Schering Aktiengesellschaft

Bayer Intellectual Property Gmbh

Bayer Schering Pharma Ag

Bayer Pharma Aktiengesellschaft

Torsten Wagner

Ralph Lipp

Adrian Funke

Werner Skuballa

Helmut Dahl

Christian Zurth

Heinrich Michel

Martin Wessel

Kristina Mueller

J&uuml;rgen Westermann

Bernd Iffert

Methods for improving solubility and bioavailability of lipophilic compounds are described. Particularly, described are stabilized supersaturated solid solutions, particularly in power from, of lipophilic drugs, such as steroidal molecules.

Stabilised supersaturated solids of lipophilic drugs

The present invention relates to oral solid dosage forms containing a very low dose of estradiol. The dosage forms are formulated in a manner so as to avoid degradation of the estradiol and to minimise the content of polyvinylpyrrolidone, while still achieving similar fast dissolution of the estradiol. The dosage forms are useful in preventing or treating a physical condition in a woman caused by insufficient endogenous levels of estradiol.

Oral solid dosage forms containing a low dose of estradiol

A process for the production of encased, spherical granular grains comprising spraying grains which consist of a prostane derivative and a cyclodextrin vehicle, forming together a prostane-cyclodextrine-clathrate, with an aqueous polymer dispersion of ethyl cellulose and/or poly(methyl)acrylic acid ester in a fluidized or boiling bed is disclosed. The polymer dispersion is applied in a thickness equivalent to 1-5% (w/w) of the total mass of the encased grains. The coated grains are cured for at least 24 hours. Grains produced according to this method have a pharmaceutical active ingredient release profile which remains unchanged over the storage time.

Method for producing encased spherical granular grains

The invention relates to the use of an oxidation inhibitor, i.e. active carbon, for ambient air in industrial manufacturing, especially in the processing of prostane derivatives, whereby the oxidation inhibitor removes ozone from the process air before contact with said prostane derivatives. The concentration of decomposition products is reduced.

Oxidation inhibitors in prostane derivatives

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Berlin, Germany

Torsten Wagner