544 results about "Estradiols" patented technology

Drospirenone for Hormone Replacement Therapy A pharmaceutical composition comprising as a first active ingredient an estrogen, such as estradiol or estradiol valerate, in sufficient amounts to treat disorders and symptoms associated with deficient endogenous levels of estrogen in women, and as a second active ingredient 6beta,7beta; 15beta; 16beta-dimethylene-3-oxo-17alpha-preg-4-ene-21,17-carbolactone (drospirenone, DRSP) in sufficient amounts to protect the endometrium from the adverse effects of estrogen is useful for, amongst others, treating peri-menopausal, menopausal and post-menopausal women. This composition may be used for hormone replacement therapy and may be administered as a multi-phased pharmaceutical preparation. This combination therapy may comprise continuous, sequential or interrupted administration, or combinations thereof, of DRSP and estrogen, each optionally in micronized form.

Drug eluting coating compositions are composed of at least one therapeutic agent dispersed in modified, biologically active binders. The therapeutic agents included in the coating composition are paclitaxel, sirolimus, tacrolimus, everolimus, actinomycin-D, dexamethasone, mycophenolic acid, cyclosporins, estradiol, and derivatives and analogs thereof. These therapeutic agents are applied to the surface of the medical device by a modified, biologically active binders. By using these biologically active binders, the therapeutic agents can be applied to at least one surface of a medical implant without using inert polymer carriers.

Described are pharmaceutical compositions comprising at least one steroidal drug such as a progestin (e.g. drospirenone, progesterone, eplerenone, etonogestrel) and / or an estrogen (estradiol and esters thereof) in molecularly dispersed form. The composition comprises a steroidal drug, preferably drospirenone, which is present in the composition in a non-particulate form. Preferably, the drug is present in a dissolved state in the excipient. The molecularly dispersed drug will be released very fast as dissolution takes place instantly when the dosage unit has disintegrated. Also described are methods for preparing the pharmaceutical compositions and methods of using the compositions.

PCT No. PCT / EP96 / 05759 Sec. 371 Date Sep. 14, 1998 Sec. 102(e) Date Sep. 14, 1998 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97 / 23227 PCT Pub. Date Jul. 3, 1997The invention concerns a transdermal patch for the release through the skin of estradiol and a progestogen agent and a process for its production.

A composition of matter is provided having a mixture of active estrogenic compounds. The mixture is present in chemically pure form. The mixture includes salts of conjugated estrone, conjugated equilin, conjugated Δ8,9-dehydroestrone, conjugated 17α-estradiol, conjugated 17α-dihydroequilin, conjugated 17β-dihydroequilin, conjugated 17β-estradiol, conjugated equilenin, conjugated 17α-dihydroequilenin, and conjugated 17β-dihydroequilenin. The mixture also contains the same essential estrogenic compounds present in naturally derived equine conjugated estrogens. Drug products including the composition of matter are also provided, as are methods of using these drug products to treat mammals in need of treatment. Methods of analyzing mixtures containing conjugated estrogens are also provided.

Drug-delivery stents capable of providing release of two or more drugs such as everolimus and estradiol are provided. The stents can be used for treating a disease such as restenosis and vulnerable plaque.

Methods of improving the bioavailability of ethinyl estradiol by orally administering to a patient a solid dosage form containing ethinyl estradiol or prodrug thereof where that dosage form releases at least some of the ethinyl estradiol or prodrug thereof in the oral cavity for absorption through the oral mucosa to treat the patient for a predetermined indication such as, for example, hormone replacement therapy or contraception. The solid dosage forms may be selected from, among others, chewable tablets, fast melt tablets, films, dissolving films, mucoadhesive tablets, lozenges, and chewing gum.

The present invention provides sustained release formulations of estradiol metabolites whereby the in vivo pharmacokinetics are manipulated by a method selected from the group consisting of chemical modification, crystal packing formation, particle size or a combination thereof. Such compositions are useful in the long-term treatment of a wide variety of diseases.

Chronic glaucoma, cataract, ocular and periocular aging are treated and prevented by the administration of agents that affect metabolic subsystems such as (i) mitochondrial bioenergetics, (ii) free radical moderation and glutathione maintenance, (iii) constitutive nitric oxide / endothelin-1 balance, and (iv) calcium wave signaling and associated neuronal excito-toxicity. Included among the agents are tetrahydrobiopterin, R-alpha-lipoic acid, coenzyme Q10, 17 alpha-estradiol, and glutathione.

The present invention provides improved sustained release formulations of estradiol metabolites, including 2-hydroxyestradiol, 2-methoxyestradiol, 4-hydroxyestradiol and 4-methoxyestradiol, useful for therapeutic treatments. The invention also provides methods of producing sustained release forms of estradiol metabolites. The compositions of the present invention include microparticles, nanoparticles, patches, crystals, gels, rods, stints, pallets, discs, lozenges, wafers, capsules, films, microcapsules nanocapsules, hydrogels, liposomes, implants and vaginal rings. Compositions also include formulations for transdermal and intravenous delivery of estradiol metabolites. The present invention provides numerous improvements over previous forms of estradiol metabolites, such advantages including the sustained release of normally short half-life compounds to maintain therapeutic blood levels.

A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17β-estradiol-3-lower alkanoate, most preferably 17β-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17β-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.

