The absolute bioavailability of caffeine in man

  title={The absolute bioavailability of caffeine in man},
  author={James Blanchard and STEWART J. A. Sawers},
  journal={European Journal of Clinical Pharmacology},
SummaryThe absolute bioavailability of orally administered caffeine was investigated in 10 healthy adult male volunteers, aged 18.8 to 30.0 years. The subjects were administered a 5 mg/kg dose of caffeine as either an aqueous oral solution or an intravenous infusion, on separate occasions about 1 week apart, in a randomized crossover fashion. Plasma samples were collected over the 24-h period following each dose and assayed for their caffeine content using a high-performance liquid… 
Comparison of caffeine disposition following administration by oral solution (energy drink) and inspired powder (AeroShot) in human subjects
Inspiration of caffeine as a fine powder using the AeroShot device produces a similar caffeine profile and effects compared to administration of an oral solution (energy drink).
Impairment of caffeine clearance by chronic use of low-dose oestrogen-containing oral contraceptives
Caffeine clearance, previously reported to be a specific marker of cytochrome P-448 activity in man, is decreased by chronic OCS use, which suggests that OCS may cause significant impairment of this enzyme activity as assessed in vivo.
Urinary caffeine metabolites in man
Caffeine degradation was impaired in patients with cirrhosis and was increased in persons who smoked heavily or who were on phenytoin therapy, and the possibility of noninvasively investigating gross differences in caffeine disposition by analysis of the urinary pattern of its metabolites is document.
Caffeine Use in Sports, Pharmacokinetics in Man, and Cellular Mechanisms of Action
Evidence from in vitro studies provides a wealth of different cellular actions that could potentially contribute to the observed effects of caffeine in humans in vivo, although a variable degree of contribution cannot be readily discounted on the basis of experimental data.
Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition
A simple pharmacokinetic model for the caffeine-quinolone interaction was developed, which provides a unified method for evaluation and comparison of the effect of quinolones on the disposition of caffeine.
Time to Recover From Daily Caffeine Intake
The findings unveil that conventional daily caffeine intake does not provide sufficient time to clear up psychoactive compounds and restore cerebral responses, even after 36 hours of abstinence, and suggest investigating consequences of a paraxanthine accumulation during daily caffeine Intake.
Effects of moderate exercise on the pharmacokinetics of caffeine
Both during exercise and at rest, HD had a greater half-life elimination and volume of distribution than LD, and an increase in its distribution due to regular heavy coffee intake.
A Randomized, Two-Way Crossover Study to Evaluate the Pharmacokinetics of Caffeine Delivered Using Caffeinated Chewing Gum Versus a Marketed Caffeinated Beverage in Healthy Adult Volunteers
Existing scientific literature on caffeine, based mostly on data from caffeinated beverages, can be leveraged to support the safety of caffeine delivered by chewing gum and current maximum safe caffeine dose advice should be applicable irrespective of delivery method.
Validated HPLC method for determination of caffeine level in human plasma using synthetic plasma: application to bioavailability studies.
The method was successfully applied to monitor caffeine levels in healthy volunteers with correction of caffeine levels using the mean ratio of the slopes of the calibration's curves constructed using human and synthetic plasma.
Population pharmacokinetics of caffeine and its metabolites theobromine, paraxanthine and theophylline after inhalation in combination with diacetylmorphine.
The presented model adequately describes the population pharmacokinetics of caffeine and its dimethylxanthine metabolites after inhalation of the caffeine sublimate of a 100 mg tablet.


Pharmacokinetic profile of caffeine in the premature newborn infant with apnea.
The fate of caffeine in man and a method for its estimation in biological material.
A sensitive method for the estimation of caffeine in biological material is described and it is shown that although a considerable amount of caffeine accumulates in the body of moderately heavy coffee drinkers during the day, there is no day to day accumulation of the drug.
Some Comments on the Evaluation of Bioavailability Data
It is concluded that the half-life correction should be evaluated in all cases where the variability in half- life is random, and applied if it results in a significant decrease in the standard deviation associated with the average measure of bioavailability, and not if there is a significant difference or strong indication of a difference inHalf-life between treatments.
Improved liquid-chromatographic determination of caffeine in plasma.
A rapid, specific, and sensitive liquid-chromatographic micro-method for caffeine in plasma that is ideally suited for measuring caffeine in the plasma of infants and small animals as well as adults.
Normalization in the fitting of data by iterative methods. Application to tracer kinetics and enzyme kinetics.
  • J. Ottaway
  • Environmental Science
    The Biochemical journal
  • 1973
It was found that dividing each deviation by the mean of observed and calculated variable appropriate to it produces a weighting that is fairly free from bias as judged by the criteria mentioned above.
Statistical estimations in pharmacokinetics
Several important statistical aspects of pharmacokinetic analyses by digital computer are discussed. These include selection of appropriate equations, weighting of data, precision of parameter
The Mathematical Approach to Physiological Problems
This is a revised and updated edition of a book of fundamental importance in the rigorous theory of solutions of the Navier-Stokes equations. The authoress considers the questions of their existence