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  • bioavailability
  • Springer  (16)
  • American Chemical Society
  • 2005-2009
  • 1985-1989  (16)
  • 1980-1984
  • 1985  (16)
Collection
Keywords
Publisher
  • Springer  (16)
  • American Chemical Society
Years
  • 2005-2009
  • 1985-1989  (16)
  • 1980-1984
Year
  • 1
    Electronic Resource
    Electronic Resource
    Bioavailability and diuretic effect of furosemide during long-term treatment of chronic respiratory failure (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 53-59 
    Details
    ISSN: 1432-1041
    Keywords: furosemide ; respiratory failure ; furosemide glucuronide ; first-pass metabolism ; diuretic effect ; bioavailability ; food effect ; chronic treatment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability and diuretic effect of furosemide 40 mg administered orally for at least 6 months have been compared in patients with chronic respiratory failure and in healthy controls. The mean urinary recovery of unchanged drug was 11.5 mg and 9.41 mg in 24 h after pre- and postprandial administration to 10 patients, whereas the recovery was 14.4 mg in 10 healthy subjects. The diuretic effect, in terms of urine flow and sodium ion excretion in the 6 h after administration, was also less in patients than in healthy subjects. This was ascribed to the lower bioavailability of furosemide in patients, based on the urinary recovery of unchanged drug, and not to a lower level of response to furosemide than in healthy subjects. The mean absolute bioavailability of furosemide in 6 patients was 41.3% and 63.4%, respectively, calculated from unchanged drug and total drug (unchanged plus glucuronide conjugate). Approximately 53.9% of the dose of furosemide was excreted as the glucuronide conjugate after oral administration, and 34.2% after i.v. injection in the 6 patients. In 3 of the 6 patients studied, a distinct first-pass effect for glucuronidation of furosemide was observed after oral administration. In another study, the mean glucuronide fraction recovered in 24-h urine was 20.7% and 7.3% (p〈0.01) in 38 patients and 12 healthy subjects, respectively. The fraction in urine was not affected by changing the dose of furosemide from 20 to 120 mg. The lower bioavailability in patients as compared to healthy subjects is ascribed to enhanced glucuronidation and incomplete drug absorption.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635708
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  • 2
    Electronic Resource
    Electronic Resource
    Generalization of distribution – Free confidence intervals for bioavailability ratios (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 85-88 
    Details
    ISSN: 1432-1041
    Keywords: bioavailability ; distribution-free statistical method ; confidence limits
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The confidence interval approach to bioavailability assessment depends first on selection of the confidence level, usually 95%, and then determination of the confidence limits for the expected bioavailability ratio AUC(Test)/AUC(Reference). In practice, however, it is sometimes of greater interest to know the probability that the expected bioavailability will fall below a critical value, for example 0.75, or within a clinically set bioequivalence range, for example 0.80 to 1.25. Up to now, posterior probability distributions have been suggested, based on classical analysis of variance (ANOVA) with its rather restrictive assumptions, including that of a (logarithmic) normal distribution. In this report, a distribution-free confidence interval based on the Wilcox-on signed-rank statistic has been generalized so that confidence probabilities can be obtained for any given confidence limits. In the case of unimodal and almost symmetrical sampling distributions, the results obtained are very similar to those of the ANOVA-based posterior probability distribution. However, skewed or multimodal sampling distributions are better reflected by the proposed distribution-free method, and more valid information is obtained in these cases, as demonstrated by examples.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635713
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and metabolism of isosorbide-dinitrate after intravenous and oral administration (1985)
    Springer
    European journal of clinical pharmacology 27 (1985), S. 637-644 
    Details
    ISSN: 1432-1041
    Keywords: isosorbide-dinitrate ; pharmacokinetics ; analytical method ; bioavailability ; drug metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailabilities of a conventional and two slow release 20 mg isosorbide dinitrate (ISDN) formulations were compared after oral administration in a three way cross-over study in 8 male volunteers. In a further group of 6 male volunteers the pharmacokinetics and metabolism of ISDN were investigated after intravenous infusion of a median dose of 14.1 mg for 2.5 h. A new analytical procedure was developed for the determination of isosorbide-5-mononitrate-2-glucuronide (IS-5-MN-2-Glu) and of isosorbide (IS). Kinetic data analysis on a molar basis was performed by the program package KINPAK providing model independent parameters. The median elimination half-lives of ISDN, IS-5-MN, IS-2-MN and IS-5-MN-2-Glu were 0.7, 5.1, 3.2 and 2.5 h, respectively. The systemic clearance of ISDN was 3.7 l/min and the distribution volume 2521 (3.1 l/kg). Apart from IS-5-MN-2-Glu, with a renal clearance of 5.9 l/min which suggested substantial glucuronidation in the kidney, the renal clearances of ISDN, IS-5-MN, IS-2-MN and the corresponding amounts excreted were negligible. 