Continued investigation into the influence of loaded dose on the performance of dry powder inhalers: surface smoothing effects

Drug Dev Ind Pharm. 2006 Nov-Dec;32(10):1135-8. doi: 10.1080/03639040600712920.

Abstract

The aerosolization of salbutamol sulfate, measured as fine particle dose (FPD LD) and fine particle fraction (FPF LD) (<6.4 microm mass median aerodynamic diameter), from two sieved (63-90 microm) lactose monohydrate carriers, one as supplied, one smoothed by controlled surface dissolution, was studied. In general, no significant variation in FPD LD was observed at drug loadings between 10 and 63.5 microg and 10 and 135 microg for the surface dissolved and as supplied lactose monohydrates, respectively. Increasing the drug load above these levels resulted in linear increases in FPD LD with increasing drug load with the surface dissolved lactose monohydrate exhibiting higher FPD LD and FPF LD. This suggests that, at lower drug loadings, areas of the carrier exhibiting higher adhesion, so-called active sites, were being preferentially occupied and filled. Since there was no evidence of drug agglomeration using scanning electron microscopy, the observations suggest that the number and range of such higher energy "active sites" can be reduced by modifying the surface roughness, that is, energies, of the carrier.

MeSH terms

  • Administration, Inhalation
  • Aerosols
  • Albuterol / administration & dosage*
  • Binding Sites
  • Bronchodilator Agents / administration & dosage
  • Drug Carriers / administration & dosage*
  • Drug Carriers / chemistry*
  • Lactose / administration & dosage
  • Lactose / chemistry
  • Microscopy, Electron, Scanning
  • Particle Size
  • Powders
  • Surface Properties

Substances

  • Aerosols
  • Bronchodilator Agents
  • Drug Carriers
  • Powders
  • Lactose
  • Albuterol