99 results about "Dihydrotestosterone" patented technology

A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and / or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies of skin and hair. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes affecting skin and hair.

A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and / or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and / or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and / or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.

The invention discloses a testosterone detection reagent based on a microparticle chemiluminescence immunoassay technology; the testosterone detection reagent comprises the following components: 0.002%-0.01% of paramagnetic microspheres, 0.4 mug / ml-1 mug / ml of acridinium ester labeled testosterone antibodies, a composite testosterone release agent, a luminescence liquid A, a luminescence liquid B, 0ng / dl-1500ng / dl of a testosterone calibrator and a cleaning fluid with a certain concentration; and the testosterone release agent is a mixture of dihydrotestosterone, danazol and heparin sodium. The testosterone detection reagent has the advantages of simple operation, high sensitivity, fast detection efficiency, low cost, easy automation and the like, and by combination of the selected composite release agent and different binding globulin, combined-state testosterone in serum can be fully released, so that the content detection of total testosterone is more accurate.

The present invention describes a composition that contains a plant sterol or plant stanol or their fatty acid esters and an emulsifier for treating conditions that are related to elevated dihydrotestosterone. The compositions can be prepared in a dry form for use as a food ingredient, tablet or capsule. Alternatively, the compositions can be dissolved in oil.

The composition of the invention relates generally to a nutritional supplement, which is capable of ameliorating the biologically detrimental effects of dihydrotestosterone (DHT). The present composition comprises a combination of natural plant-derived extracts, and minerals including Saw palmetto berry extract; pumpkin seed (Curcubito pepo) extract; beta-sitosterol; quercetin; Polygonum multiflorum root extract; a lycopene, for example from tomato extract; isoflavones, for example from Pueraria lobata root extract, and soybeans; zinc; selenium or any combination thereof. The ingredients are combined into any suitable form to be administered, and consumed by an individual for the prevention or treatment of hair loss, or prostatic hyperplasia or both.

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies of skin and hair. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes affecting skin and hair.

The invention provides a new synthetic method of finasteride, belonging to the technical field of drug synthesis. The method comprises the following steps of: a. synthesis of dihydro finasteride iodo complex; and b. synthesis of finasteride; the synthesis method can transform dihydrotestosterone finasteride (F9) into the finasteride with a theoretic volume, avoids the use of harmful and toxic chemicals which are sensitive to the environment, has the advantages of total two-step reaction yield of more than 90%, purity of over 99.0%, good product yield, high purity, easy refining, simple operation, low cost, and less three-waste, conforms with the requirements of green chemical synthesis, and can achieve the requirements of high yield, high purity, green cleaning and industrial production of the finasteride.

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.

A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and / or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and / or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and / or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

The isoflavone equol has the ability to mimic estrogen at the receptor level, as well as the ability to mitigate the deleterious effects of dihydrotestosterone (DHT) in vivo, thus resulting in potential health benefits for both men and women. Only an approximated one-third of the global population has the inherent ability to produce equol. Diet and colonic bacterial composition play a large role in natural equol production. The present invention can increase the probability of producing significant quantities of equol in vivo. Experimentation has shown the repeatable and measurable evidence of equol. Data from male test subjects indicates clinically significant positive effects on androgenic alopecia and acne vulgaris.

Chimeric polypeptides comprising a dihydrotestosterone (DHT) reductase moiety, such as 3 alpha-hydroxysteroid dehydrogenase (3α-HSD), fused to a signal peptide moiety, polynucleotides encoding same, and compositions comprising at least one microorganism cell capable of secreting the chimeric polypeptide, are provided. Further provided are methods and kits for treating, preventing or ameliorating androgen-dependent disorders, including but not limited to androgenic alopecia.

The present invention provides an external preparation of dihydrotestosterone. The preparation contains 0.01 percent to 5 percent of the dihydrotestosterone by weight percentage in a medicinal carrier of the preparation uniformly; wherein, the medicinal carrier is selected from solution, suspension, lotion, gel, ointment, cream, paste and patch. The preparation can remedy the primary, the secondary and the senile hypogonadism, the prostatic hyperplasia, the gynaecomastia and the lichen sclerosis et atrophicus. The medicated part can be arm, shoulder, inner thigh, chest, abdomen and genitalia.