27.8% of the administered ISDN was excreted as IS-5-MN-2-Glu (8.7%) and IS (19.1%). Calculations based on the two mononitrate metabolites formed from ISDN showed an incomplete recovery of 84.1%, leading to the assumption that a simultaneous denitration to IS must have occurred. The rate of denitration at each nitro group in ISDN was almost twice as high as for the same position in the corresponding mononitrate. The bioavailability of the conventional ISDN formulation was 19%, although complete absorption was indicated by comparison of the percentages of mononitrate metabolites formed after the different routes of administration. On the same basis the absorption of the two sustained release formulations was found to be poor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547041
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  • 4
    Electronic Resource
    Electronic Resource
    Human plasma and skin blister fluid levels of griseofulvin following a single oral dose (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 109-113 
    Details
    ISSN: 1432-1041
    Keywords: griseofulvin ; skin blister fluid levels ; pharmacokinetics ; healthy subjects ; bioavailability ; protein binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Griseofulvin and 6-demethylgriseofulvin (6-DMG) in plasma, suction blister fluid (SBF) and cantharides blister fluid (CBF) and urinary excretion of 6-DMG, were evaluated following administration of single oral doses of an ultramicrosize and a microsize formulation of griseofulvin to 6 healthy volunteers. The bioavailability of griseofulvin was higher following the ultramicrosize formulation when 64% of the dose was recovered (via metabolites) versus 52% after the microsize preparation. Penetration into skin blister fluid was delayed as compared to plasma levels; the peak concentration in plasma was observed at 3–4 h, whereas griseofulvin in CBF increased up to 6 h. The terminal half-live was calculated from plasma levels to 9.3 h. The half-lives calculated from SBF and CBF concentrations were 9.2 and 9.8 h, respectively, (n=5). In plasma 84% of griseofulvin was bound to proteins, predominantly to albumin; binding in SBF and CBF was 72 and 82%, respectively. 3 h after drug administration the free concentration in plasma significantly exceeded the free concentrations in SBF and CBF. Distribution equilibrium between plasma and skin blister fluid was observed after 27 h. Thus, during chronic administration, the plasma griseofulvin level should reflect its concentration in the target organ.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547378
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  • 5
    Electronic Resource
    Electronic Resource
    Absorption of glibenclamide from different sites of the gastro-intestinal tract (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 193-197 
    Details
    ISSN: 1432-1041
    Keywords: Glibenclamide ; intestinal absorption ; small and large intestine ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a study of eight volunteers and six patients, glibenclamide was placed at different sites of the gastro-intestinal tract under visual control. The dose was instilled once into the stomach and once into the duodenum of the eight volunteers in a randomized crossover design. The six patients underwent diagnostic colonoscopy, and the dose was placed into the ascending colon if pathological findings were not present. The area under the concentration-time curve, completed by extrapolation, and the mean residence time of the drug in the body were calculated. These pharmacokinetic characteristics were examined using a Jonckheere test for ordered alternatives and a Wilcoxon signed rank pair test. The means of the areas under the curve were 477±131 ng·h ml−1 for the stomach, 475±142 ng·h ml−1 for the duodenum and 486±301 ng·h ml−1 for the colon. The mean residence time changed from 2.67±0.35 h for the stomach to 2.42±0.48 h for the duodenum and 3.55±0.68 h for the colon. These results indicate that although glibenclamide is absorbed from all three sites of the gastro-intestinal tract to the same extent, the rates of absorption are different. It is discussed whether these findings really confirm the pH-partition hypothesis in drug absorption. Since glibenclamide — a weak acid — has a pK-value of about 6.5, these data seem to confirm the pH-partition hypothesis of drug absorption.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547421
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  • 6
    Electronic Resource
    Electronic Resource
    Effect of two antacids on the bioavailability of paracetamol (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 251-253 
    Details
    ISSN: 1432-1041
