A novel gas phase method for the combined synthesis and coating of pharmaceutical particles

Pharm Res. 2008 Jan;25(1):242-5. doi: 10.1007/s11095-007-9464-4. Epub 2007 Oct 20.

Abstract

Purpose: A novel aerosol flow reactor method for the combined gas phase synthesis and coating of particles for drug delivery has been developed.

Materials and methods: As an example, micron-sized salbutamol sulfate particles were produced via droplet-to-particle conversion and in-situ coated by the physical vapor deposition (PVD) of L-leucine vapor.

Results: During the deposition, L-leucine vapor crystallized on the surfaces of amorphous salbutamol particles. The size of L-leucine crystallites increased with increasing vapor concentration of L-leucine. The salbutamol particles with rough L-leucine surfaces exhibited good flowability enabling to them to be dispersed into air flow without the delivery aid of coarse lactose carriers.

Conclusions: The fraction of particles smaller than 5 micrometers varied between 0.35 and 0.48 when dispersed into 60 l/min air flow having a jet Reynolds number of 30700. When the coated fine particles were blended with lactose carriers, the fine particle fraction was as high as 90%. The L-leucine coating also improved the stability of salbutamol particles when stored at 45% relative humidity atmosphere.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aerosols
  • Albuterol / administration & dosage
  • Albuterol / chemistry
  • Bronchodilator Agents / administration & dosage
  • Bronchodilator Agents / chemistry
  • Drug Compounding
  • Gases
  • Leucine / chemistry
  • Microscopy, Electron, Scanning
  • Nanoparticles / chemistry*
  • Particle Size

Substances

  • Aerosols
  • Bronchodilator Agents
  • Gases
  • Leucine
  • Albuterol