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  • pharmacokinetics  (30)
  • Triticum aestivum  (9)
  • Differential-scanning-calorimetry  (8)
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  • Springer  (60)
  • 2015-2019
  • 1980-1984  (60)
  • 1983  (49)
  • 1980  (11)
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  • Springer  (60)
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  • 2015-2019
  • 1980-1984  (60)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 17 (1980), S. 111-116 
    ISSN: 1432-1041
    Keywords: zimelidine ; norzimelidine ; antidepressants ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The systemic availability of a new antidepressant, zimelidine, and of its pharmacologically active metabolite, norzimelidine, was studied in six healthy male volunteers. Three single doses of zimelidine (25 mg and 100 mg orally and 25 mg i.v.) and two single doses of norzimelidine (25 mg orally and i. v.) were given to each volunteer allowing at least seven days between administrations. Plasma concentrations of zimelidine and norzimelidine were determined in serial blood samples by HPLC. Following oral zimelidine peak plasma concentrations of the metabolite were attained about 3 h after dosing. Oral administration of norzimelidine itself resulted in a plasma concentration profile for this compound that was similar to that observed after oral zimelidine. Utilising the plasma concentration data following intravenous infusion of each compound, the elimination half-lives for zimelidine and norzimelidine were calculated to be 5.1 h (range 4.3–6.0) and 15.5 h (range 10.6–22.9) respectively. The total body clearances of the 2 compounds were similar at 0.52 l · min−1 (range 0.26–0.70) for zimelidine and 0.56 l · min−1 (range 0.28–0.83) for norzimelidine. The substantially longer elimination half-life of norzimelidine was apparently the result of a larger volume of distribution (9.4 l · kg−1; range 7.8–11.4) for this metabolite, as compared to zimelidine (3.21 · kg−1; range 1.6–4.9). The calculated bioavailability of zimelidine was 26% (range 9.1–39) after the 25 mg oral dose, and 29% (range 14–46) after the 100 mg dose. The bioavailability of norzimelidine was 66% (range 36–91). However, oral administration of zimelidine resulted in as much or more norzimelidine reaching the systemic circulation, as the oral administration of norzimelidine itself. This is important as a large part of the activity of the drug may be due to the metabolite.
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  • 2
    ISSN: 1432-1041
    Keywords: cimetidine ; intravenous infusion ; pharmacokinetics ; peptic ulcer ; duration of infusion ; acute dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The use of cimetidine administered by bolus intravenous injection to critically ill patients has been associated with serious cardiac arrhythmias, due presumably to high initial plasma concentrations. The aim of this study was to determine the range of infusion times of a single 200 mg dose of cimetidine which would avoid high initial drug concentrations while maintaining a duration of effective concentrations no less than that resulting from bolus injection. Computer simulations of both maximum plasma cimetidine concentrations and duration of effective plasma cimetidine concentrations versus duration of infusion were based on mean pharmacokinetic date from 6 peptic ulcer patients who had received cimetidine 200 mg i.v. over 5 min. The simulations indicated that to reduce maximum plasma cimetidine concentrations by at least 50%, while maintaining the duration of effective plasma concentrations, the infusion time should be at least 30 min and no longer than 4.5 h. The validity of the simulations was subsequently tested in 4 of the patients, who received cimetidine 200 mg i.v. over 30 min. The mean maximum plasma concentration for the 30 min infusion (4.57±0.53 µg/ml) was, as predicted, approximately half that corresponding to bolus administration in these patients (8.97±1.96 µg/ml). Moreover, the duration of effective concentrations for the infusion (1.43±0.28 h) was significantly greater than that for the 5 min infusion (1.21±0.31 h). We suggest that where an acute intravenous dose of cimetidine (200 mg) is indicated, it should be administered over at least 30 min rather than as a bolus.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 567-568 
    ISSN: 1432-1041
    Keywords: astemizole ; ethanol ; antihistamine ; pharmacodynamics ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of astemizole (10 mg daily for 7 days) on the kinetics and CNS depressant activity of ethanol have been examined in a double-blind cross-over study agonist placebo in 7 volunteers. There was no significant change in the elimination rate or AUC of the plasma ethanol concentration-time curve after astemizole. Central nervous system effects of ethanol as monitored by visual analogues of sedation, visual discrimination, pursuit rotor and reaction time were also unaffected by astemizole pretreatment.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 24 (1983), S. 349-352 
    ISSN: 1432-1041
    Keywords: diltiazem ; pharmacokinetics ; intravenous dose ; oral dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetic profile of diltiazem, a novel calcium antagonist, was studied in 12 volunteers following oral (60 mg) and intravenous (15 mg) administration. After i.v. administration biphasic elimination was observed, with a distribution half-life of 0.3±0.2 h and an elimination half-life of 3.1±1.0 h; the apparent volume of distribution was 5.3±1.71/kg and the total clearance was 1.28±0.48 l/kg/h. After the oral dose the elimination phase had a half-life of 3.2±1.3 h. The absolute bioavailability of diltiazem ranged from 24 to 74% (mean 42±18%). The interindividual variation may be explained by a variable first pass effect.
