51 results about "Conjugated estrogen" patented technology

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.

A pharmaceutical preformulation in the form of a solid, free-flowing dry extract of a natural mixture of conjugated equine estrogens, which is particularly suitable use in for solid galenic forms, e.g. tabletting. The conjugated estrogens are available for further galenic processing in a form which assures the chemical stability of the hormones and permits advantageous processing into solid galenic forms, for example a tablet. The invention furthermore relates to a method for producing these preformulations in the form of a dry extract.

Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w / w of a cellulose ingredient, and less than about 50% w / w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w / w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40° C. and about 75% relative humidity for about 2 months.

The present invention is directed to pharmaceutical vaginal cream compositions comprising a conjugated estrogen and a stabilizer. The present invention is also directed to a method of treating a menopausal condition in a female in need thereof, said method comprising vaginally administering a pharmaceutical vaginal cream composition comprising a conjugated estrogen twice per week for at least 2 weeks.

The present invention is directed to monophasic pharmaceutical compositions comprising a conjugated estrogen and a hydrophilic or lipophilic excipient. The present invention is also directed to kits and applicators comprising the pharmaceutical compositions. The invention is also directed to methods for treating menopausal conditions in a female comprising administration of the pharmaceutical compositions.

The present invention relates to compositions containing unconjugated estrogens and methods of their use in the treatment of conditions associated with hypoestrogenism or reduced estrogen levels in females.

The present invention relates to solid dosage formulations containing conjugated estrogens and bazedoxifene, or a salt thereof. In some embodiments, the compositions include a core comprising conjugated estrogens, and at least one coating that comprises bazedoxifene, or a salt thereof.

A pharmaceutical matrix film tablet with controlled release of natural mixtures of conjugated estrogens which have been obtained from the urine of pregnant mares.

A slowly releasing conjugated oestrogen composition for preventing and treating femal climacteric syndrome, osteoporosis and coronary heart disease and male senile dementia is composed of slow-releasing layer and core containing conjugated oestrogen and progestogen.

The invention provides a pharmaceutical composition for treating polycystic ovary syndrome (PCOS). The pharmaceutical composition consists of a traditional Chinese medicine composition and chemical drugs, wherein the traditional Chinese medicine composition comprises the medicinal materials such as anemarrhena, fritillary bulb, tortoise plastron, fleece-flower root, lilyturf root, hippocampus andthe like; and the chemical drugs comprise one or more compound molecules of dexamethasone, spirolactone, ethinyloestradiol, estradiol valerate, conjugated estrogen and pharmaceutically acceptable salt. The pharmaceutical composition has the advantages of reducing the level of androgens and androgen receptors of patients suffering from PCOS, improving the level of sex hormone-binding globulin (SHBG), lowering the level of free testosterone (F-TESTO), further raising the level of in-vivo estrogens, improving growth and development of follicles and increasing ovulation rate and pregnancy rate ofthe patients.

The present invention is directed to pharmaceutical vaginal cream compositions comprising a conjugated estrogen and a stabilizer. The present invention is also directed to a method of treating a menopausal condition in a female in need thereof, said method comprising vaginally administering a pharmaceutical vaginal cream composition comprising a conjugated estrogen twice per week for at least 2 weeks.

The invention relates to the technical field of chemical detection, and provides a method for rapidly detecting the content of conjugated estrogens in pregnant mare urine by utilizing near infrared spectroscopy. Aiming at different conjugated estrogen components, a quantitative analysis and correction model of each conjugated estrogen is established by adopting a partial least square method through preprocessing and selecting characteristic spectral bands. Compared with an HPLC (high performance liquid chromatography) method, the near infrared spectroscopy provided by the invention is simpler,more convenient and quicker to operate, is suitable for content determination of large-batch samples, can meet the requirements on large-scale sample information acquisition in industrial production,and has important significance on the drug production process and stability controllability of a terminal product. Results of the embodiment show that the method provided by the invention is relatively high in detection accuracy, relative deviation between a predicted value obtained by adopting the method provided by the invention and a real value is less than 15%, and accuracy is relatively high.

