Jenapharm Gmbh & Co. Kg

Jenapharm Gmbh

Peter Moellmann

Sven Ring

Michael Dittgen

Sigfrid Schwarz

Detlef Grawe

Bernd Undeutsch

Peter Hoesel

Carsten Timpe

Bernd Erhart

Harald Raethe

Klaus Matthey

Gisela Weber

Gerhard Teichmueller

Hans-Joachim Palme

Carmen Pfeiffer

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

The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel). Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.

Steroid intermediate products and method of their production

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Jena, Germany

Peter Moellmann