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  • 5
    ISSN: 1432-2242
    Keywords: HMW glutenin subunit genes ; cDNA clones ; Tandem DNA repeats ; Chromosomal location ; Gene copy number ; Wheat ; Triticum aestivum
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary cDNA clones encoding wheat HMW glutenin subunits have been isolated from a cDNA bank made to poly A+ RNA from developing wheat endosperm var. Chinese Spring. One such clone, pTag 1290, has enabled us to identify the HMW glutenin mRNA species. The DNA sequence of this clone has been partially determined and it contains several tandem DNA repeats. The sequence is discussed in relation to the generation of the HMW glutenin subunit gene family. Analysis of the organization of the HMW glutenin sequences in the wheat genome revealed that the genes encoding HMW glutenin subunits exist in low copy number and are located on the long arm of each of the homoeologous group 1 chromosomes.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 11 (1983), S. 183-187 
    ISSN: 1573-8744
    Keywords: nonlinear regression ; parameter estimation ; invariance ; transformation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract It is shown that when one nonlinear regression model is a reparametrization of a second model, the parameter estimates, and their standard errors, for one model can be obtained directly from those obtained from fitting the other model.
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  • 7
    ISSN: 1573-8744
    Keywords: naltrexone ; controlled release ; pharmacokinetics ; gas chromatography ; biodegradable copolymer delivery system ; release rate quantitationin vivo ; Loo-Riegelman method
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Naltrexone release rates from a controlled release delivery system have been quantitated over a time period greater than one month in the monkey. The method requires calibration of the pharmacokinetic parameters of each monkey utilizing an intravenous bolus dose and assay of unchanged naltrexone levels in plasma as a function of time after dosing. Also required are periodic plasma levels of unchanged naltrexone obtained subsequent to administration of the delivery system. Release rates are then calculated as well as the total amount released. Application of the methodology to a biodegradable copolymer naltrexone delivery system in three monkeys showed an initial release rate of 3– 8% of the dose per day over the first 3– 5 days followed by a slow, rather constant release rate of 1– 3% per day from day 5 to the time of the last measurable plasma sample (36– 43 days). Comparison of alternative calculation methods using both experimental and simulated plasma naltrexone data verified the accuracy of the release rate calculations. The sum of the calculated total amount of naltrexone released plus the assayed amount remaining in the delivery system after removal from the animal accounted for 91– 94% of the administered dose in the two monkeys in which complete data were obtained.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Colloid & polymer science 261 (1983), S. 286-292 
    ISSN: 1435-1536
    Keywords: Differential-scanning-calorimetry ; homologous lecithins ; phase transition enthalpies ; phase transition temperatures ; hydration behaviour
