Astrazeneca Ab

Saeed Moshashaee

Mikael Bisrat

Goran Eric Sundholm

H&aring;kan Nyqvist

Mustafa Demirb&uuml;ker

Mustafa Demirbuker

A process for preparing particles of a substance, such as a protein or polypeptide, comprising: (a) preparing a first liquid comprising water, the substance and a modulator, wherein the modulator has a solubility in water which decreases with increasing temperature; and (b) contacting the first liquid with a second liquid comprising a fluid gas and an organic solvent using an anti-solvent fluid gas technique under conditions of temperature and pressure which result in the precipitation of particles comprising the substance, wherein the temperature of the first liquid is at or above the cloud point temperature of the first liquid when the first liquid contacts the second liquid. Also claimed are particles obtained according to the process and compositions containing the particles.

Process

Process for preparing particles

The invention provides a process for crystallization of amorphous and/or meta-stable crystalline regions of preformed particles by treating the particles with a supercritical or subcritical fluid containing an anti-solvent and a solvent. The invention further provides formulations comprising particles produced according to the present process containing one or more pharmacologically active substances and one or more pharmaceutically acceptable excipients, use of said formulations in the treatment of an allergic and/or inflammatory condition of the nose or lungs and methods for treatment of such conditions.

Composition of matter

The invention provides finely divided, substantially crystalline particles of budesonide characterized in that they are substantially smooth and having a BET value of from 1 to 4.5 m2/g, a process for their preparation, a pharmaceutical composition comprising said particles, the use of said particles in the treatment of and in the manufacture of a medicament for use in the treatment of respiratory disorder, and a method of treatment of respiratory disorders by administration of said particles to a host in need of such treatment.

Budesonide particles and pharmaceutical compositions containing them

The invention provides a process for preparing essentially crystalline particles containing a substance in solvated form, by dissolving the substance in a first solvent, introducing the solution and a supercritical or subcritical fluid into an apparatus, wherein the fluid contains an anti-solvent and a second solvent, which is water. Preferably, the anti-solvent is carbon dioxide which is totally saturated with the second solvent, which is water. The invention further provides formulations comprising particles produced according to the present process containing one or more pharmacologically active substances and one or more pharmaceu-tically acceptable excipients, use of said formulations in the treatment of an allergic and/or inflammatory condition of the nose or lungs and methods for treatment of such conditions.

Crystallization using supercritical or subcritical fluids

The invention provides finely divided, substantially crystalline particles of budesonide characterized in that they are substantially smooth and having a BET value from 1 to 4.5 m /g, process for their preparation, a pharmaceutical composition comprising said particles, the use of said particles in the treatment of and in the manufacture of a medicament for use in the treatment of a respiratory disorder, and a method of treatment of respiratory disorders by administration of said particles to a host in need of such treatment.

Growing community of inventors

Stockholm, Sweden

Saeed Moshashaee