Abstract: 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.

Abstract: The transdermal system includes a sex hormone-containing adhesive matrix, which contains inclusions of a sex hormone in a hydrophilic non-crosslinked polymer in dissolved or dispersed form. The inclusions have a concentration of 20 to 90 percent by weight of the sex hormone, which is more than 50 percent by weight amorphous. The hydrophilic non-crosslinked polymer can be polyvinylpyrrolidone, methylcellulose, ethylcellulose or hydroxyethylcellulose. The adhesive matrix can be a polyisobutylene, ethylene-vinyl-acetate copolymer or a polystyrene-butadiene block copolymer.

Abstract: 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.

Abstract: The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds. The compounds according to the invention have a hybrid-type profile of action in the sense that they act as inhibitors of 5?-reductase and simultaneously as gestagens. They are therefore suitable for treating diseases that are the result of elevated androgen levels in certain organs and tissues in men and women. Together with other hormonal substances, such as an estrogen, testosterone or a strong androgen, the compounds according to the invention are suitable as contraceptive agents for women and for men.

Abstract: A biodegradable, injectable oligomer-polymer composition is described, which consists of a combination of at least two biologically degradable inert materials and at least one biologically active ingredient. The inventive, oligomer-polymer composition coagulates when injected into the body of a mammal and forms an implant, from which the biologically active ingredient is released. The rate of release can be adjusted by controlling the type and amount of the ingredients of the oligomer-polymer composition.

Abstract: Described are novel equilenin derivatives of general formula I methods for producing the same and medicaments containing these compounds. The new compounds have antioxidative activity and are usable for geroprophylaxis in women and men.

Abstract: The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount of a chemically modified derivative of 17&agr;-estradiol, a chemically modified derivative of 17&bgr;-estradiol and/or a chemical modified derivative of estriol. Pharmaceutical preparations containing 14&agr;, 15&agr;-methylene-1,3,5(10),8-tetraene-3,17&agr;-diol are particularly preferred.

Abstract: The method of treating or preventing a disease in a human male or a male animal caused by a decreased production of androgens, such as testosterone, in the human male or male animal includes administering an effective amount of a glucocorticoid receptor antagonist to the human male or the male animal in order to increase production of the androgens. These diseases include male sexual dysfunction, infertility and hypogonadism. Novel androgen receptor antagonist compounds and methods of synthesis are also described.

Abstract: A method of administering dienogest to a women in high dosages for reducing the body of the breast is described. The dosage should be at least ten times the effective dosage for inhibiting ovulation in the women. A pharmaceutical composition for use in the method is also described. Furthermore, retrogression of mastopathic changes in the body of the breast can be brought about. Dienogest is also outstandingly suitable for the prophylaxis of mastopathies. In high dosages, dienogest prevents the formation of mastopathic changes in the body of the breast.

Abstract: The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formula R—SO2—O— at their C3 position wherein R is a R1R2N group wherein R1 and R2 are independent of each other and represent a hydrogen atom, a C1-C5 alkyl radical or, together with the N atom, a polymethylene imino radical containing 4 to 6 C atoms, or a morpholino radical. The preparations according to the invention can be used for hormonal contraception and for hormon replacement therapy (HRT). They exhibit a low hepatic estrogenity.

Abstract: Described are new, unsaturated 14,15-cyclopropano-androstanes of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are characterized by hormonal (gestagenic and/or androgenic) activity and may be used for hormone replacement therapy.

Abstract: This invention relates to new 19-nor-17&agr;-pregna-1,3,5(10)-trien-17&bgr;-ols with a 21,16&agr;-lactone ring of formula II, 1

Abstract: New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, especially for administration in post-menopausal women and in men. The compounds of the invention can also inhibit aromatase and sulfatase.

Abstract: Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical preparations that contain these compounds. The compounds are distinguished by hormonal (gestagenic and/or androgenic) activity.

Abstract: Thiol esters of S-substituted 11&bgr;-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula I their pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical preparations containing these compounds are described. These compounds bind to progesterone receptors and have distinctly reduced anti-glucocorticoid action.

Abstract: 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.

Abstract: 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 1:1 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.

Abstract: 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.

Abstract: Pharmaceutical preparations containing selected steroid compounds and methods of treating estrogen deficiency in the central nervous system (CNS) without influencing other organs or systems are described. These steroids have selective neurotropic estrogen-like transcription action in contrast to the systemically acting natural and synthetic estrogen compounds, such as 17&agr;-estradiol. The selected steroids surprisingly have a selective influence on the transcription estrogen-dependent gene in the CNS and cause changes of physiological parameters as well as CNS-specific transcription effects in the dosages used with no biological effects in reproductive system tissues. They have CNS specific transcription effects at those dosages at which neither 17 &bgr;-estradiol nor 17&agr;-estradiol had any action and the transcription estrogen-dependent gene in the CNS is not influenced by secondarily formed 17&bgr;-estradiol.

Abstract: 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.