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Description / Table of Contents: Abstract 1. By means of differential-scanning-calorimetry the phase transition temperatures and -enthalpies were determined and evaluated for the three following lecithin/water systems: 1,2-dimyristoyl-lecithin/water; 1,2-dipalmitoyl-lecithin/water; 1,2-distearoyllecithin/water. 2. The preparation of the lecithin/water mixtures was made by adsorption of water from the gaseous phase. The adsorption isotherms were evaluated by the BET equation. 3. Four phase transitions were found for the monohydrates of the lecithins. The parameters depend systematically on the length of the alkyl residues. 4. In the heterogeneous two phase region the main-transition and the pre-transition occurred. The thermodynamical parameters of both transitions depend on the alkyl chain length. 5. Whole the results refer to the conclusion that the lecithin head group hydration is a stepwise process. The hydration of the first shell is finished if 5 to 6 molecules water per molecule lecithin are present, while the second hydration shell is complete when about 13 water molecules are adsorbed
    Notes: Zusammenfassung 1. Mittels Differential-Scanning-Kalorimetrie wurden die Umwandlungstemperaturen und -enthalpien folgender 3 binärer Systeme im Konzentrationsbereichx W=0,5 bisx W=0,97x W=Molenbruch, bezogen auf Wasser) systematisch untersucht und ausgewertet: 1,2-Dimyristoyllecithin/Wasser, 1,2-Dipalmitoyllecithin/Wasser und 1,2-Distearoyllecithin/Wasser. 2. Die Herstellung der Lecithin/Wasser-Mischungen erfolgte durch Adsorption des Wassers aus der Gasphase. Die Adsorptionsisotherme wird angegeben und mittels BETGleichung ausgewertet. Für die Monoschichtadsorption wird ein Wert von 2,5 mol Wasser/mol Lecithin gefunden. 3. Der Vergleich des Phasenverhaltens der Lecithin-Monohydrate ergibt 4 Umwandlungspeaks, deren Umwandlungsparameter in regelmäßiger Weise von der Kettenlänge der KWReste beeinflußt sind. Sie entsprechen temperaturaufwärts folgenden Strukturänderungen:L C →R α →Q α →H α (L C=lamellare Phase, KW-Ketten rigid;R α=rhomboedrische Phase, KW-Ketten fluid;Q α=kubische Phase, KW-Ketten fluid;H α=hexagonale Phase, KW-Ketten fluid). 4. Mit zunehmendem Wassergehalt verschwinden die Hochtemperaturumwandlungen der Monohydrate. Im heterogenen Zweiphasengebiet tritt dann neben der Hauptumwandlung temperaturabwärts zusätzlich die Vorumwandlung auf. Die Parameter beider Umwandlungen sind kettenlängenabhängig. 5. Die Temperaturen der Hauptumwandlungen fallen mit steigendem Wassergehalt, insbesondere in der Nähe des wasserreichen Gebietesx W∼0,85), sprunghaft ab und bleiben im heterogenen Zweiphasengebiet konstant. Umgekehrt steigen die Enthalpien der Hauptumwandlung, bezogen auf die wasserfreien Lecithine, im gleichen Gebiet sprunghaft an. Die Umwandlungsenthalpien der Lecithin/Wasser-Mischung zeigen dagegen einen linearen Verlauf in Abhängigkeit vom Wassergehalt der Mischung. 6. Der Verlauf der Konzentrationsabhängigkeit der Umwandlungstemperaturen und-enthalpien der 3 binären Systeme läßt den Schluß zu, daß die Lecithinkopfgruppe stufenweise hydratisiert wird. Der Aufbau der 1. Hydrathülle ist bei ungefähr 5–6 Molekülen Wasser pro Molekül Lecithin abgeschlossen und die 2. Hydrathülle bei etwa 13 Molekülen Wasser pro Molekül Lecithin abgeschlossen
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Colloid & polymer science 261 (1983), S. 329-334 
    ISSN: 1435-1536
    Keywords: Differential-scanning-calorimetry ; 1,2-di-palmitoyl-phosphatidyl-choline/water-mixtures ; phase transitions ; phase diagram
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Description / Table of Contents: Abstract 1. By means of the differential scanning calorimetry technique the phase diagram of 1,2-dipalmitoyl-lecithin/water was determined. The own results are discussed on a pure thermodynamical point of view together with the literature data. The contradictions which are obvious from the existence of different phase regions in the literature are considered. 2. The thermodynamical parameters of the pre-transitions as a function of the lecithin chain length was analysed and compared. The kinetics of the pre-transition was investigated.
