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  • 42.55  (16)
  • bioavailability  (15)
  • Springer  (31)
  • National Academy of Sciences
  • 1975-1979  (31)
  • 1977  (31)
Collection
Publisher
  • Springer  (31)
  • National Academy of Sciences
Years
  • 1975-1979  (31)
Year
  • 1
    ISSN: 1432-0630
    Keywords: 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Lasing in atomic lines of noble gases and fluorine, prior to excimer radiation, was observed in an electric discharge ArF/XeF excimer laser. Some Ar/Xe lines end at metastable levels, which are very important for the formation of ArF/XeF excimer molecules. Five new lasing lines of atomic fluorine have been obtained. Consideration is given to the use of lasing in atomic and molecular lines, that occurs in one burst, in investigations of the excitation kinetics of excimer states under the conditions of a high-pressure electric discharge.
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  • 2
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    Applied physics 14 (1977), S. 277-282 
    ISSN: 1432-0630
    Keywords: 42.55 ; 52
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract The paper deals with the properties andI-V characteristics of discharges in narrow capillaries used, for example, for He−Ne waveguide lasers. It has been observed that discharges in He−Ne waveguide lasers are unstable because of the strongly falling characteristic. A theory is presented which assumes that at low currents wall charges restrict the positive column to a narrow plasma channel and are the main reason for the observed falling characteristic. A numerical evaluation for helium gives results which agree well with experimental data.
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  • 3
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    Applied physics 13 (1977), S. 97-99 
    ISSN: 1432-0630
    Keywords: 42.55 ; 82.50
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract First cw laser oscillation with thresholds below 1 mW was observed for various B1Пu → X1 ∑ g + transitions of diatomic molecular sodium excited by different argon laser lines in the range of 454–488 nm. For pump powers of 0.5 W output powers up to 3 mW and single-pass gain up to 0.1 cm−1 were obtained. Some properties of the heat pipe laser system are discussed.
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  • 4
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    Applied physics 13 (1977), S. 383-385 
    ISSN: 1432-0630
    Keywords: 42.55 ; 42.80
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract An optically pumped FIR laser was operated with a copper mesh Fabr-Perot output coupler. With this device a Gaussian output beam was obtained andthe degree of coupling could be varied continuously, thus allowing optimum coupling. From the measured properties of the wire mesches grains of two FIR laser lines are calculated and the saturation intensities estimated.
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  • 5
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    Applied physics 14 (1977), S. 25-28 
    ISSN: 1432-0630
    Keywords: 42.55 ; 42.80
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract A new device for magnetically displacing the output mirror of a laser resonator and synchronously tilting an etalon in order to obtain single-mode tuning of a dye laser over a tuning range of at least 10 GHz is described. Comparatively large displacements with good linearity of a coil mounted on a membrane and placed inside the strong magnetic field of a ring magnet are obtained for currents in the order of several hundred milliamperes. Together with etalon flats of appropriate thickness and reflection mounted in the resonator of the laser a versatile instrument for application in intra and extra cavity spectroscopy has been developed.
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  • 6
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    Applied physics 14 (1977), S. 393-398 
    ISSN: 1432-0630
    Keywords: 34 ; 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract A flowing afterglow method has been used to study a number of reactions of importance in KrF lasers using NF3 as the fluorine donor. Total rate constants are reported for Kr*(3 P 2)+NF3 and Kr++NF3. The thermal energy attachment coefficient has been measured for NF3 and the cross section for the electron excitation process Kr*(3 P 2) +e→Kr*(3 P 1)+e has been estimated. The relevance of these results to discharge pumped KrF lasers is discussed.
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  • 7
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    Applied physics 14 (1977), S. 193-197 
    ISSN: 1432-0630
    Keywords: 42.55 ; 52
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Planar and cylindrical discharges for argon lasers are compared by plasmatheoretical calculations. The maximum laser output power available in the two arrangements is computed in dependence of various parameters neglecting saturation mechanisms. A transverse discharge arrangement confining the positive column by two parallel walls is described and experimental laser threshold values for the current and pressure are reported.
