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METHOD FOR ENLARGING THE PARTICLE SIZE OF CRYSTALLINE MICROPARTICLES OF ACTIVE SUBSTANCE
专利权人:
Jesalis Pharma GmbH
发明人:
Detlef Grawe,Sabine Gliesing
申请号:
US14442354
公开号:
US20160271145A1
申请日:
2013.11.18
申请国别(地区):
US
年份:
2016
代理人:
摘要:
A method for enlarging the particle size of crystalline microparticles of active substance by providinga first suspension prepared from crystalline microparticles of active substance with a first d50 value of 0.5-5 μm, solvent and antisolvent for the active substance, wherein the solubility of the active substance in the solvent-antisolvent mixture of the first suspension is 0.001-0.5 wt. %, such that the average particle diameter (d50 value) at the end or the method is at least 0.03 μm larger than the starting d50 value. The d50 values of a first batch can also serve to control the particle coarsening of a second batch. In addition, particles of fluticasone propionate having an average particle size d50 of 1.0-1.5 μm and simultaneously a narrow particle size distribution with a span <;1.35 and high crystallinity with an amorphous fraction of <;0.5 wt. % can be prepared.
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