    Keywords: paracetamol ; antacids ; acetaminophen ; bioavailability ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of two antacids on the bioavailability of paracetamol has been investigated in 12 young healthy volunteers. Following a random cross over design, each subject swallowed, on three separate occasions, one weak apart, 500 mg paracetamol alone, or together with two different aluminium hydroxide, magnesium hydroxide preparations (Dimalan and Maalox). Plasma paracetamol levels were measured by HPLC. The bioavailability of paracetamol was not altered by either antacid, but they both delayed the time to peak plasma concentration (0.85 h; 1.43 h; 1.25 h, without antacid, with Dimalan and with Maalox respectively). The peak plasma concentration was not affected by concurrent antacid administration.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00547432
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  • 7
    Electronic Resource
    Electronic Resource
    Human plasma and skin blister fluid levels of griseofulvin after its repeated administration (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 351-354 
    Details
    ISSN: 1432-1041
    Keywords: griseofulvin ; skin blister fluid ; plasma concentration ; blister fluid concentration ; pharmacokinetics ; microsize formulation ; urinary excretion ; bioavailability ; different formulations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Griseofulvin was administered orally to 6 healthy volunteers for 6 days. The subjects received 500 mg of a microsize formulation and 330 mg of an ultramicrosize formulation, according to a cross-over design. The drug was determined in plasma, suction blister fluid (SBF) and cantharides blister fluid (CBF) following the last dose. Urinary excretion of the main metabolites 6-demethylgriseofulvin (6-DMG) and its glucuronic acid conjugate was also measured. The pharmacokinetic parameters were compared with those obtained from a recent single dose experiment. On repeated administration, the bioavailability of griseofulvin was significantly lower from the microsize formulation; the urinary recovery of total 6-DMG was 33.8% versus 53.6% on administration of the ultramicrosize material. Bioavailability was reduced as compared to ingestion of a single dose. The reduction was more prominent following the microsize (36%) than the ultramicrosize (17%) formulation. Penetration into skin blister fluid was not altered as compared to the single dose experiment. Relative areas under the blister fluid-time curves amounted to 51% (SBF) and 80% (CBF) of the area under the plasma level-time curve. The concentration of unbound griseofulvin in these body fluids was identical throughout the entire dosage interval. Unbound griseofulvin levels were low in comparison with the minimum inhibitory concentrations for strains of trichophyton and microsporum.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544093
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  • 8
    Electronic Resource
    Electronic Resource
    A non-parametric confidence interval method (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 379-381 
    Details
    ISSN: 1432-1041
    Keywords: confidence intervals ; bioavailability ; Bayesian analysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544099
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  • 9
    Electronic Resource
    Electronic Resource
    Bioavailability and pharmacokinetics of ketanserin in elderly subjects (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 411-417 
    Details
    ISSN: 1432-1041
    Keywords: ketanserin ; ketanserinol ; pharmacokinetics ; age ; healthy volunteers ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The bioavailability of ketanserin has been examined in a cross-over experiment in 21 elderly subjects (aged 59–72 years) by administration of tablets (40 mg), solution (40 mg) and injectable solution (10 mg). After two weeks of treatment with 40 mg ketanserin tablets further 18 blood samples for analysis were collected under steady-state conditions. Plasma levels were measured by HPLC. The absolute bioavailability of ketanserin tablets was 52.7%; their relative bioavailability compared to a solution containing an equal quantity of active compound was 85.5%. Therefore, the low absolute bioavailability of ketanserin cannot be attributed to the formulation. The active compound was rapidly liberated from the tablet, reaching a peak of 103.8 ng/ml after 0.97 h. Individual plasma level-time curves were fitted to an open three compartment model and a half-life of 17.7±7.26 h was calculated for the terminal elimination phase. An average terminal elimination half-life of 15.4±4.2 ng/ml was found after administration of the ketanserin solution. Multiple dosing with 40 mg tablets b.d.s. resulted in an AUC over one dosing interval at steady-state of 666±201 ng × h/ml. The AUC extrapolated to infinity was 1200±405 ng × h/ml for the last tablet. This is 1.8-times the AUC in one dosing interval, and 2.3-times the AUC of a single dose. Under steady-state conditions, the mean peak plasma level was 155.1 ng/ml (1.08 h after dosing) and the terminal half-life was 19.1±5.1 h. For the metabolite ketanserinol terminal half-lives of 21.4 h after a single tablet and 31.0 h after discontinuation of multiple dosing were calculated. Compared to the parent compound there was much more marked accumulation of ketanserinol. Despite moderate accumulation and prolongation of the terminal half-life of ketanserin under steady-state conditions, dosage adjustment is not required in elderly people. First-pass metabolism and bioavailability remained in the range found in previous studies of ketanserin in young subjects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544359
