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  • bioavailability
  • Springer  (8)
  • Periodicals Archive Online (PAO)
  • 1990-1994  (8)
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  • Springer  (8)
  • Periodicals Archive Online (PAO)
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  • 1
    ISSN: 1432-1041
    Keywords: Methylprednisolone ; Rheumatoid arthritis ; bioavailability ; pharmacokinetics ; clinical response ; pulse steroid therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A commercially available 1.0 g intravenous (i.v.) dosage formulation of methylprednisolone, as the sodium hemisuccinate salt (Solu MedrolR, Upjohn) was administered both parenterally and orally (pulse steroid therapy) on separate occasions, to eight elderly (mean 65 y) patients with active rheumatoid arthritis. The relative oral bioavailability of the sterol was 69.2%. Elimination of methylprednisolone was prolonged when given orally; the mean residence times were 7.23 h and 3.94 h for oral and i.v. administrations, respectively. Clinical response to pulse steroid therapy was no different with respect to route of administration. There were no significant differences in standard clinical and laboratory assessments of disease activity when the two therapies were compared. Oral administration of methylprednisolone in patients requiring high-dose pulse steroid therapy is convenient and avoids the discomfort and inconvenience associated with i.v. administration.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: Glyceryl trinitrate spray ; pharmacokinetics ; a/b-ratio ; pulmonary artery diastolic pressure ; finger pulse curve ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The time course and the magnitude of the effect of glyceryl trinitrate (GTN) on central venous (pulmonary artery diastolic pressure-PAPd) and peripheral arterial (a/b-ratio of the finger pulse wave) haemodynamics were compared in a randomized double-blind cross-over study in 12 patients suffering from congestive heart failure (NYHA II–III) with elevated PADd at rest (≥15 mm Hg). The data were obtained in a bioavailability study of two sprays of glyceryl trinitrate, which differed in their galenical characteristics and in the dose of GTN (0.4 mg vs. 0.8 mg). Following sublingual administration of each spray, PAPd, a/b-ratio and the plasma concentrations of GTN and its metabolites were measured up to 30 min. The relative bioavailability of GTN of the test preparation was estimated to be 157%, 161% and 147%, when calculated from the plasma concentration-time data or the integrated effect of GTN on a/b-ratio or PAPd, respectively. The mean time courses of the decrease in PAPd and the increase in the a/b-ratio of the finger pulse curve were mirror images. Thus, there was a strong correlation between the mean values of PAPd and a/b-ratio following the administration of glyceryl trinitrate. Since the slope of the relationship differed considerably between the patients, the magnitude of effect of GTN on PAPd in the individual patient could not be predicted from the changes in a/b-ratio.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 46 (1994), S. 333-337 
    ISSN: 1432-1041
    Keywords: Erythropoietin ; recombinant human erthropoietin ; pharmacokinetics ; subcutaneous ; absorption ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics of recombinant human erythropoietin (RhEPO) were investigated after subcutaneous (s.c.) injection in the thigh and in the abdominal wall. Eleven healthy subjects, age 24.4 years (median), were studied. Each subject received two s.c. injections of 100 U·kg-1 RhEPO dissolved in 1 ml water: one injection in the thigh and another in the abdomen. Serum erythropoietin was measured regularly by radioimmunoassay until 144 h after each injection. The mean residence time was significantly longer after injection in the thigh than in the abdomen (32.7 vs 26.2 h). The estimated half-life of absorption was significantly longer after injection in the thigh than after abdominal application (14.9 vs 12.3 h). The estimated half-life of elimination was not significantly different (4.4 vs 4.8 h). The relative difference in the area under the curve between injection in the abdomen and the thigh in the same subject ranged from -36% to +68% but there was no significant difference in bioavailability. The peak concentration was not significantly different and appeared at around 10 h (Cmax thigh, 175 U·l-1 vs Cmax abdomen, 216 U·l-1). A twin-peak configuration of the concentration vs time curve with a significant second peak at 24 h was found after injection in the thigh but not after abdominal injection. In conclusion, the mean residence time was longer after administration in the thigh, probably due to delayed absorption, but bioavailability was not significantly different. Following injection in the thigh the concentration curve had two peaks. The differences may be due to regional variations in lymph flow and to physical activity. The overall differences in pharmacokinetics appeared to be too small to recommend a general preference of the injection site.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-904X
