Schering Aktiengesellschaft

Jesalis Pharma Gmbh

Bayer Pharma Aktiengesellschaft

Hapila Gmbh

Sabine Gliesing

Detlef Grawe

Hagen Gerecke

Peter Hoesel

Uwe Mueller

Robert Eilers

Annette Eichardt

Michael Sander

Bernd Erhart

Ulf Tilstam

Thomas Michel

Uwe Knabe

Michael Mosebach

David Voigtlaender

Jürgen Jacke

Klaus Bahl

Ulf Bohlmann

Dieter Wehmeier

Peter Hosel

Uwe Muller

A method and device for producing crystalline active ingredient particles. The active ingredient is crystallized from a supersaturated solution on the surface of particles of the active ingredient. A suspension of active ingredient particles is subjected to wet grinding in a supersaturated solution of the active ingredient in a first module. At least a part of the suspension is fed from the first module into the second module where it is cooled and simultaneously subjected to ultrasound. The suspension is fed back into the first module after cooling and being subjected to ultrasound. Active ingredient solution and optionally antisolvent are added to the suspension and active ingredient particles and liquid phase are extracted. A relative supersaturation of the active ingredient in the liquid phase of the suspension, relative to the entire liquid phase, is &#x2266;90%, and the extracted active ingredient particles comprise a mean particle size of 10-500 &#x3bc;m.

Method for producing crystalline active ingredient particles

A method for producing highly crystalline and stable microparticles of an active substance with a very narrow size distribution. The microparticles being crystallized out of a suspension made of primary particles of the active substance, a solution of the active substance, a non-solvent for the active substance and inert formed pieces. The resulting microparticles hare are highly stable largely independent of the physiochemical properties of the active substance and can be especially suitable for fast release dosage forms of pharmaceuticals.

Crystalline active ingredient microparticles, method for producing the same and use thereof in drugs

An arrangement and a method for producing high-purity crystals, such as temperature-sensitive pharmaceutical agents, in a countercurrent crystallization process. The arrangement comprises a plurality of crystallizers, mother liquor lines, each of which has a shut-off valve, and crystallization product lines, each of which has a shut-off valve, so that a mother liquor flow can be generated which is directed from a crystallizer to the second-next crystallizer in the direction of decreasing purity, and a crystallization product flow can be generated which is directed from a to dissolved crystallization product that is about to crystallize to the next crystallizer in the direction of higher purity.

Arrangement and method for producing high-purity crystals

The present invention relates to a method for the reliable and reproducible preparation of 4-[17&#x3b2;-methoxy-17&#x3b1;-methoxymethyl-3-oxoestra-4,9-dien-11&#x3b2;-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

Method for preparing 4-[17&#x3b2;-methoxy-17&#x3b1;-methoxymethyl-3-oxoestra-4,9-dien-11&#x3b2;-yl]benzaldehyde (E)-oxime (asoprisnil)

The process for making crystals of a 11 &#x3b2;-benzaldoxim-estra-4,9-diene derivative having an average particle size of from 3 &#x3bc;m to 25 &#x3bc;m and a maximum particle size of 100 &#x3bc;m, includes subjecting a supersaturated solution containing a special 11&#x3b2;-benzaldoxim-estra-4,9-diene derivative of formula (I) to a wet milling by a wet milling apparatus while crystallizing, In order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described and are part of the invention.

Process for production of crystals of 11&#x3bc;-benzaldoxim-estra-4,9-diene derivatives, crystals obtained thereby and pharmaceutical preparations containing them

The process for making steroid crystals having a predetermined average particle size of from 1 &#x3bc;m to 25 &#x3bc;m and a maximum particle size that does not exceed a predetermined maximum value of 100 &#x3bc;m, includes subjecting a supersaturated solution containing a steroid to a wet milling by wet milling apparatus while crystallizing, in order to obtain a primary particle suspension. Crystals obtained according to this process and pharmaceutical preparations containing them are also described.

Process for production of steroid crystals, steroid crystals obtained thereby and pharmaceutical preparations containing them

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Jena, Germany

Sabine Gliesing