Limited information is available on the pharmacokinetics and bioavailability of prednisone and prednisolone in patients with different disease states. This is partly due to difficulty in measuring these drugs in biological fluids at the usual dosages prescribed to patients. This article attempts to comprehensively review these studies categorized under the following four sections: (1) bioavailability—healthy volunteers, patients with respiratory disease, patients with liver disease, patients with kidney disease, pediatric patients with various diseases, effect of antacids, effect of food, effect of other drugs (aminophylline, cholestyramine); (2) pharmacokinetics—healthy volunteers, patients with respiratory disease, patients with liver disease, patients with kidney disease, pediatric patients with various diseases, effect of other drugs, enzyme induction of steroids and the effect on the kinetics of steroids and other drugs; (3) protein binding; and (4) analytical methods. The literature is reviewed through August 1979.

Pharmacokinetics and bioavailability of prednisone and prednisolone in healthy volunteers and patients: A review

I. Introduction THE PHARMACOLOGICAL response (dynamics) to corticosteroids is determined by the affinity of these steroids to specific receptors at the target organ and by the availability and duration of time spent at receptor sites (1). The latter is determined by kinetic factors such as systemic availability, protein binding, distribution, metabolism, and excretion. Two comprehensive reviews of the pharmacokinetics of prednisolone have been published by Pickup in 1979 (2) and Jusko and Rose in 1980 (3). This review examines factors which modulate the kinetics and dynamics of prednisone/prednisolone, the most commonly prescribed synthetic glucocorticosteroids in clinical practice. II. Analytical Techniques In the past, investigations of prednisone and prednisolone metabolism were performed by analyzing the plasma disappearance of [3H]prednisolone (4,5). In those studies chromatography was mandatory before radioactive counting in order to distinguish between prednisolone or prednisone and labeled metabol...

Kinetics and Dynamics of Prednisolone

Two fourtreatment crossover studies were performed using 12 adult male volunteers in each with seven different commercially available prednisolone tablets. Plasma samples were assayed for prednisolone by a radioimmunoassay method. Statisacal analyses of the data, by analysis of variance for crossover design (ANOVA), showed no significant differences among the treatment averages at any of the sampling times except at 0.25 and 4 hr in one of the studies. There were also no significant differences among the treatment averages for peak plasma level, time of peak plasma level, area 0–12 hr, area 0–24 hr, and the halflife of elimination of prednisolone. We conclude that the average plasma concentrations of prednisolone are superimposable in a statistical sense and that the tablets tested are bioequivalent. Results of dissolution studies of six tablets of each of the seven lots of prednisolone tablets, using deaerated water in the spin filter apparatus, are presented.

Bioavailability of prednisolone tablets

Two commercial prednisone tablets were studied which had previously been shown by Sullivan et al.5,6 to have the slowest and fastest in vitro rates of dissolution, and the slowest and fastest rise to peak plasma prednisolone concentrations in human beings. The effect of food on the adsorption of these two tablets was studied in a crossover study, which also repeated the fasting conditions used by Sullivan et al.6 Marked differences in mean prednisolone plasma concentrations during the 0- to 2-hour absorption phase were observed between the two tablets again, but food did not affect either tablet with respect to mean plasma prednisolone concentrations.

http://deepblue.lib.umich.edu/bitstream/handle/2027.42/97294/j.1552-4604.1976.tb01500.x.pdf;sequence=1

M.A. Schork

Papers

Statistical survey of “saturation analysis” calibration curve data for prednisolone, prednisone and digoxin