The invention belongs to the technical field of testing or analyzing substances by measuring chemical or physical properties, and discloses a model for distinguishing between androgen and antiandrogeneffects of a substance, and a construction method and application thereof. The model for distinguishing between androgen and antiandrogen effects of the substance adopts a Surflex-Dock program of theSYBYL to dock a ligand into an AR. The model is established by binding mode of dihydrotestosterone (DHT) and hydroxyflutamide (HFT) with AR, and is further used in a novel brominated flame retardant;after the simulation is ended, the agreement between the antagonist-bound H12 helix and other structures is significantly weakened, so that the stability of the H12 helix is reduced, but the agonistcan maintain the stability of H12; and the method can be used to initially screen the agonism and antagonism of the substance.

The invention belongs to the field of skin-care products, and provides a whitening, acne-removing, blackhead-removing and anti-aging composition, and an application and a preparation thereof. The composition provided by the invention has whitening, acne-removing, blackhead-removing and anti-aging efffects, can inhibit the expression of inflammatory factors, namely IL-1 and TNF-a at the same time,reduces the effect of androgen dihydrotestosterone, and has the advantages of no drug resistance and no side effect compared with hormone for treatment.

The invention relates to a method for determining dihydrotestosterone in a medicine through a derivatization HPLC method. The method comprises the steps that (1) a benzoyl halide compound is used as aderivatization reagent to carry out derivatization reaction on dihydrotestosterone in a medicine to be tested to acquire a sample containing a dihydrotestosterone derivatization product; and (2) a test solution is prepared by using the sample containing the dihydrotestosterone derivatization product, and the test solution is detected by high performance liquid chromatography, wherein the detectorof the high performance liquid chromatography is an ultraviolet detector. According to the invention, the method for determining dihydrotestosterone through derivatization HPLC-UVD is simple and versatile, and can be used for the determination of the medicine content in dihydrotestosterone preparations; and a methodology validation result shows that the method has the advantages of specificity, good sensitivity and high accuracy.

The invention discloses a recipe for treating androgenetic alopecia, a liquid shampoo and an application method for the recipe. The recipe comprises, by weight, 41 to 50% of potassium azeloyl diglycinate, 6 to 12% of water-soluble hesperidin, 1.6 to 9% of vitamin C and 1.2 to 6.3% of vitamin B. The application method for the recipe comprises the following steps: mixing the recipe with deionized water according to a mass ratio of 0.8-1.2: 9; heating a mixture obtained in the previous step to 40 DEG C and carrying out isothermal stirring for 10 min; and carrying out natural cooling to room temperature under stirring. When used as an external 5a-reductase inhibitor, the recipe provided by the invention can reduce dihydrotestosterone in scalps and hair follicles and improve and strengthen 5a-reductase inhibitory effect; through cooperation with vitamin B, absorption and action of vitamin B are improved, and potassium azeloyl diglycinate has improved 5a-reductase inhibitory effect; and cooperation between methyl hesperidin and vitamin C can improve the blood flow volume of capillary vessels in scalps, is beneficial for hair growth and exerts same effect as minoxidil.

The invention discloses a composition for inhibiting the activity of 5 alpha-reductase. The composition comprises lycopene, curcumin and aromatic turmerone. Researches find that compared with a singleplant extract and a model control group, the composition disclosed by the invention can obviously inhibit the activity of the 5alpha-reductase, reduces the dihydrotestosterone content in animal tissues and serum, obviously induces the activity reduction of benign prostatic hyperplasia cells and human prostatic hyperplasia epithelial cells, obviously induces the proliferation of human sebaceous gland cells, obviously promotes the proliferation of human papilla dermal cells, and has an obvious synergistic interaction effect on the prevention and treatment of prostate diseases, androgenic alopecia or acne and other androgenic diseases. The plant extract composition provided by the invention is efficient and free of toxic and side effects, and has important application value in prevention andtreatment of androgen diseases..

The invention provides a method for detecting five androgens in serum. The method comprises the following steps of: mixing a serum sample to be detected with an internal standard solution, adopting amixed extraction solvent, obtaining detection liquid through liquid-liquid extraction pretreatment, and detecting the detection liquid by adopting an ultra-high performance liquid chromatography-tandem mass spectrum technology. The ultra-high performance liquid chromatography conditions are as follows: mobile phase A is 0.1% formic acid aqueous solution, and mobile phase B is 0.1% formic acid methanol solution. The mass spectrum conditions are as follows: a positive ion mode, namely a mass spectrum scanning mode of multi-reaction monitoring; and five androgens, which are dehydroepiandrosterone, testosterone, androstenedione, dihydrotestosterone, and androsterone. The method of the invention has the advantages that the detection time for simultaneously detecting five androgens is only fiveminutes, and the detection flux is large; the operation is simple and convenient, and the time consumption is less; and the method has the advantages of strong specificity, high sensitivity, high precision, low detection limit, wide detection range and wide practical application prospect.