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  • 8
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    Applied physics 14 (1977), S. 255-268 
    ISSN: 1432-0630
    Keywords: 42.80 ; 42.55 ; 85.60
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract GaAs double heterostructure semiconductor injection lasers which now exhibit more than 25000 h cw room temperature lifetime are of great interest for future use as directly modulated transmitters for high bit-rate fiber optical communications. The effects limiting this application are modulation distortions, spectral width and additional spectral broadening in the case of modulation and spontaneous fluctuations of the output power. The dynamic and spectral behavior of injection lasers, the methods of high bit-rate modulation and the improvement of the high bit-rate modulation capability by coupling two lasers are discussed.
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  • 9
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    Applied physics 13 (1977), S. 109-110 
    ISSN: 1432-0630
    Keywords: 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract A simple technique is described that allows the generation of a short pulses (1 ns) from dye lasers pumped by a much longer (7 ns) N2-laser pulse. Dye-laser pulses, either with a narrow bandwidth or a short duration, can thus be obtained with the same N2-laser pump.
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  • 10
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    Applied physics 14 (1977), S. 121-122 
    ISSN: 1432-0630
    Keywords: 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Frequency-tunable generation by means of F 2 + and F 2 − colour centers in a LiF crystal is reported. Colour centers were created by illuminating LiF crystals with electrons of 3 meV energy at the electron current density of 1 μA/cm2. The pumping source was a ruby laser with a peak power of 20 MW, a pulse duration of 20 ns, and a repetition rate of 1 Hz. The frequency tuning is obtained in the range of 0.88–1.25 μm. Discussed are the ways of pumping of colour centers and the possibility of lasing in the spectral region of 0.85 to 2 μm in the type of colour centers under investigation.
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  • 11
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    Applied physics 13 (1977), S. 107-108 
    ISSN: 1432-0630
    Keywords: 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Intense laser oscillation has been observed from ArF molecules at 1933 Å. Excitation of the gas mixture NF3:Ar:He=1:55:630 at total pressures above 2.1 atm was produced by a transverse electric discharge. The range of fine tuning was from 1927 Å to 1936 Å. An output energy of 0.8 mJ was measured from a laser pulse 15 ns in duration.
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  • 12
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    Applied physics 13 (1977), S. 1-3 
    ISSN: 1432-0630
    Keywords: 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Disappearance of NF3 and appearance of NF2 and N2F2 in an excimer laser is followed quantitatively with a mass spectrometer. A model for the kinetics is presented.
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  • 13
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    Applied physics 13 (1977), S. 55-58 
    ISSN: 1432-0630
    Keywords: 42.55 ; 78.60
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract NdxLa1−xP5O14 (0.25≦x≦1) single crystals, placed within a confocal optical resonator, were pumped with ruby laser fundamental and second-harmonic nanosecond pulses. In both cases laser oscillations at 1.05 μm exceeding in duration many times the pumping pulse were obtained.
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  • 14
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    Applied physics 14 (1977), S. 343-350 
    ISSN: 1432-0630
    Keywords: 33 ; 42.55
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract By means of nonlinear absorption spectroscopy data necessary for the interpretation of molecular spectra can be obtained in such spectral regions, where conventional spectroscopic methods yield only a quasi-continuous absorption curve. Using a Zeeman-tuned He−Ne laser at the wavelength of 3.39μm we have measured significant differences in the intensity and temperature behaviour for several ethane absorption lines, the analysis of which made possible a preliminary qualitative assignment of these lines.
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  • 15
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    Applied physics 14 (1977), S. 377-380 
    ISSN: 1432-0630
    Keywords: 42.55 ; 42.65
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Due to spatial hole burning, standing-wave dye lasers require a large amount of selectivity inside the cavity for single-mode operation. The output power of these lasers is limited by losses caused by the frequency selecting elements. In a travelling-wave laser, on the other hand, spatial hole burning does not exist, thereby eliminating the need for high selectivity. A travelling-wave cw dye laser was realized by unidirectional operation of a ring laser, yielding single mode output powers of 1.2 W at 595 nm and of 55 mW in the UV-region with intracavity frequency doubling.
