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Absolute bioavailability of terbutaline from a CR-granulate in asthmatic children
G Fuglsang1, B Hertz, E B Holm
1Department of Pediatrics, Viborg Hospital, Denmark.
Insights
This study determined the absolute bioavailability of a new controlled-release (CR) terbutaline granulate in children with asthma. The CR-granulate demonstrated a bioavailability comparable to adult CR-tablets, suggesting it
Area of Science:
- Pharmacokinetics
- Pediatric Pharmacology
- Respiratory Medicine
Background:
- Asthma management in children often relies on effective bronchodilators.
- Controlled-release (CR) formulations aim to provide sustained drug delivery and improve patient compliance.
- Terbutaline is a commonly used beta-2 agonist for asthma treatment.
Purpose of the Study:
- To determine the absolute bioavailability of a newly developed controlled-release (CR) terbutaline granulate in pediatric asthma patients.
- To compare the pharmacokinetic profile of the CR-granulate in children with existing data from adult studies.
- To evaluate the suitability of the CR-granulate as an alternative to existing terbutaline formulations.
Main Methods:
- Eight children (aged 8-13 years) with asthma participated in the study.
- Participants received a 3 mg oral dose of the terbutaline CR-granulate.
- Simultaneously, an intravenous dose of deuterium-labelled terbutaline (0.100 mg) was administered for comparative analysis.
- Plasma concentrations of terbutaline were measured to determine pharmacokinetic parameters.
Main Results:
- The maximal plasma concentration (Cmax) of terbutaline was 8.7 nmol/L (range: 4.9-15.2 nmol/L), achieved at 4.7 hours (range: 2.2-6.0 h).
- The absolute bioavailability of the terbutaline CR-granulate was calculated to be 10.8% (range: 7.63-16.4%).
- Pharmacokinetic parameters were comparable to those observed in adult studies using terbutaline CR-tablets.
Conclusions:
- The newly developed terbutaline CR-granulate exhibits acceptable absolute bioavailability in pediatric asthma patients.
- The CR-granulate formulation is easily administered and suitable for twice-daily dosing.
- This formulation presents a viable alternative to existing terbutaline elixir or plain tablets, which require three-times-daily dosing.
Abstract:
The study aimed at finding the absolute bioavailability of terbutaline of a newly developed CR-granulate. Eight asthmatic children, aged 8-13 years, were given 3 mg of terbutaline as the CR-granulate, concomitant with the intravenous administration of 0.100 mg of deuterium-labelled terbutaline. The labelling of the intravenous dose made possible a separation, in the analytical step, of terbutaline originating from the intravenous and oral administration. Maximal plasma concentration, 8.7 (range: 4.9-15.2) nmol l-1, was reached after 4.7 (2.2-6.0) h. Absolute bioavailability was 10.8 (7.63-16.4) per cent. The parameter values were similar to those found after administration of terbutaline CR-tablets to adults. The CR-formulation is easily swallowed and can be dosed twice daily. Thus it should be a good alternative to elixir or plain tablets, dosed three times a day.