A multiphasic method of contraception comprising the steps of sequentially administering to a female of child bearing age a Phase I composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg norethindrone acetate and an estrogen in an amount equivalent to about 5 to about 15 mcg of ethinyl estradiol for about 7 to about 14 days; a Phase II composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 10 to about 25 mcg of ethinyl estradiol for about 14 to about 22 days; a Phase III composition containing a progestogen in an amount equivalent to about 0.3 to about 1.5 mg of norethindrone acetate and an estrogen in an amount equivalent to about 15 to about 35 mcg of ethinyl estradiol for about 20 to about 31 days; and an optional Phase IV composition containing (i) an estrogen in an amount equivalent to about 5 to about 20 mcg of ethinyl estradiol, or (ii) a placebo or a non-steroidal component, or (iii) a combination of (i) and (ii), for about 2 to about 8 days. The ethinyl estradiol equivalent amount of estrogen in each of the successive Phases II and III is at least 5 mcg greater than the ethinyl estradiol equivalent amount of estrogen in the immediately-preceding phase.

A method for preventing or treating a catamenial migrainous disorder in a female subject comprises administering to a vulvovaginal surface of the subject a pharmaceutical composition that is bioadhesive thereto and comprises at least one estrogenic compound in an amount of about 50 μg to about 1000 μg estradiol equivalent per unit dose of the composition. A related method comprises administering to a vulvovaginal surface of the subject a pharmaceutical composition comprising at least one estrogenic compound, wherein upon administration of the composition to the vulvovaginal surface, a decline in serum estradiol concentration during a luteal phase of a menstrual cycle is moderated.

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.

The invention relates to a human mesenchymal stem cell culture medium. According to the culture medium, the basal culture medium comprises the following components based on the final concentration: 1-2g / L of human serum albumin, 5-10mg / L of transferring, 2-8mg / L of fibronectin, 1-4mg / L of laminin, 50g / L of Fe(NO3)3.9H2O, 417g / L of FeSO4.7H2O, 1-3mu g / L of estradiol, 2-5mu g / L of testosterone, 1-3mu g / L of progesterone, 39.25-117.74 mu g / L of dexamethasone, 5-10mg / L of insulin, 376.36mg / L of riboflavin, 80.96-242.87mg / L of coenzyme A, 4.41-6.17mg / L of butanediamine, 1-2mg / L of taurine, 0.61-1.85mg / L of aminoethanol, 8.81-26.42mg / L of pyruvic acid, 3.78-7.56mu g / L of sodium selenate, 292.3-584.6mg / L of L-glutamine, 2-8mu g / L of vascular endothelial growth factor, 4-10mu g / L of epidermal growth factor, 4-10mu g / L of basic fibroblast growth factor, 1-5mu g / L of leukaemia inhibitory factor, 1-5mu g / L of insulin-like growth factor-I and 2-8mu g / L of stem cell factor. The culture medium does not contain the animal serum, the potential animal endogenous endotoxin or virus of the animal serum is eliminated, and the culture medium is conveniently applied to clinics.

The present invention provides an improved method to deliver estrogen to menopausal women comprising administering ultra-low dose estradiol alternating with standard-dose estradiol.

Methods are provided for the treatment of pulmonary hypertension and other conditions associated therewith. In particular, the methods include treatment of pulmonary hypertension with an estradiol metabolite or alkoxy analogue of an estradiol metabolite. The estradiol metabolite or alkoxy analogue thereof may be associated with biodegradable microparticles or nanoparticles alone or in combination with other therapeutic agents. Preferred estradiol metabolites include 2-methoxyestradiol, 4-methoxyestradiol, 2-hydroxyestradiol, and 4-hydroxyestradiol and preferred alkoxy analogues of estradiol metabolites include 2-ethoxyestradiol, and / or to synthetic derivatives and analogues thereof or prodrugs thereof. The compositions may also be in the form of a controlled release formulation.

A blend of at least two polymers in combination with a drug provides a pressure-sensitive adhesive composition for a transdermal drug delivery system in which the drug is delivered from the pressure-sensitive adhesive composition and through dermis when the pressure-sensitive adhesive composition is in contact with human skin.

The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and / or steroid sulphatase enzymes and / or requiring the lowering of the endogenous 17β-estradiol concentration.

According to various embodiments of this disclosure, pharmaceutical compositions comprising solubilized estradiol are provided. In various embodiments, such compositions are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.

The invention relates to a making method and an application of a CdS sensitized TiO2 environmental estrogen photoelectrochemical sensor. The method uses TiO2 as an antigen capture substrate material, a CdS photoelectric active material is in situ generated on the surface of a Cd2<+> functional TiP nanomaterial maker modified electrode through a direct Na2S dropping technology, and CdS is irritated by an LED lamp of visible light wavelength to be converted to a photoelectric current signal. The substrate material TiO2 can be well matched with CdS energy band, so the photocurrent conversion signal of CdS is further improved, thereby the competitive photoelectrochemical immunosensor for ultra sensitive detection of estradiol, estriol, diethylstilbestrol, bisphenol A, nonylphenol, oestrone and other environmental pollutants is made.

Estrogen and progesterone replacement therapies are provided herein. Among others, the following formulations are provided herein: solubilized estradiol without progesterone; micronized progesterone without estradiol; micronized progesterone with partially solubilized progesterone; solubilized estradiol with micronized progesterone; solubilized estradiol with micronized progesterone in combination with partially solubilized progesterone; and solubilized estradiol with solubilized progesterone.

According to various embodiments of this disclosure, pharmaceutical compositions comprising solubilized estradiol are provided. In various embodiments, such compositions are encapsulated in soft capsules which may be vaginally inserted for the treatment of vulvovaginal atrophy.