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  • 16
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    Applied physics 14 (1977), S. 199-203 
    ISSN: 1432-0630
    Keywords: 42.55 ; 82.50
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics , Physics
    Notes: Abstract Loss of gain in a dye medium as a result of decomposition by pump photons is considered in terms of disappearance of dye molecules and the appearance of a new, single chemical product having absorption in the fluorescence band. The cases of small signal gain and saturated gain are applied to a single pass through a transversely excited amplifier. Loss of output, defined as “quantum yield of laser deterioration”,Q L , is related to the true quantum yield of molecular destruction of the dye,Q M , and other known parameters. For the experimentally common, saturated gain condition, the smallestQ L can be isQ M , which requires a photochemically bleachable dye with high gain, preferably at high concentration, in a long cavity, operating at high injection and pumping fluxes. Reversing these conditions, the highest valueQ L can be, compared withQ M , is unrestricted.
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  • 17
    ISSN: 1432-1041
    Keywords: Cefoxitin ; lidocaine ; intramuscular ; bioavailability ; pain
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The use of lidocaine HCl solution at concentrations of 0.5 and 1.0% to reconstitute sodium cefoxitin relieves the pain associated with intramuscular injections of the antibiotic. Cefoxitin absorption by the intramuscular route is initially rapid and is virtually complete. Peak serum concentrations, corresponding to about one-half those of a comparable intravenous infusion, are achieved in 30 min. Continuing absorption tends to maintain higher serum concentrations for longer times. Renal clearance and serum half-life of cefoxitin do not appear to be affected by lidocaine at its effective anaesthetic concentrations.
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  • 18
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    European journal of clinical pharmacology 12 (1977), S. 69-72 
    ISSN: 1432-1041
    Keywords: Metronidazole ; serum concentration ; bioavailability ; food intake ; healthy subjects ; Crohn's disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The possible influence of food intake on the bioavailability of metronidazole was examined in ten healthy volunteers by administration of a single dose of metronidazole on an empty stomach, and with a standardized breakfast. Food intake did not significantly alter the bioavailability of metronidazole. The interindividual variation in bioavailability appeared to be slight. In nine patients with Crohn's disease, the absorption of metronidazole appeared to be reduced and to be more variable than in healthy subjects. In both groups there was a clear relationship between the amount absorbed and dose/kg body weight. Thus, from the pharmacokinetic point of view, metronidazole can safely be given either with or between meals. The dose should be related to body weight.
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  • 19
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    European journal of clinical pharmacology 12 (1977), S. 285-290 
    ISSN: 1432-1041
    Keywords: Phenytoin acid ; phenytoin calcium ; bioavailability ; inequivalence of generics ; normal subjects ; volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Serum phenytoin concentrations have been studied in epileptic patients and healthy subjects taking tablets of phenytoin calcium (Desitin), A, phenytoin acid (Desitin), B, and phenytoin acid (Nordmark), C. Retrospective data and prospective investigation of hospitalized patients on long-term phenytoin treatment showed that significantly higher serum concentrations of phenytoin were produced by the phenytoin acid preparations B and C than by the phenytoin calcium preparation A. In a cross over study six volunteers received 200 mg/day of preparations A, B, and C for three weeks. In this study, too, higher phenytoin serum concentrations were produced by B and C than by A, although the differences were not statistically significant. The reasons for the discrepancies between the studies in healthy and epileptic subjects are discussed.
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  • 20
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    European journal of clinical pharmacology 12 (1977), S. 383-386 
    ISSN: 1432-1041
    Keywords: Benzodiazepine ; temazepam ; pharmacokinetics ; bioavailability ; hard and soft gelatine capsules
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels of temazepam were determined in healthy subjects after single oral administration of soft and hard gelatin capsules, and after 7 consecutive night-time doses in soft capsules. Absorption from soft gelatin capsules was significantly faster and produced earlier and higher peak plasma levels. The two pharmaceutical forms did not show any significant difference in relative availability. The apparent half-life of temazepam after night-time administration was significantly shorter than after morning administration, but no change in half-life was observed between the first and seventh night-time doses.
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  • 21
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    European journal of clinical pharmacology 11 (1977), S. 277-281 
    ISSN: 1432-1041
    Keywords: Proscillaridin ; oral administration ; portal venous sample ; porto-peripheral concentration difference ; bioavailability ; 86Rb-uptake inhibition assay
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption of proscillaridin A was studied in four patients undergoing catheterization of the portal vein for diagnostic purposes. Proscillaridin 1.5 mg was given as a single oral dose and plasma glycoside activity was analyzed by the86Rb-uptake inhibition technique. Proscillaridin appeared rapidly in the portal blood, peak activity being found after 15 min in three and after 30 min in one patient. In peripheral blood the peak activity occurred after approximately 35 min. Despite rapid passage across the gut wall, porto-peripheral differences in glycoside activity were small; they were zero after 4 h. The mean amount absorbed as active proscillaridin during the first 4 h after the dose was calculated to be only 7.1% of the given amount. Late porto-peripheral differences, probably due to enterohepatic recycling, appeared after 6 h in three patients. The results suggest that proscillaridin undergoes first pass inactivation in the gut wall. Enterohepatic recirculation may contribute to the amounts of active glycoside that reach the systemic circulation.
