Jenapharm Gmbh & Co. Kg

Bayer Intellectual Property Gmbh

Jenapharm Gmbh

Other

Lts Lohmann Therapie-systeme Ag

Otto Bock Pur Lifescience Gmbh

Bayer IP Gmbh

Entec Gesellschaft Fuer Endokrinologische Technologie M.b.h.

Bayer Schering Pharma Ag

Michael Dittgen

Michael Oettel

Sabine Fricke

Carsten Timpe

Thomas Langguth

Dirk Schenk

Hagen Gerecke

Herbert Hoffmann

Siegfried Golbs

Thomas Graser

Detlef Grawe

Stefan Bracht

Petra Huber

Jan-Peter Ingwersen

Hubert Kaffl

Stephan Mletzko

Holger Zimmermann

Claudia Moore

Doris Hubler

Christoph Luderschmidt

Jochen Schumacher

Monika Ostertag

Manfred Suesse

Christoph V&ouml;lkel

Walter Elger

Markus Krumme

Birgitt Schneider

Guenter Kaufmann

Keith Jensen

Peter Gansen

Peter Hoesel

Hermann Osterwald

Kai K&ouml;pke

Sascha General

Annette Eichardt

Peter Moellmann

Michael Ernst

Ralf Ladwig

Kathrin Ahrens

Theodor Hermann Lippert

Thomas Gr&auml;ser

Ines-Patricia M&ouml;ller

Sven Claussen

Manfred Boese

Doris Huebler

Jochen Schuhmacher

Juergen Henze

Christian Schulte

Ingeborg Steinfatt-Hoffmann

Albert Radlmaier

Klaus Matthey

Drik Schenk

Jürgen Henze

The invention relates to a pharmaceutical composition in the form of a system in film form for transmucosal administration of steroid hormones. An administration system for steroid hormones which dissolves in the mouth and which releases with a high bioavailability is disclosed. The administration system in film form dissolves in the mouth preferably in a period of less than 30 min, and the steroid hormone entering the bloodstream transmucosally from the administration system leads to a rapid rise in the concentration in the blood. It is thus possible to achieve a maximum concentration of this steroid hormone in the blood in a period of less than 60 min after administration.

Wafer comprising steroid hormones

The invention relates to a UV stable transdermal therapeutic system (TTS) consisting of a back layer, at least one matrix containing an active substance and optionally, a withdrawal film and an UV-radiation absorber. An adhesive layer containing said UV-radiation absorber is arranged between the back layer and the matrix containing an active substance which is distant as much as possible from a surface, a separation layer is arranged between the adhesive layer containing said UV-radiation absorber and the matrix containing an active substance, which is as remote as possible from the surface which is impermeable to the active substance and UV-radiation absorber. The inventive transdermal therapeutic system exhibits a high stability and is devoid of inconveniences of existing TTS containing a light-sensitive substance.

UV stable transdermal therapeutic plaster with a UV absorbing self-adhesive layer separated from the drug matrix

The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.

Transdermal delivery of hormones with low concentration of penetration enhancers

Transdermal delivery of hormones without the need of penetration enhancers

A method for producing an active substance-containing polyurethane plaster for transdermal application is described, said plaster containing at least one active substance at a highly accurate declared dose. In the described method, a solvent-free active substance-containing polyurethane is produced by reactively coating a solvent-free active substance-containing polyurethane material (), which is mixed in a coating unit () immediately before or during the application process, onto an elastic backing foil () that has been rendered non-extensible at least in the direction in which the applied polyurethane material is processed by means of a supporting, adhering auxiliary foil () which is at least mono-axially non-extensible.

Polyurethane plaster for the transdermal application of active substances, and method for the production thereof

The invention relates to a UV stable transdermal therapeutic system (TTS) consisting of a back layer, at least one matrix containing an active substance and, optionally, a withdrawal film and an UV-radiation absorber. An adhesive layer containing said UV-radiation absorber is arranged between the back layer and the matrix containing an active substance which is distant as much as possible from a surface, a separation layer is arranged between the adhesive layer containing said UV-radiation absorber and the matrix containing an active substance, which is as remote as possible from the surface which is impermeable to the active substance and UV radiation absorber. The inventive transdermal therapeutic system exhibits a high stability and is devoid of inconveniences of existing TTS containing a light-sensitive substance.