    Notes: Zusammenfassung 1. Auf der Grundlage kalorimetrischer Messungen wurden die Phasengebiete des Zustandsdiagrammes 1,2-Dipalmitoyllecithin/Wasser exakt ermittelt und thermodynamisch widerspruchsfrei unter Berücksichtigung von Strukturuntersuchungen interpretiert. Die eigenen Ergebnisse werden Literaturdaten gegenübergestellt und diskutiert. 2. Die Analyse der Umwandlungsparameter der Vorumwandlung der untersuchten Lecithine Di-C14-PC, Di-C16-PC, Di-C18-PC und Di-C20-PC im wasserreichen Gebiet (heterogenes Zweiphasengebiet) führt zu einer eindeutigen Kettenlängenabhängigkeit. Untersuchungen zur Kinetik der Rückbildung derL β-Phase zeigen, daß die strukturellen Veränderungen, die mit der Vorumwandlung zusammenhängen, langsame Prozesse sind. 3. Untersuchungen zur Hydratation derL β- undx-Phase ergaben, daß bei 273 K (Eispeak-Auswertung) für alle untersuchten Lecithine ein Wert von 13–14 mol W/mol L gefunden wird. Mit Temperaturerhöhung erhöht sich die Hydratationszahl geringfügig.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Colloid & polymer science 261 (1983), S. 417-422 
    ISSN: 1435-1536
    Keywords: Differential-scanning-calorimetry ; homologous phospholipids ; influence of substituents ; phase transition temperatures ; phase transition enthalpies
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Description / Table of Contents: Abstract By means of the differential scanning calorimetry technique the phase transition temperatures (T u) and enthalpies (ΔH u ) of phospholipid/water systems were evaluated. The major reason of this investigations was the variation of the chemical structure of the phospholipids. The results show that the influence of the substituents, in both, the hydrophobic and hydrophilic parts of the phospholipids affects a systematical change in the phase transition parameters.
    Notes: Zusammenfassung 1. Unter Verwendung der Methodik der Differential-Scanning-Kalorimetrie wurden die UmwandlungstemperaturenT u und UmwandlungsenthalpienΔH u der thermischen Phasenumwandlung von Phospholipid-Wasser-Systemen unterschiedlicher chemischer Phospholipidstruktur, insbesondere von Ether- und Ketalphospholipiden sowie von Lecithinen mit unterschiedlicher Anzahl von Methylgruppen am N-Atom, untersucht; die Ergebnisse wurden verglichen. 2. Die Variation der Kettenlänge homologer Phospholipide (Lecithine, Kephaline, Etherlecithine, Ketallecithine) führt im wasserreichen heterogenen Zweiphasengebiet zu einem linearen Anstieg derΔH u Werte der Hauptumwandlung. DieT u -Werte steigen monoton an. Kettenverzweigungen im Säurerest der Lecithine bewirken eine Erniedrigung derT u undΔH u -Werte im Vergleich zu den unverzweigten Verbindungen. 3. Variation der Substituenten im hydrophoben Teil der Phospholipidmoleküle (Ester, Ether, Ketale) bei gleicher Länge der KW-Ketten führt ebenfalls zu regelmäßigen Veränderungen in den Umwandlungsparametern sowie zu Verschiebungen im Temperaturabstand zwischen Vor- und Hauptumwandlung. 4. Der Einfluß der Anzahl der Methylgruppen am N-Atom der Phosphatidylkopfgruppe zeigt sich insbesondere im Hydratisierungsvermögen der Phospholipide. Mit diesem sind zugleich systematische Verschiebungen der Parameter der Hauptumwandlung im wasserreichen heterogenen Zweiphasengebiet verbunden.
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