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Monday 22 October 2007

A Novel Gas Phase Method for the Combined Synthesis and Coating of Pharmaceutical Particles.

By: Raula J, Lähde A, Kauppinen EI.

Pharm Res 2007 Oct;(): [Epub ahead of print]

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.

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