    Keywords: procaterol ; bronchodilator ; healthy volunteers ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics and relative oral bioavailability of procaterol, an orally active β2-adrenergic agonist bronchodilator were evaluated in healthy volunteers. Procaterol was rapidly absorbed after oral administration. Mean plasma procaterol concentration–time profiles and pharmacokinetic parameters for both formulations were essentially superimposable. Following tablet administration, the mean C max was 358 pg/mL and the corresponding mean t max was 1.6 hr. Mean renal clearance was 163 mL/min and accounted for approximately one-sixth of the mean apparent oral plasma clearance (988 mL/min). The mean apparent elimination half-life of procaterol was 4.2 hr. Hepatic metabolism appears to be the primary mechanism for elimination of procaterol from the body, and first-pass metabolism may limit systemic bioavailability.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1573-5117
    Keywords: acid volatile sulfide ; metal ; bioavailability ; sediment ; freshwater ; temperature ; seasonal
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Acid volatile sulfide (AVS) is a natural agent in sediments which complexes some cationic metals and thereby influences the toxicity of these metals to benthic organisms. Because of its influence on metal bioavailability, AVS has been proposed as a key normalization phase for the development of sediment quality criteria for metals. However, studies conducted primarily in marine and estuarine systems have shown that AVS concentrations can vary markedly both temporally and with (sediment) depth. In this study, AVS concentrations were measured monthly for 16 mo in several segments of sediment cores from three freshwater lakes: Caribou Lake, Fish Lake and Pike Lake in northeastern Minnesota, USA. The concentrations of AVS in cores from the three lakes varied inversely with sediment depth. AVS concentrations also varied seasonally by as much as two orders of magnitude and were directly correlated with changes in water temperature. The correlation between AVS and temperature likely was related both to changes in primary productivity and sediment microbial activity.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1573-5117
    Keywords: heavy metals ; bioavailability ; coastal lagoons ; sediments ; macrophytes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The distribution and bioavailability of trace metals in two contrasting tropical coastal lagoons were studied. The concentration of trace metals in aquatic macrophytes was compared with those found in sediments under weakly and strongly bound forms. The results showed that total metal concentrations in sediments did not explain the concentration found in plants. The highest concentrations in macrophytes were observed in the lagoon which had a higher fraction of metals weakly bound to sediments, but presented the lower total metal content. Low redox potential was the major variable keeping metals in non-bioavailable forms, possibly as refractory sulfides and metal-organic complexes. Among the macrophytes, rooted species showed lower concentrations of metals as compared to algae.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 10 (1993), S. 1083-1086 
    ISSN: 1573-904X
    Keywords: kappa agonist analgesic ; nasal absorption ; bioavailability ; pharmacokinetics ; ED50.
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1573-904X
    Keywords: ibuprofen enantiomers ; pharmacokinetics ; bioinversion ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract An open, randomized, six-way crossover study was conducted in 12 healthy males to assess pharmacokinetics and bioinversion of ibuprofen enantiomers. The mean plasma terminal half-life (t1/2) of R(–)ibuprofen was 1.74 hr when intravenously infused as a racemic mixture and was 1.84 hr when intravenously infused alone. The mean t1/2 of S( + )ibuprofen was 1.77 hr when dosed as S( + )ibuprofen. Examination of values of both the absorption and disposition parameters of R(–)ibuprofen revealed that the kinetics of R(–)ibuprofen were not altered by concurrent administration of S( + )ibuprofen. In this study, there was little or no presystemic inversion of R(–)ibuprofen to its S( + )isomer. Also, 69% of the intravenous dose of R(–)ibuprofen was systemically inverted and 57.6% of the oral dose of R(–)ibuprofen lysinate was bioavailable as S ( + )ibuprofen. These results indicate that the bioinversion of R(–)ibuprofen administered orally is mainly systemic. Because bioinversion of R(–)ibuprofen is not complete, S( + )ibuprofen produced higher bioavailability of S( + )ibuprofen (92.0%) than either racemic ibuprofen (70.7%) or R(–)ibuprofen (57.6%). However, bioavailability of R(–)ibuprofen (83.6%) when dosed alone was not significantly different from when dosed as racemic mixture (80.7%).
    Type of Medium: Electronic Resource
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