Abstract
PURPOSE: Engineering of inhalation particles incorporating, in each individual particle, a combination of a long-acting beta-agonist and a glucocorticosteroid in a pre-determined and constant ratio for delivery via a dry powder inhaler (DPI).
METHODS: Individual crystalline particles containing both the glucocorticosteroid fluticasone propionate (FP) and long-acting beta-agonist salmeterol (SX) were prepared, in a ratio of 10:1, using the solution atomization and crystallization by sonication (SAX) process. Combination drug particles were characterized by particle size, morphology, crystallinity and aerosolisation efficiency using inertial impaction.
RESULTS: Combination drug particles were spherical and crystalline, with a median diameter of 4.68 +/- 0.01 microm. Aerosolisation of formulations containing combination drug particles resulted in greater uniformity in delivery ratios of both actives across all stages of the impactor before and after storage.
CONCLUSIONS: Actives in a pre-determined dose ratio can be crystallised in a single particle using the SAX process.
| Original language | English |
|---|---|
| Pages (from-to) | 2657-2666 |
| Number of pages | 10 |
| Journal | Pharmaceutical Research |
| Volume | 26 |
| Issue number | 12 |
| Early online date | 25 Sept 2009 |
| DOIs | |
| Publication status | Published - 1 Dec 2009 |
Keywords
- Administration, Inhalation
- Adrenal Cortex Hormones
- Adrenergic beta-Agonists
- Albuterol
- Androstadienes
- Bronchodilator Agents
- Calorimetry, Differential Scanning
- Drug Combinations
- Drug Storage
- Inhalation
- Microscopy, Electron, Scanning
- Particle Size
- Powders
- Protein Engineering