Schering Aktiengesellschaft

Jenapharm Gmbh & Co. Kg

Other

Bayer Pharma Aktiengesellschaft

Hagen Gerecke

Michael Dittgen

Detlef Grawe

Sabine Fricke

Sabine Gliesing

Peter Hoesel

Uwe Mueller

Annette Eichardt

Christoph V&ouml;lkel

Peter Hosel

Uwe Muller

Carsten Timpe

Michael Sander

Bernd Erhart

Thomas Michel

Kai K&ouml;pke

Robert Eilers

Ulf Tilstam

Ulf Bohlmann

Dieter Wehmeier

Uwe Knabe

Ines-Patricia M&ouml;ller

Kathrin Ahrens

Michael Mosebach

David Voigtlaender

Jürgen Jacke

Klaus Bahl

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

This invention relates to an in-situ implant that can be produced by placing a sterile, injectable, and water-insoluble complex from a biodegradable polymer and a biocompatible polyether with functional end-groups in the organism, and coagulating them under the influence of the body fluid. This coagulate may optionally contain at least one bioactive substance selected from the group of hormones, immunomodulators, immunosuppressants, antibiotics, cytostatics, diuretics, gastro-intestinal agents, analgesics, local anaesthetics and/or neuropharmacological agents.

Injectable implant

The invention relates to a transdermal therapeutic system for application to the skin and/or mucosa consisting of at least one active substance in the form of a solid dispersion in combination with at least one destructuring agent and/or at least one structuring agent in a common matrix.

Transdermal compositions with enhanced skin penetration properties

The method of making a solid drug with controlled effective ingredient delivery for oral administration includes selecting a predetermined number of at least three of four compressed compositions containing an effective ingredient or effective ingredient combination defined by their release profile of effective ingredient and/or effective ingredient combination. The solid drug or medicinal preparation is formed according to known methods requiring only comparatively small apparatus expense and minimal time. Perorally administered solid drugs are made by this process which can provide widely varying pharmaceutically-required release profiles of effective ingredients or effective ingredient combinations, for example delayed release, uniformly maintained release or pulsatile release adjusted to fit a special rhythm.

Method of making a perorally administered solid drug with controlled

Growing community of inventors

Jena, Germany

Hagen Gerecke