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  • Articles: DFG German National Licenses  (3)
  • 1980-1984  (3)
  • 1960-1964
  • theophylline  (2)
  • Tracer experiments  (1)
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Anatomy and embryology 169 (1984), S. 237-247 
    ISSN: 1432-0568
    Keywords: Vater-Pacini corpuscle ; Cat mesentery ; Freeze-fracture ; Tracer experiments
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Correlated thin-section, freeze-fracture and tracer examinations were used to examine the blood-nerve barrier of the Vater-Pacini corpuscles in cat mesentery. A laminar inner core and a multilayered outer core enfolded the terminal nerve fiber of the corpuscle. The lamellar cells of both cores were characterized by numerous vesicular membrane invaginations. Freeze-fracture images and tracer experiments employing lanthanum nitrate proved that these invaginations are static structures mediating in neither active pinocytosis nor the transcellular transport of metabolites. In both inner and outer cores, lamellar cells were connected to one another by tight junctions of either the zonula or the fascia type, that occurred between lamellar-cell processes within the lamella and between the cells of adjacent lamellae. Intravascularly applied lanthanum lay at the out-ermost regions of the corpuscles without entering their internal zones, apparently because lamellar-cell tight junctions hindered further penetration. The results of our investigations suggest strongly that the Vater-Pacini corpuscle lamellae enfolding the nerve terminal form an effective diffusion barrier against the permeation of tissue fluids, thus preserving the corpuscle internal circumference.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: theophylline ; smoking habit ; absolute bioavailability ; pharmacokinetics ; sustained release preparation ; plain tablet preparation ; antipyrine pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability and pharmacokinetics of theophylline from a plain uncoated and 2 newly designed, sustained-release tablet formulations, as compared to intravenous aminophylline, were studied in 12 healthy adult male volunteers. The subjects were divided into two groups (n=6) with respect to smoking habit and on 4 separate occasions each received, on a randomized cross-over basis, a single dose of 400 mg equivalent of theophylline from every dosage form. The intravenous aminophylline study showed that habitual smoking had a significant (p〈0.05) effect on plasma theophylline clearance (0.051±0.006 vs 0.035±0.004 l/kg/h). Smoking significantly reduced the raw AUC from the 4 dosage forms (p〈0.05), but did not change the characteristics of absorption of each formulation. There was a non-significant trend towards reduced absolute bioavailability of theophylline from sustained-release formulations in smokers (percentage mean difference — 16% for one formulation and 13% for another). The trend was not observed for the plain uncoated tablet, which was rapidly absorbed (p〈0.01 to 0.05 in Ka, tmax and Cmax compared to sustained-release tablets). Similarity of the in vitro dissolution profiles of the two sustained-release formulations did not imply similarity of the in vivo absorption characteristics. Plasma clearances of theophylline and antipyrine were significantly correlated (p〈0.05,r=0.693,n=10). Thus, smoking enhanced the elimination of theophylline regardless of the dosage form administered. However, the extent to which habitual smoking may affect the hepatic first-pass effect on theophylline from sustained-release formulations requires further study. The results also suggest that theophylline and antipyrine may share a similar or common and presumably polycyclic hydrocarbon-inducible form(s) of microsomal drugmetabolizing enzyme.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1041
    Keywords: theophylline ; smoking ; sustained release formulation ; dosage forms ; multidose pharmacokinetics ; bioavailability ; circadian variation in kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and bioavailability of theophylline following 10 days of multiple doses of a plain uncoated (640 mg, q.i.d.) and a sustained-release tablet formulation (600 mg, b.i.d.) were related to habitual smoking in 11 healthy adult male volunteers, who had previously taken part in a single-dose study of an intravenous preparation of theophylline and of the same oral dosage form. There were significant differences (p〈0.05 to 0.01) in the steady-state mean and minimum theophylline concentration and AUC between the groups (6 smokers versus 5 nonsmokers), but not between other variables. A difference (p〈0.05) in peak time was also found between the dosage forms. The mean elimination t1/2 was significantly (p〈0.05) shorter in smokers than in nonsmokers. The intersubject variability in plasma theophylline concentration observed on the final trial day in the smoking group was larger and diverged more from simulation curves generated from the mean pharmacokinetic parameters of the single-dose study of the same formulations as compared to that of the nonsmoking group. There was no significant difference between the two groups in the mean accumulation ratio and absolute bioavailability of the two dosage forms. The mean morning (7 a.m.) trough theophylline concentrations after both formulations were significantly (p〈0.05 to 0.01) greater than the evening (7 p.m.) values within the same group. The average number of reported side-effects was significantly (p〈0.001) greater during the earlier period (Days 1 to 3) than the later period of the trial. A trend was observed suggesting that the incidence of side-effects was less in smokers than in nonsmokers. The results indicate that smoking is a determinant not only of enhanced elimination of theophylline but that it also produces more variability in the plasma level, irrespective of the dosage form administered or the dosing scheme employed. There may be circadian variation in theophylline kinetics.
    Type of Medium: Electronic Resource
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