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Theophylline pharmacokinetics in children, comparing sustained release spheres (Theo-Dur sprinkle) with elixir
N I Kjellman1, S Croner, I Leijon
1Department of Paediatrics, University Hospital, Linköping, Sweden.
Insights
A new sustained release theophylline preparation (Theo-Dur Sprinkle) significantly reduced theophylline level fluctuations in children with asthma compared to elixir. This improved dosing consistency and was preferred by parents.
Area of Science:
- Pediatric Pulmonology
- Pharmacokinetics
- Drug Formulation
Background:
- Bronchial asthma management in children requires consistent therapeutic drug levels.
- Traditional theophylline elixir formulations often result in significant pharmacokinetic fluctuations.
- Sustained-release theophylline preparations aim to improve dosing convenience and therapeutic efficacy.
Purpose of the Study:
- To compare the pharmacokinetic profiles of a new sustained-release theophylline preparation (Theo-Dur Sprinkle, TDS) with a theophylline elixir in children with asthma.
- To evaluate the fluctuation and bioavailability of theophylline from TDS.
- To assess parental preference for the new formulation.
Main Methods:
- An open-label, randomized cross-over study involving eight children (4-10 years) with bronchial asthma.
- Administered TDS twice daily (b.i.d.) and theophylline elixir three times daily (t.i.d.) at a dose of approximately 20 mg/kg/day.
- Collected serum theophylline concentrations 11 times over 24 hours on day 3 of each treatment regimen.
Main Results:
- TDS demonstrated significantly lower fluctuations in serum theophylline levels (54%) compared to elixir (276%).
- Morning theophylline levels were more consistent with TDS, with less inter-day variability.
- The bioavailability of theophylline from TDS was 94%, and parents preferred TDS in seven out of eight cases.
Conclusions:
- Theo-Dur Sprinkle exhibits satisfactory sustained-release properties, leading to more stable serum theophylline concentrations in pediatric asthma patients.
- The reduced fluctuation and improved dosing consistency of TDS offer potential advantages over elixir formulations.
- Individualized theophylline dosage, guided by symptom monitoring and serum concentration measurements, remains crucial for optimal asthma management.
Abstract:
A new sustained release theophylline preparation (Theo-Dur Sprinkle, TDS) was given b.i.d. and a theophylline elixir t.i.d. to eight children with bronchial asthma, 4-10 years of age, in an open study with a randomized cross over design. The serum concentration curves of theophylline were compared. The individual theophylline dose was close to 20 mg/kg body weight per day. On day 3 of each regimen, blood samples were taken 11 times over 24 h. There were great differences between morning concentrations of theophylline, with a range from 0.9-10.7 mg/l in children given elixir, while corresponding values for children given TDS were 4.1-19.3 mg/l. Fluctuation during a dosing interval was 276% for elixir but only 54% in the case of TDS. The morning theophylline levels on two consecutive days did not differ significantly when the children were treated with TDS. The bioavailability of theophylline from TDS was 94% (range 54%-121%). Parents preferred TDS in seven of the eight cases. TDS showed satisfactory sustained release properties but the study confirmed the need for individually tailored dosage of theophylline based on monitoring of symptoms and serum concentrations.