Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Jesalis Pharma Gmbh

Bayer Pharma Aktiengesellschaft

Bayer Schering Pharma Ag

Hapila Gmbh

Detlef Grawe

Sabine Gliesing

Peter Hoesel

Hagen Gerecke

Robert Eilers

Uwe Mueller

Michael Dittgen

Carsten Timpe

Annette Eichardt

Gabriele Winter

Michael Sander

Bernd Erhart

Thomas Michel

Holger Zimmermann

Herbert Hoffmann

Ulf Tilstam

Jochen Schumacher

Harald Raethe

Peter Moellmann

Ulf Bohlmann

Dieter Wehmeier

Peter Hosel

Uwe Knabe

Uwe Muller

Michael Mosebach

Barbara Schmidt

David Voigtlaender

Wilfried Fischer

Jürgen Jacke

Klaus Matthey

Klaus Bahl

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 invention relates to novel solid body forms of mesoprogestin 11&#x3b2;-[4E-(hydroxyiminomethyl)-phenyl]-17&#x3b1;-methoxymethyl-17&#x3b2;-methoxy-estra-4,9-dien-3-one (oxime J 867), particularly a highly pure and stable amorphous or highly crystalline form (ansolvate/anhydrate) of compound J 867. The invention also relates to methods for producing said novel solid body forms and to the use thereof in pharmaceutical compositions. The novel solid body forms are characterized by exhibiting a high degree of stability. The solid body forms of oxime J 867 can, in particular, be used in the area of fertility control and in hormone replacement therapy.

Solid body forms of mesoprogestin 11&#x3b2;-{4E-(hydroxyiminomethyl)-phenyl}-17&#x3b1; methoxymethyl-17&#x3b2;-methoxy-estra-4,9-dien-3-one

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

The method of isolating an anhydrous etidronate disodium particulate includes preparing a liquid-liquid dispersion consisting of an aqueous-organic phase and an etidronate-disodium-salt-containing aqueous phase; adjusting a temperature of the liquid-liquid dispersion to between 0 and 30&#xb0; C. and intensely agitating so that a coarse-particle fraction precipitates from the liquid-liquid dispersion, then drawing off a fine-particle suspension and allowing a fine-particle fraction to precipitate from it and filtering and drying the coarse particle fraction. In a preferred embodiment the fine-particle fraction is separated from the fine-particle suspension for recycling The resulting anhydrous etidronate disodium particulate has a grain size of from about 0.1 to 1 mm and a bulk density of 0.4 to 0.6 g/cmwith good properties for pharmaceutical applications.

Method for isolating pharmaceutically exploitable etidronate disodium

The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.

Laminates containing an active substance transdermal system

A homogeneous steroid-containing preformulation for production of solid and semi-solid pharmaceutical preparations containing a uniform constant dosage of at least one steroid in a range from 0.001 to 1 percent by weight is described. This steroid-containing preformulation contains of from 0.001 to 50 percent by weight of the at least one steroid. The homogeneous steroid-containing preformulation is made by a method including dissolving the at least one steroid in a solvent to form a dispersant; dispersing an adjuvant consisting of adjuvant particles in the dispersant in a mass ratio of the adjuvant to the at least one steroid of,to 1000:1 to form a suspension; and creating a spray-mist of the suspension so as to evaporate and remove the solvent from the suspension and thus to form a dried particulate which includes steroid-containing particles. The droplets in the spray mist have a droplet diameter greater than a mean diameter of the adjuvant particles. The maximum particle size of the dried particulate forming the steroid-containing preformulation is increased by less than 30 percent in comparison to an average particle size of the adjuvant particles.

Homogeneous preformulations containing high concentrations of steroids, for producing low-dose solid and semi-solid pharmaceutical preparations

This invention relates to a bioadhesive tablet containing at least one bioadhesive adjuvant and at least one lubricant, with at least one surface of the tablet comprising concentric or parallel, straight and/or curved depressions, and to a method for producing the bioadhesive tablets as well as to pharmaceuticals in the form of the bioadhesive tablets.

Bioadhesive tablet

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Kleinromstedt, Germany

Detlef Grawe