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  • 22
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    European journal of clinical pharmacology 11 (1977), S. 207-212 
    ISSN: 1432-1041
    Keywords: Chlorpropamide ; hypoglycaemic agent ; bioavailability ; plasma concentrations ; bioequivalence ; dissolution tests
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of chlorpropamide from two new formulations (Melitase® tablets) has been compared to that from a reference formulation which is currently in clinical use as a hypoglycaemic agent. In both rate and extent of bioavailability, all three formulations may be considered equivalent, providing allowances are made for differences in drug content. With 95% confidence, the mean bioavailability of chlorpropamide from the new formulations was within about 16% of the mean from the reference formulation, and formulation-related differences were not statistically significant. Although all three formulations were shown to have similar dissolution profiles, dissolution of chlorpropamide was pH-dependent in vitro. Dissolution was almost complete during 30 min at pH 7.2, but only 40%–60% had dissolved during 90 min at pH 2.0. A peak mean concentration of 22.7 µg/ml was reached 3 h after administration of 2×100 mg tablets of the new formulation and peak mean concentrations of 26.8 µg/ml and 27.4 µg/ml were reached 3 h and 4 hours after administration of one 250 mg tablet of the new formulation and one 250 mg tablet of the reference formulation respectively. Formulation-related differences of mean plasma concentrations (after scaling for equal doses of 250 mg) were not significant and each formulation provided similar plasma concentrations at corresponding times after administration. Statistically significant subject-related differences in all the parameters of bioavailability were shown by analyses of variance.
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  • 23
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    European journal of clinical pharmacology 11 (1977), S. 219-224 
    ISSN: 1432-1041
    Keywords: Nortriptyline ; 10-OH-nortriptyline ; bioavailability ; plasma metabolites ; first pass metabolism ; oral dose ; intramuscular dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Nortriptyline was given orally and intramuscularly to six depressed patients. Plasma concentrations of parent drug and the unconjugated and conjugated principal metabolite, 10-hydroxynortriptyline, were determined by mass fragmentography. There was a significant decrease in the area under the nortriptyline plasma concentration — time curve after the oral route of administration, whilst the elimination rate was unchanged. With the oral dose, plasma concentrations of the metabolites were higher and peaked earlier than after intramuscular administration, whilst the opposite was true for the parent compound. This proves that the difference in bioavailability between the two routes of administration was due to first pass metabolism. As determined from the ratio between corresponding areas, the relative bioavailability of the oral dose was 66±21 S.D. per cent. This fraction is higher than that reported previously when intravenous nortriptyline was used as the reference dosage form.
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  • 24
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    European journal of clinical pharmacology 12 (1977), S. 281-284 
    ISSN: 1432-1041
    Keywords: Tetracycline ; bioavailability ; plasma levels ; nutritional state ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Relative bioavailability after oral administration of a single dose and Cmin levels of tetracycline in plasma after multiple doses were determined in groups of well-nourished and undernourished subjects. The relative bioavailability of tetracycline, assessed by the area under serum concentration time-curves, did not differ in undernourished and well-nourished patients. The plasma levels were not different in the two groups after the conventional dose of tetracycline HCl 250 mg at 6 hour intervals. However, in these studies undernourished subjects received a higher dose per kg body weight, which could have compensated for any effect of a shortened half life of the drug. When the dose per kg body weight was reduced, the Cmin levels were lower. On the other hand, with the same dose per kg body weight at more frequent intervals, the plasma concentrations were similar to those in well-nourished subjects. These studies indicate that the dosage regimen should be based both on body weight and on the nutritional status of the individual.
