Comparison of physical and inhalation properties of spray-dried and micronized terbutaline sulphate.
Terbutaline sulphate particles, for use in dry powder inhaler formulations, were prepared by spray-drying, using a Büchi 190 mini spray dryer. Spray-drying conditions were chosen to allow the production of spray-dried terbutaline sulphate with a size similar to micronized terbutaline sulphate, that is to say about 2.9 microm of volume mean diameter. The physical properties and in vitro inhalation behaviour of micronized and spray-dried terbutaline sulphate were compared. X-ray diffraction, DSC, SEM and laser size analysis were investigated. Spray-dying produced spherically shaped particles with amorphous structure. After blending with different lactoses, adhesion and aerodynamic properties were investigated. Evaluation of adhesion was carried out with a mechanical sieve and an Alpine air-jet sieve. The adhesion of terbutaline sulphate on the lactoses tested was lower in the case of the spray-dried drug. Aerodynamic evaluation of fine particle dose and emitted dose was conducted using a twin stage impactor. The emitted doses and the fine particle doses were higher with the spray-dried terbutaline sulphate. The Alpine air-jet sieve assays showed that there was a correlation between drug separation from a carrier by sieving and that obtained from longer in vitro deposition studies. There was a linear relationship between the adhesion characteristics and the fine particle dose.
Thi
Thanh Huong Hoang
TH
Laboratoire de Pharmacotechnie Industrielle, Faculté des Sciences Pharmaceutiques et Biologiques, Université de Lille, Lille Cedex, France.
Danède
Florence
F
Descamps
Marc
M
Flament
Marie-Pierre
MP
D000280:Administration, Inhalation; D000336:Aerosols; D001993:Bronchodilator Agents / Q000008:administration & dosage / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003890:Desiccation; D004337:Drug Carriers; D007785:Lactose / Q000737:chemistry; D009330:Nebulizers and Vaporizers; D010316:Particle Size; D011208:Powders; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*; D013726:Terbutaline / Q000008:administration & dosage / Q000737:chemistry*; D000267:Tissue Adhesions
D000336:Aerosols; D001993:Bronchodilator Agents; D004337:Drug Carriers; D011208:Powders; D007785:Lactose; D013726:Terbutaline