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  • 10
    Electronic Resource
    Electronic Resource
    Nasal bioavailability and systemic effects of the glucocorticoid budesonide in man (1985)
    Springer
    European journal of clinical pharmacology 29 (1985), S. 477-481 
    Details
    ISSN: 1432-1041
    Keywords: budesonide ; glucocorticoid ; nasal administration ; pharmacokinetics ; bioavailability ; systemic effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Budesonide, a topically potent glucocorticoid, was administered to 4 healthy volunteers by i.v. infusion and by nasal instillation of 100 µg tritium-labelled drug. Plasma was analyzed by liquid chromatography plus scintillation counting of collected fractions. After i.v. administration the plasma clearance was 0.92 l/min and the apparent volume of distribution was 2.8 l/kg. After nasal administration, the time to reach the peak plasma level was approximately 30 min, and the systemic availability was 102%. Budesonide had marginal effects on plasma cortisol and white blood cell counts either after i.v. or nasal administration. Thus, nasally instilled budesonide in solution is rapidly and completely absorbed from the nasal mucosa. The systemic effects after this clinically recommended nasal dose were negligible.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613465
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  • 11
    Electronic Resource
    Electronic Resource
    Intramuscular bioavailability of chlorazepate as compared to diazepam (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 229-230 
    Details
    ISSN: 1432-1041
    Keywords: diazepam ; dipotassiumchlorazepate ; benzodiazepines ; bioavailability ; administration ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Dipotassium chlorazepate (DPC) and diazepam (DZM) were given i.m. and i.v. to 6 healthy volunteers in doses of 20 mg (48.9 µmol) DPC and 15 mg (52.0 µmol) DZM. The interval between the injections was at least 1 week. Plasma samples were analyzed for DPC and DZM by HPLC. The bioavailability of DPC and DZM after i.m. administration, determined from computer calculated AUCs, was 1.04 and 0.85, respectively.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609698
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  • 12
    Electronic Resource
    Electronic Resource
    The influence of ascites on the pharmacokinetics of piretanide in cirrhotic patients (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 581-583 
    Details
    ISSN: 1432-1041
    Keywords: piretanide ; liver cirrhosis ; ascites ; bioavailability ; pharmacokinetics ; diuretic
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of piretanide, a new loop diuretic, were studied in seven patients with severe liver disease before and after resolution of ascites. The time to maximum concentration was significantly prolonged by the presence of ascites. Tmax after relief of ascites was similar to that seen for normal volunteers. Area under the curves, bioavailability, volumes of distribution and elimination half-lives did not change after resolution of the ascites: two patients in whom diuretic resistant ascites occurred showed similar pharmacokinetics to that of the diuretic responders. Reduced responsiveness to piretanide therapy in patients with gross ascites does not appear to be the result of decreased bioavailability.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544070
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  • 13
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of oral moclobemide in healthy human subjects and effects on MAO-activity in platelets and excretion of urine monoamine metabolites (1985)
    Springer
    European journal of clinical pharmacology 28 (1985), S. 89-95 
    Details
    ISSN: 1432-1041
    Keywords: moclobemide ; Ro 11-1163 ; pharmacokinetics ; bioavailability ; MAO activity in platelets ; monoamine metabolites in urine ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma concentrations of the MAO-inhibitor moclobemide (Ro 11-1163) were determined in six healthy male subjects after oral (tablets) administration. Effects on MAO activity in platelets and excretion of monoamine metabolites in urine were investigated. The design of the study was a double-blind cross-over study with single oral doses of placebo, 50, 100 and 200 mg of moclobemide. The elimination profile of the drug showed that the half life of the unchanged drug ranged between 1 and 2 h except in one subject with a half-life of about 4 h. The mean bioavailability calculated using flow model concepts was F=0.43 after 50 mg, F=0.47 after 100 mg and F=0.59 after 200 mg. The outlier with a t1/2 of 4 h was found to have a bioavailability of more than 0.80 after all 3 doses. The slightly increasing bioavailability with higher doses was interpreted as evidence of saturable hepatic first-pass elimination of the drug. MAO activity in platelets was measured before and 2, 6 and 24 h after drug administration. No inhibition of platelet MAO was obtained at any point in time or dose level, as to be expected since moclobemide preferentially inhibits MAO A. Urine excretion of the monoamine metabolites homovanillic acid (HVA), dihydroxyphenylacetic acid (DOPAC), 3-methoxy-4-hydroxy-phenylglycol (MOPEG) and 5-hydroxyindoleacetic acid (5-HIAA) was followed during 48 h after placebo, 50 and 200 mg of moclobemide. Time but not dose contributed significantly to the variability in excretion of the monoamine metabolites. An apparent reduction of HVA and DOPAC levels was obtained in the early phase after the administration of 200 mg of moclobemide. In 1 subject with a mild drug reaction a pronounced decrease in the levels of all the metabolites was obtained. In the other 5 subjects, the compound was very well tolerated with a few reported side-effects like increased activity, somnolence or sweatings. There was a slight but significant increase in blood pressure following 50 and 100 mg but not 200 mg of moclobemide.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00635714