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  • 25
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    European journal of clinical pharmacology 12 (1977), S. 65-68 
    ISSN: 1432-1041
    Keywords: Indomethacin ; antacids ; drug-drug interactions ; bioavailability ; drug combinations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The biovailability of indomethacin from two indomethacin-antacid (aluminum hydroxide magnesium carbonate and magnesium hydroxide) combinations was compared with the bioavailability of oral indomethacin. Relative bioavailability was estimated by three methods: comparison of plasma concentrations at various times, comparison of areas under plasma concentration time curves, and comparison of the amount of drug excreted unchanged in the urine. A double blind three-way crossover study was conducted in twelve healthy volunteers. The combination with the slightly smaller amount of antacid (preparation A) showed significantly decreased bioavailability by all three methods in comparison with indomethacin alone (preparation C). The combination with the larger amount of antacid (preparation B) was also less bioavailable than preparation C. This effect was significant only for the comparison of areas under curves and not for plasma levels, although the mean plasma levels produced by preparation B at all times were lower than those for preparation C. These findings suggest that aluminum hydroxide magnesium carbonate and magnesium hydroxide decrease the bioavailability of indomethacin.
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  • 26
    ISSN: 1432-1041
    Keywords: Tolmetin ; pharmacokinetics ; bioavailability ; antacid ; oral dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of this study was to determine whether a concomitant single dose of antacid or multiple doses of antacid administered prior to, and with tolmetin, alter the pharmacokinetics of tolmetin when the drug was administered as a commercially available tablet containing tolmetin sodium. The possible effects of the antacid on plasma concentrations and urinary excretion of tolmetin and its major metabolite were evaluated following administration of: (a) tolmetin sodium alone; (b) antacid four time a day for three days prior to a single dose of tolmetin sodium, with continuation of the antacid during the day tolmetin was given; and (c) co-administration of single doses of tolmetin sodium and antacid. The twenty-four subject study was of the crossover type. There were no significant differences among treatment means for: (i) peak plasma concentrations of both tolmetin and metabolite, (ii) AUC 0–8 h and AUC 0-∞ for both tolmetin and metabolite, (iii) time to peak plasma concentration for both tolmetin and metabolite, (iv) plasma concentrations of both tolmetin and the metabolite at all sampling times (except for tolmetin at 2 h), (v) renal clearance of both tolmetin and its metabolite, and (vi) the amount of metabolite excreted in the 0–24 h urine. There were small, but significant, differences among amounts of tolmetin excreted in the 0–24 h urine. Semilogarithmic plots of both tolmetin and metabolite plasma concentrations past the peak concentrations were curved over the entire 8-h observation period; although the elimination half-life of tolmetin has been reported to be about one hour, the half-life most probably exceeds 2.6 h in most subjects. The results of this study indicate a lack of a significant drug-drug interaction between the non-steroidal anti-inflammatory agent, tolmetin sodium, and a commonly used antacid, which is a mixture of magnesium and aluminium hydroxides.
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  • 27
    ISSN: 1432-1041
    Keywords: Coumarin ; 7-Hydroxycoumarin ; drug disposition ; first-pass effect ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of coumarin (C) upon i.v. and p.o. administration and its metabolites 7-hydroxy-coumarin (7-HC) and 7-hydroxy-coumarin glucuronide (7-HCG) have been studied. Six healthy volunteers were involved in this investigation. Four of the volunteers participated in a crossover study. Coumarin was administered i.v. and p.o. in dose sizes of 0.25 mg/kg and 0.857 mg/kg, respectively. Coumarin is rapidly absorbed p.o., however the availability to systemic circulation is less than 4%. The rest of the dose appears quantitatively as 7-HC and 7-HCG in systemic circulation suggesting an extensive firstpass effect. Coumarin and 7-HCG are best fitted to an open two-compartment model, whereas 7-HC is best fitted to an open one-compartment model. The biological half-life of both C (0.80 vs. 1.02 h) and 7-HCG (1.47 vs. 1.15 h) was not significantly different for the two routes of administration. The large total clearance of C again suggests a first-pass effect; while that of 7-HCG, which is nearly exclusively eliminated into urine, indicates active tubular secretion of the glucuronide.
