.87 vs. 1.97 hr) of 4-hydroxypropranolol. The data suggest that etintidine, like cimetidine, impaired the elimination of propranolol. Etintidine also protracted the elimination of 4-hydroxypropranolol, an active metabolite of propranolol.
    Type of Medium: Electronic Resource
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