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Pharmacokinetic characteristics of a novel controlled-release sprinkle formulation of salbutamol
S Mulligan1, J Devane, M Martin
1Elan Corporation plc., Athlone, Ireland.
Insights
A new controlled-release salbutamol sprinkle offers a more acceptable and convenient option for pediatric asthma patients. This novel formulation shows potential for effective asthma control in children, improving ease of administration.
Area of Science:
- Pharmacology
- Pediatric Medicine
- Drug Delivery Systems
Background:
- Childhood asthma affects 5-12% of children, commonly treated with salbutamol.
- Aerosolized salbutamol presents practical administration challenges, especially for young children.
- There is a need for convenient and effective pediatric salbutamol formulations.
Purpose of the Study:
- To compare a novel controlled-release salbutamol sprinkle formulation with a reference salbutamol tablet.
- To evaluate the suitability of the sprinkle formulation for pediatric asthma treatment.
Main Methods:
- A six-subject, unblinded, single-dose, cross-over study.
- Comparison of 8 mg salbutamol sprinkle (pharmaZome technology) with 8 mg salbutamol tablet (Proventil Repetabs).
- Administration of sprinkle formulation mixed with jam.
Main Results:
- Pharmacokinetic parameters (time to peak concentration, half-life, peak-to-trough ratio) were similar between formulations.
- Mean plasma and peak salbutamol levels were slightly lower for the sprinkle formulation.
- The sprinkle formulation was administered easily and acceptably.
Conclusions:
- The novel controlled-release salbutamol sprinkle formulation is a potential effective bronchodilator.
- This formulation offers significant advantages for pediatric dosing due to ease and acceptability.
- Further development may provide an improved option for managing childhood asthma.
Abstract:
Childhood asthma, which commonly effects between 5 and 12% of children, is often treated with the beta agonist salbutamol which relaxes bronchial smooth muscle, resulting in bronchodilation. Although a popular mode of administration, delivery of salbutamol by aerosol is not often practical, particularly in younger children. A need therefore exists for a pediatric salbutamol dosage form, which not only controls asthma but is also convenient and acceptable to use. Enhanced control of asthma may be achieved using a controlled-release formulation of salbutamol. This also serves to increase patient compliance which may be further improved, in the case of children, by presenting the formulation in a more acceptable paediatric dosage form. In this study, a novel controlled-release sprinkle formulation of salbutamol was compared with a reference salbutamol tablet (Proventil Repetabs). This was conducted as a six subject unblinded, single-dose, cross-over study comparing a single dose (8 mg) of salbutamol sprinkle with a single dose (2 x 4 mg) of the reference tablet. The salbutamol sprinkle was formulated using the controlled-release polymeric micromatrix pharmaZome technology and was administered as a single dose dispersed in a spoonful of jam. The time to peak concentration, half-life and peak-to-trough ratio were similar for both formulations. Mean plasma salbutamol levels and mean peak salbutamol levels were slightly lower for the sprinkle formulation when compared with the reference. This novel sprinkle formulation has potential as an effective controlled-release bronchodilator which also offers distinct advantages for paediatric dosing, in terms of ease and acceptability of administration.