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  • 28
    ISSN: 1573-8744
    Keywords: accelerated convergence method to estimate AUC0-∞ and A e ∞ ; bioavailability ; estimation of total areas ; estimation of total amounts excreted ; blood sampling schemes for digoxin ; elimination half-life of digoxin ; intra- and interindividual variation of renal clearance of digoxin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Five methods are compared to estimate the total area under the digoxin plasma or serum concentrationtime curve (AUC0-∞) after a single dose of drug. To obtain accurate estimates of AUC0-∞, data required are concentrations at a sufficient number of sampling times to define adequately the concentration-time curve prior to the log-linear phase, and at least three, but preferably four or more equally spaced points in the terminal loglinear phase. One method (designated Method I) requires a digital computer; another (Method III) is the classical method (these two methods do not require equally spaced points in the loglinear phase). Method IIA is the accelerated convergence method of Amidon et al.; Methods IIB and IIC are modifications of this method, but incorporate usual and orthogonal least squares, respectively, which make them more accurate with real (noisy) data. Methods I and IICgave very comparable estimates of AUC0-∞. Results indicate that digoxin administered orally in aqueous solution was completely (100%) absorbed when bioavailability estimates were based on oral and intravenous AUC0-∞ estimates and the actual doses, whereas formerly only about 80% absorption was reported, based on areas, under plasma concentration curves which were truncated at 96 hr. It is shown that the sampling scheme of blood can produce biased apparent bioavailability estimates when areas under truncated curves are employed, but an appropriate sampling scheme and application of method IIyield accurate bioavailability estimates. This is important particularly in those bioavailability studies where one is attempting to determine the appropriate label dose for a new “fastrelease” digoxin preparation relative to the label dose and bioavailability of currently marketed tablets. It is shown that the magnitudes and variability of apparent elimination rate constants and halflives of digoxin, estimated from urinary excretion data by the σ− method, depend on which value of A e ∞ is used. The formerly reported greater interindividual variability of AUC data compared to At data for digoxin is explained in that the AUCs, but not the Ae,'s, involve the renal clearance, which exhibits considerable inter- and intraindividual variation.
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  • 29
    ISSN: 1573-8744
    Keywords: aspirin ; dissolution ; bioavailability ; effect of antacids ; acid ; capacity ; consuming ; in vivo ; buffering effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The in vitrodissolution profile, in vitroand in vivobuffering characteristics, and single-dose bioavailability of various buffered aspirin tablet formulations were studied. Buffering agents,such as magnesium and aluminum hydroxides (formulations B and C) or magnesium carbonate and aluminum glycinate (formulation D), significantly increased the rate of aspirin dissolution from solid dosage forms as compared to an unbuffered tablet (formulation A). The extent of aspirin absorption was equivalent with all formulations;however, the faster rate of dissolution (t50 and t90)with buffered formulations resulted in earlier and higher peak concentration of salicylate compared to that with unbuffered formulation, following a two-tablet dose in the fasting state. A comparison of the in vivobuffer capacity of a four-tablet dose of formulations B and D was performed in the postcibal state at the time of maximal meal-induced acid secretion, using a radiotelemetry procedure for determination of pH. Formulation B prolonged the interval of elevation of intragastric pH 〉 3 for 32 min as compared to 12 min for D.
    Type of Medium: Electronic Resource
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  • 30
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 133-146 
    ISSN: 1573-8744
    Keywords: bioavailability ; phenytoin sodium capsules ; plasma levels ; human studies
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Eleven single lots of 100-mg phenytoin sodium capsules were evaluated for their relative bioavailability in 12 normal human volunteers. These products were manufactured by eight different companies and met all compendial specifications. The products were evaluated with respect to plasma levels at various times up to 96 hr following administration of single 100-mg doses, times of peak level, peak plasma concentrations, and areas under the plasma level—time curve. Several of the products exhibited statistically significant differences in the various parameters studied.
    Type of Medium: Electronic Resource
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  • 31
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 5 (1977), S. 183-192 
    ISSN: 1573-8744
    Keywords: propranolol ; kinetics ; volunteers ; bioavailability ; threshold dose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of propranolol in blood was studied in healthy volunteers, following intravenous administration of 0.1 mg/kg and increasing oral doses of 10,20, and 40 mg, using a specific and sensitive gas Chromatographie method. The systemic availability of orally administered propranolol varied from 9% to 38% between subjects, but it was constant within each subject. A linear relationship was found between the area under the blood concentration-time curve and the oral dose. At variance with literature data, we could not observe a threshold dose.
    Type of Medium: Electronic Resource
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