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  • 14
    Electronic Resource
    Electronic Resource
    A nonlinear physiologic pharmacokinetic model: I. Steady-state (1985)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 13 (1985), S. 73-92 
    Details
    ISSN: 1573-8744
    Keywords: pharmacokinetic theory ; venous equilibration (“well-stirred”) model ; compartment model ; linear pharmacokinetics ; nonlinear pharmacokinetics ; bioavailability ; intrinsic clearance ; liver blood flow ; clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The two-compartment model of Rowland et al.,(2) has been extended by replacing first order elimination with Michaelis-Menten elimination kinetics. All of the equations for steady-state concentrations and clearances for zero order (constant rate) input orally (into compartment #2) and intravenously (into compartment #1) are derived and reported. The steady-state concentration in compartment #1, following intravenous administration, is shown to be a nonlinear function of maximal velocity of metabolism, Vm,the Michaelis constant, Km,and liver blood flow, Q;and, following oral administration is dependent only upon Vm and Km and is independent of Q.However, oral bioavailability is a function of Vm, Km,and Q.The model allows physiologic pharmacokinetic interpretation of both linear and nonlinear data; and, together with simple modification of the model, can explain much observed pharmacokinetic data to date particularly for first-pass drugs. Future articles in the series will be concerned with single doses, evaluation of literature data in terms of the model, application of the theory in toxicology and in clinical pharmacokinetics and therapeutics.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01073657
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  • 15
    Electronic Resource
    Electronic Resource
    Distribution, elimination, metabolism and bioavailability of hexamethylenebisacetamide in rats (1985)
    Springer
    Investigational new drugs 3 (1985), S. 263-272 
    Details
    ISSN: 1573-0646
    Keywords: HMBA ; hexamethylenebisacetamide ; bioavailability ; toxicity ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Hexamethylenebisacetamide (HMBA), an in vitro differentiating agent, was studied for its pharmaco-dynamic actions in animals. Plasma stability, organ distribution, excretion, oral bioavailability, and estimates of pharmacokinetic parameters and acute lethality were determined in rats. The single dose intraperitoneal LD50 was greater than 3000 mg/kg in both mice and rats. The drug was stable in plasma from several different species during an 8 h in vitro incubation at 37°C. Following a single intravenous (iv) bolus injection (1000 mg/kg) to rats, HMBA was removed from the plasma with a half time of 2.2 ± 0.5 h, and 65 ± 8% of the dose was excreted unchanged in the urine during the first 24 h after dosing. During an 8 h iv infusion, plasma concentrations of 4 mM were easily maintained with no apparent adverse effects. Drug was uniformly distributed, with highest concentrations found in thymus, kidney, liver, and lymph node throughout the first 24 h after a single iv bolus dose. In vivo metabolism was very small, and the presence of apparent metabolites was undetectable until 48 h after iv administration. Oral bioavailability was good (32%), with peak plasma concentrations of 2 mM achieved one hour after oral administration. After oral dosing urinary excretion and plasma decay were comparable to similar data obtained after iv dosing.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00179430
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  • 16
    Electronic Resource
    Electronic Resource
    New method for bioavailability assessment of slow-release preparations of theophylline (1985)
    Springer
    Journal of pharmacokinetics and pharmacodynamics 13 (1985), S. 571-587 
    Details
    ISSN: 1573-8744
    Keywords: theophylline ; bioavailability ; variability in clearance ; siow-release preparations ; urinary metabolites
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Variability in an individual's clearance of theophylline is an important consideration when estimating bioavailability. A method is described for compensating for this problem, using the serum concentration of theophylline and urinary excretion data on its major metabolites to make an estimation of the clearance after oral administration using the intravenous dose as reference. The method is particularly useful for assessing the bioavailability of slow-release theophylline preparations.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01058902
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