An improved hair color formulation treats hair to provide volume, viscosity, color and hair follicle stimulation. The color formulation is appointed to be used in hair products, and comprises a natural color agent and at least one agent providing anti-dihydrotestosterone (DHT) effects. Hair products include styling products, cleansing products, concealment products, and dying products. In one embodiment, the formulation comprises an aqueous emulsion, at least one hydrocarbon, at least one thickening agent, at least one humectant, at least one emollient, at least one fatty acid ester, and at least one agent providing anti-dihydrotestosterone (DHT) effects, such as caffeine, and at least one color agent. Preservatives, fibers and further treatments for male / female pattern baldness may also be added to the composition. Natural colorants are added to the hair color formulation to provide temporary coloring in addition to enhanced volume, viscosity and hair follicle stimulation.

A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and / or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

The invention relates generally to the use of anti-sense oligonucleotides, small interfering RNA, and ribozymes to modulate expression of the human steroid 5α-reductase gene and thereby modulate levels of dihydrotestosterone (DHT). Elevated levels of DHT are associated with various disorders including, but not limited to, skin diseases, hair loss, hirsuitism, and benign prostatic hyperplasia. The invention specifically relates to formulations of these anti-sense oligonucleotides, small interfering RNA, and ribozymes for administration to treat and prevent disorders

The present disclosure describes compositions for preparing a myofiber or myotube from a skeletal muscle stem cell or progenitor cell comprising a carnitine and / or a derivative thereof, a fatty acid a steroid and combinations thereof. Preferred embodiment comprises of 0,1 mM L-carnitine, 0.2 mM 9-cis-linoleic acid and 10 mM dihydrotestosterone. Also disclosed is a composition for inducing expansion of skeletal muscle stem cells or progenitor cells comprising a fibroblast growth factor agonist, a Notch signalling agonist, a nucleic acid, and combinations thereof. Preferred embodiment comprises 20 ng / ml basic fibroblast growth factor (bFGF), 50 [mu]g / ml [Delta]-like ligand 1 (DLL1), 10 mM hypoxanthine and 1.6 mM thymidine.

Provided is a pharmaceutical composition, a health food composition, or a quasi drug composition for preventing, treating, or improving a disease caused by overproduction of dihydrotestosterone, including fucoxanthin or a Phaeodactylum tricornutum extract as an active ingredient.

The invention discloses a steroid hormone detection method that comprises the following steps: adding an internal standard substance into a sample to be detected; carrying out a derivatization reaction; detecting an analyte by using chromatography tandem mass spectrometry; the analyte comprises a first steroid hormone and a second steroid hormone at the same time; the first steroid hormone is selected from at least one of the following steroid hormones: estradiol and estriol; and the second steroid hormone is selected from at least one of the following steroid hormones: dehydroepiandrosterone,dehydroepiandrosterone sulfate, testosterone, dihydrotestosterone, androstenedione, cortisol, cortisone, 11-deoxycortisol, 17alpha-hydroxyprogesterone, 17alpha-hydroxypregnenolone, aldosterone, cortisol, deoxycortisol, progesterone and pregnenolone. The detecting method has the advantages of few operation steps and short detection time, and can specifically, sensitively, accurately and quantitatively analyze the analyte substance.

The invention provides the use of an extract of a plant of the genus Elephantorrhiza and at least one compound selected from quercitin-3′-O-glucoside, trans-3-O-galloyl-3,3′,5,5′,7-pentahydroxyflavan, taxifolin-3′-O-glucoside, catechin and epicatechin in the preparation of a medicament for the treatment of benign prostatic hyperplasia (BPH). The mode of action is by a route selected from blocking the conversion of testosterone to dihydrotestosterone by inhibiting the 5α-reductase enzyme or by reducing oxidative stress or both.

The invention dislcoses application of crocetin in preparation of a drug or a health care product for preventing and treating polycystic ovarian syndrome. On the basis of the existing effects of the crocetin, a foetal period dihydrotestosterone-induced polycystic ovarian syndrome mouse model is adopted to deeply research therapeutic action of the crocetin. Results show that the crocetin can remarkably relieve estrous cycle dysrhythmia of a polycystic ovarian syndrome model mouse, reduce ovary weight and an atresia ovary amount, increasing amounts of corpora lutea big antral follicles and follicles before ovulation, and remarkably improve levels of estradiol, luteinizing hormone, follicle-stimulating hormone, progesterone and testosterone of the polycystic ovarian syndrome model mouse, andhas a good effect of treating the polycystic ovarian syndrome. Moreover, in an experiment process, obviously untoward effects do not appear, and the safety is high.