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Absolute and relative bioavailability of a slow release theophylline preparation in asthmatic children
A L Boner1, G De Stefano, G Vallone
1Paediatric Clinic, University of Verona, Italy.
Insights
This study compared three theophylline preparations in children with asthma. Slow-release theophylline demonstrated good bioavailability, similar to other pediatric formulations.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Respiratory Medicine
Background:
- Asthma management in children requires effective theophylline delivery.
- Understanding the pharmacokinetics of different theophylline formulations is crucial for optimizing treatment in pediatric patients.
Purpose of the Study:
- To compare the bioavailability and pharmacokinetic profiles of three theophylline preparations in asthmatic children.
- To evaluate slow-release theophylline capsules against intravenous aminophylline and oral normal-release lysine theophyllinate.
Main Methods:
- A crossover study design involving 14 asthmatic children aged 7-13 years.
- Administration of three single doses (100 mg active ingredient): intravenous aminophylline, oral lysine theophyllinate solution, and oral slow-release theophylline capsules.
- Plasma theophylline concentrations were measured using fluorescent polarization immunoassay and analyzed via compartmental and non-compartmental methods.
Main Results:
- Slow-release theophylline achieved a maximum plasma concentration of 3.19 +/- 0.63 microgram/ml at 8.71 +/- 2.30 hours.
- Oral normal-release solution yielded a higher maximum concentration (4.51 +/- 0.94 microgram/ml) at an earlier time (1.96 +/- 0.85 hours).
- Mean absolute bioavailability for slow-release theophylline was 92.7 +/- 23.2%, and relative bioavailability was 83.14 +/- 14.69%.
Conclusions:
- Slow-release theophylline exhibits favorable bioavailability in asthmatic children, comparable to other pediatric formulations.
- The pharmacokinetic profile suggests slow-release theophylline is a viable option for managing asthma in this age group.
- Further research may explore long-term efficacy and safety of slow-release theophylline in pediatric asthma.
Abstract:
This study was carried out on 14 asthmatic children 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 microgram/ml and 8.71 +/- 2.30 h, respectively, compared to 4.51 +/- 0.94 microgram/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.