This study was carried out on 14 asthmatic childen aged 7–13 years. They all received three preparations (aminophylline by intravenous infusion, lysine theophyllinate orally in solution and slow release theophylline orally as capsules) in a single dose of 100 mg active ingredient in a crossover design. Plasma theophylline concentrations, determined by a fluorescent polarization immunoassay, were evaluated both by compartmental and non-compartmental analysis. After administration of slow release theophylline, its maximum plasma concentration and the time needed to reach this were (± SD) 3.19 ± 0.63 μg/ml and 8.71 ± 2.30 h, respectively, compared to 4.51 ± 0.94 μg/ml and 1.96 ± 0.85 h, respectively, for the oral normal release solution. Mean absolute and relative percentage bioavailabilities for slow release theophylline in asthmatic children were (± SD) 92.7 ± 23.2% and 83.14 ± 14.69%, respectively. These are similar to the values found with other slow release formulations in paediatric patients.

1986-04-01·British Journal of Clinical Pharmacology2区 · 医学

The interaction between i.v. theophylline and chronic oral dosing with slow release nifedipine in volunteers.

2区 · 医学

Article

作者: Johnston, A. ; Shah, K. ; Jackson, S. H. D. ; Debbas, N. M. G. ; Turner, P. ; Peverel-Cooper, C. A.

Eight healthy volunteers received a 5 min i.v. infusion of lysine theophylline, equivalent to 197 mg anhydrous theophylline, both before (day 1) and during (day 5) steady state chronic oral dosing with slow release nifedipine 20 mg 12 hourly. A theophylline pharmacokinetic profile was performed on day 1 and day 5 and a nifedipine pharmacokinetic profile was performed on day 4 and day 5. The greatest difference in serum theophylline concentrations was seen at the first sampling time (5 min after completion of the infusion) with a mean concentration of 9.9 mg l‐1 during nifedipine administration and 14.6 mg l‐1 with theophylline alone. Thereafter, the difference fell to approximately 1 mg l‐1 until 6 h when they became almost identical. Repeated measures analysis of variance using the theophylline serum concentrations at each of ten time points over 8 h as the repeated measures showed a small but significant effect of nifedipine (F(1,151) = 7.0, P less than 0.01) on serum theophylline concentrations. Mean volume of distribution (V) rose from 0.33 +/‐ 0.07 to 0.39 +/‐ 0.06 1 kg‐1 corrected body weight (CBW) in the presence of nifedipine (t = 2.23, P = 0.052). Theophylline clearance, area under the curve to 8 h AUC (0‐8), area under the curve to infinity AUC (0‐infinity) and elimination half‐life (t1/2) did not change appreciably. No statistically significant changes in nifedipine pharmacokinetics occurred in the presence of theophylline.

1984-08-01·British Journal of Clinical Pharmacology2区 · 医学

The stimulatory effects of caffeine, theophylline, lysine‐theophylline and 3‐isobutyl‐1‐methylxanthine on human sperm motility.

2区 · 医学

Article

作者: Turner, P. ; Kilfeather, S. A. ; Pearson, R. M. ; Jiang, C. S.

The potencies of caffeine, theophylline, lysine‐theophylline and 3‐ isobutyl‐1‐methylxanthine (IBMX) in stimulating sperm motility have been compared, and we have found IBMX to be significantly more potent than the other three compounds, which did not exhibit significant differences in potency from each other.

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