Dr. Robert Pfleger Chemische Fabrik Gmbh

Dr.r.pfleger Chemische Fabrik Gmbh

Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Dr. R. Pfleger Gmbh

Albert Schaupp

Rolf Sachse

Manfred Stohrer

Ulrich Schwantes

Gerd Jung

Roland Schneider

Sergej Anschütz

Any pharmaceutical preparation for oral administration with controlled release of active ingredient in the small bowel, on the basis of active ingredient carriers provided with at least one active ingredient which are provided with an inner layer to control the release of active ingredient and with a gastro-resistant coating layer disposed thereon, which is characterized in that the inner layer is formed from at least two diffusion layers whose permeability for the diffusing active ingredient decreases from the inside to the outside, and a method for the production thereof, are described.

Pharmaceutical preparation for oral administration with controlled active ingredient release in the small intestine and method for its production

The invention relates to a process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate, as well as the latter product. Endo-nortropine is the key product for the production of important azonia-spironortropanol esters, which are used as pharmaceuticals, particularly spasmolytics. There are three different synthesis methods for the preparation of said intermediate, which lead to different disadvantages. These problems are obviated by the present invention through the two-stage treatment of 8-benzyl-nortropan-3-one perchlorate with catalytically activated hydrogen, the starting product initially being prehydrogenated in aqueous suspension and at atmospheric pressure and ambient pressure with a palladium catalyst, at the end of the reaction the catalyst is recovered by filtration, the filtrate is passed over an anion exchanger and the now alkaline reacting solution is rendered turbulent at 1000 to 1500 r.p.m. with hydrogen activated by Raney nickel at atmospheric pressure and ambient temperature. This new synthesis method using the novel perchlorate salt as an intermediate is extremely economic and environmentally friendly and supplies substantially completely stereoselectively the desired endo-form of nortropine.

Process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate as the intermediate, as well as the latter salt

A process for the production of endotropine by catalytically reducing tropanone with hydrogen with Raney nickel or Raney copper. This process is conducted with tropanone in an aqueous solution absent of organic solvents, in a closed system, at atmospheric pressure and ambient temperature and subject to turbulent action at 1000 to 1500 r.p.m. The process leads to average yields of 94%. The process improves on prior art processes which use an overpressure and organic solvents which involve a high fire and explosion risk.

Process for the production of endotropine

Compositions of the anticholinergic agent trospium chloride suitable for localized administration are provided, in the form of an aqueous solution having a pH-value of.gtoreq.4.5, that is prepared prior to administration. Methods of using the provided compositions for treating dysfunctions of the bladder and the urinary system are also provided. The treatment methods are characterized by the intravesicular administration of the inventive composition into the bladder of a patient in need thereof

Use of trospium chloride and 2-component system for the same

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Strullendorf, Germany

Albert Schaupp