The present invention relates to a method for obtaining a natural mixture of conjugated estrogens from urine of pragnant mares (PMU) and use of a macroporous adsorption resin in the method. The method for obtaining a natural mixture of conjugated estrogen from PMU includes the steps of pretreating raw PMU; adsorbing the natural mixture of conjugated estrogens contained in PMU with a macroporous adsorption resin; washing the macroporous adsorption resin laden with the mixture of conjugated estrogens with an alkaline aqueous solution; and eluting the washed adsorption resin with an eluting agent to obtain the mixture of conjugated estrogens. The macroporous adsorption resin is a styrene-divinylbenzene semipolar macroporous adsorption resin with ester group structure. The method according to the invention solves the problems of low adsorptive capacity and high cost existed in the conventional methods, and is suitable for large-scale production.

The invention provides sugar-containing compositions suitable for use in coating solid preparations such as tablets, pills, granules and grains. Methods of using such coatings are provided, as are solid dosage forms coated with the compositions. In some embodiments, the methods provide sugar coated tablets comprising conjugated estrogens, and a progestin, for example medroxyprogesterone acetate.

The present invention relates to a nucleic acid aptamer molecule that includes a domain that binds to an estrogen receptor, molecular complexes that include the nucleic acid aptamer molecule and an estrogen receptor, and constructed DMA molecules and expression systems, as well as host cells, that the contain an RNA aptamer molecule of the invention. Use of these aptamers and encoding constructs to inhibiting estrogen receptor activity in a cell and to treat estrogen receptor-positive cancers is also described.

A method for obtaining an extract from a natural mixture of conjugated estrogens from the urine of pregnant mares (PMU) by solid-phase extraction on semipolar adsorption resins in which the resulting extract meets the pharmaceutical specifications for conjugated estrogens and the content of free estrogens is minimized even if old pregnant mares' urine and / or pregnant mares' urine which has been stored or transported at elevated temperatures is used.

The invention relates to a natural pregnant mare conjugated estrogen purification and refinement method and application of a nonionic nonpolar fine separation resin used by the same. The method comprises the following steps: 1. adsorbing an initial liquid containing a pregnant mare conjugated estrogen crude extract by using a nonionic nonpolar fine separation resin; and 2. eluting the nonionic nonpolar fine separation resin carrying the conjugated estrogen mixture by using an eluting solvent to obtain the purified and refined conjugated estrogen mixture liquid. Compared with the prior art, the purity of the conjugated estrogen prepared by the method is up to 42.6-61.8%, and the total conjugated estrogen yield is 90.8-97.2%; and the conjugated estrogen has no peculiar smell and obviously lighter color (fine light yellow), which is very important for preparing the high-quality conjugated estrogen active pharmaceutical ingredient and preparation products. The method has the advantages of simple technique and high refinement efficiency, and is especially suitable for large-scale production.

This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and / or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and / or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, conjugated estrogens, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

The invention provides monoclonal antibodies that bind the estrogen receptor α (ER α) when phosphorylated at serine 118 (Ser118) in the N-terminal domain, but do not bind to ER α when not phosphorylated at this site. Also provided are methods for determining the phosphorylation of ER α in a biological sample, profiling ER α activation in a test tissue, and identifying a compound that modulates phosphorylation of ER α in a test tissue, by using the disclosed monoclonal antibodies. The sample or test tissue may be taken from a subject suspected of having cancer, such as breast cancer. Kits comprising the phospho-ER α (Ser118) monoclonal antibodies of the invention are also provided.

Oral conjugated estrogen formulations are disclosed and described. In one aspect, the oral formulation may be a tablet having a core and one or more coatings thereon. In addition to conjugated estrogen ingredients, the core may include one or more organic excipients and one or more inorganic excipients. In one aspect, the organic excipients may include less than about 20% w / w of a cellulose ingredient, and less than about 50% w / w of a sugar ingredient. In another aspect, the inorganic excipients may include less than about 10% w / w of a calcium phosphate tribasic ingredient. In yet another aspect, the formulation does not crack when stored at about 40° C. and about 75% relative humidity for about 2 months.

The present invention is directed to monophasic pharmaceutical compositions comprising a conjugated estrogen and a hydrophilic or lipophilic excipient. The present invention is also directed to kits and applicators comprising the pharmaceutical compositions. The invention is also directed to methods for treating menopausal conditions in a female comprising administration of the pharmaceutical compositions.