UV stable transdermal therapeutic plaster with a UV absorbing adhesive layer separated from the drug matrix

The method of making a bioadhesive tablet for controlling testosterone blood level, especially in elderly men suffering from partial androgen deficiency, includes spray-drying an alcoholic solution or suspension of testosterone and at least one testosterone ester, preferably in a ratio of 1:10 to 1:1.5, separately or together, with an organic polymer and optionally one or more auxiliary ingredient to form an active ingredient premix. Then various other auxiliary ingredients are mixed, as needed, with the active ingredient premix to form the bioadhesive tablet with an active ingredient layer and an adhesive layer. The active ingredient layer contains an effective amount of the active ingredient premix. The adhesive layer includes auxiliary ingredients including the bioadhesive polymer. The bioadhesive tablet may be buccally administered to provide a predetermined timed release profile of testosterone, advantageously varying according to a circadian rhythm.

Bioadhesive tablet containing testosterone/testosterone ester mixtures and method for producing a predetermined testosterone time-release profile with same

The combination preparation for contraception includes from 2 to 4 first stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient, from 16 to 22 second stage daily dosage portions each including an effective amount of a combination of at least one natural estrogen and at least one natural or synthetic gestogen as active ingredient; from 2 to 4 third stage daily dosage portions each including an effective amount of at least one natural estrogen as sole active ingredient; and from 2 to 4 final stage daily dosage portions containing a pharmaceutically acceptable placebo. The estrogen may be estradiol, an estradiol compound that is metabolized to estradiol when taken into the body, a conjugated equine estrogen or a phytoestrogen. The natural or synthetic gestogen can be natural progesterone or a synthetic gestogens, such as medroxyprogesterone acetate.

Combination preparation for contraception based on natural estrogens

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

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 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 pharmaceutical composition, especially for treating skin with seborrhea,,and androgonically conditioned alopecia, contains a hormonal agent including the gestogen, dienogest, or a combination of dienogest and an estrogen, as active ingredient. Methods for treatment of this type of skin condition include topical application of the composition including the dienogest which results in an outstanding sebosuppression, a drastic reduction of androstandiol glucuronide and a moderate competitive blockage of androgen receptor sites. Galenic formulations are described which limit and/or prevent the permeation of the active ingredient through the skin. The pharmaceutical preparation including the dienogest and conventional dermatologically acceptable carrier and auxiliary substances in the described galenic formulation advantageously provides a drastic reduction in androstandiol glucuronide and moderate androgen receptor blockage without passing through the skin barrier so that systemic effects including side reactions are substantially prevented.

Hormonal agent for skin treatment

The use of melatonin for the production of peroral pulsatile forms of medications assures the safeguard of an effective level of the medical substance of melatonin in the blood, and which realize a relatively short invasion phase with a controlled delivery in comparison to conventional forms of medication containing melatonin, and which simultaneously exclude the known side effects. A control of the delivery of the melatonin is effected which is associated with the precise adaptation to the illness episodes or the pain attacks of certain illnesses, which can be treated prophylactically and therapeutically with the active agent melatonin.

Melatonin for the production of a peroral pulsatile form of medication

The combination preparation for contraception includes a first stage of 2 to 4 first stage daily dosage portions, a second stage of two groups of second stage daily dosage portions, a third stage of 2 to 4 third stage daily dosage portions and an additional stage of 2 to 4 additional stage daily dosage portions. The first stage daily dosage portion is an effective amount of natural estrogen, the second stage daily dosage portion is an effective amount of a combination of natural estrogen and natural or synthetic gestogen, the third stage daily dosage portion is another effective amount of natural estrogen and an additional stage daily dosage portion consists of a placebo. The first group of the second stage consists of 3 to 5 daily dosage portions and the second group, 13 to 17 daily dosage portions. More of the gestogen is included in the effective amount in the second group of the second stage than in the first group. The effective amount of the natural estrogen is constant in both the first and third stages, but smaller in the third stage than in the first stage.

Combination compound for contraception based on natural estrogen

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

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Apolda, Germany

Michael Dittgen