The invention relates to the technical field of chemical detection, and provides a method for detecting the content of conjugated estrogens in pregnant mare urine. Carbonate in the pregnant mare urinecan form neutral salt, water and carbon dioxide gas when encountering inorganic acid; the column efficiency is improved, so that the problems that 30 samples cannot be measured each time, the columnpressure is increased, the column efficiency is reduced and the like when the content of conjugated estrogens in pregnant mare urine is measured by HPLC can be solved, the measurement accuracy of thesample content is ensured, and reliable data is provided for production. The pH value is adjusted to 7.0-8.0 by using an alkaline substance because: a, the existence state of bound estrogen is relatively stable under an alkaline condition; b, the pH value of the pregnant mare urine is about 7.5-8.5, and the pH value of the pregnant mare urine is adjusted to be slightly alkaline (7.0-8.0), so thatthe pregnant mare urine is closer to the original conditions of the pregnant mare urine; and c, the authenticity and the reproducibility of a detection result have advantages when the sample is slightly alkaline.

The invention discloses novel applications of ritonavir, and metabolite thereof and / or a metabolite derivative and / or a structural analogue of ritonavir as an estrogen receptor modulator. An inhibition effect of ritonavir to tumor cells is partially depended on an estrogen receptor. Ritonavir down-regulates protein expression level and gene transcription level of an alpha subtype estrogen receptor of the tumor cells; ritonavir inhibits F promoter activity of the alpha subtype estrogen receptor; interactive experiments of rotonavir and the alpha subtype estrogen receptor-ligandb inding domain demonstrate that ritonavir is a selective antagonist of the alpha subtype estrogen receptor, belongs to the estrogen receptor modulator, and can bind the estrogen receptor and modulate transcription and expression level of the estrogen receptor, thereby generating effects of inhibiting growth of the tumor cells and increasing cell mortality rate. Reposition of conventional drugs can reduce risks and reduce research cost. The drug is expected to be used for preparing tumor-treating drugs for drug resistance and chemotherapy resistance of conventional antitumor drugs.

A method for obtaining an extract containing the natural mixture of conjugated equine estrogens in which a mixture of conjugated estrogens obtained by solid-phase extraction from pregnant mares' urine is depleted in phenolic urine contents and in non-conjugated lipophilic compounds selected from the group consisting of non-conjugated flavonoids, non-conjugated isoflavonoids, non-conjugated norisoprenoids, non-conjugated steroids, in particular androstane and pregnane steroids, and comparable non-conjugated compounds.

A method for obtaining an extract containing the natural mixture of conjugated equine estrogens in which a mixture of conjugated estrogens obtained by solid-phase extraction from pregnant mares' urine is depleted in phenolic urine contents and in non-conjugated lipophilic compounds selected from the group consisting of non-conjugated flavonoids, non-conjugated isoflavonoids, non-conjugated norisoprenoids, non-conjugated steroids, in particular androstane and pregnane steroids, and comparable non-conjugated compounds.

This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and trimegestone.

The present invention discloses a selective modulator of a human estrogen receptor alpha36 subtype, and a use of the selective modulator in preparation of drugs for prevention and treatment of diseases caused by estrogen receptor abnormality. According to the present invention, the selected compounds can be selectively bound with the estrogen receptor alpha36 subtype in theory; experiment results confirm that: the compounds can activate the ERK channel, inhibit the cancer cell cycle, and initiate apoptosis through the estrogen receptor alpha36 subtype so as to provide inhibition effects for cancer cells, wherein the cell growth inhibition activity of the compounds is superior to the cell growth inhibition activity of a variety of the currently-researched selective modulators of the estrogen receptor alpha36 subtype; and with the skeleton diversity of the compounds, the target compound has advantages of broad transformation space, synthetic route choice and the like, and the application prospects are broad.

The invention discloses a molecular compound of 17 beta-estradiol and vitamin C as well as a preparation method and application thereof. The molecular compound is formed by compounding 17 beta-estradiol molecules and vitamin C in a molar ratio of 0.25: 1, 0.5: 1, 0.75: 1, 1: 1, 1: 0.25, 1: 0.5 or 1: 0.75. The invention further provides a method for preparing the molecular compound of 17 beta-estradiol and vitamin C. The molecular compound of 17beta-estradiol and vitamin C provided by the invention can be distributed to bone tissues in a bone targeting manner, so that not only the anti-osteoporosis activity of 17beta-estradiol is remarkably improved, but also the side effects of hyperplasia endometrii and thrombosis caused by treating with 17 beta-estradiol and conjugated estrogens can be effectively avoided.