24 results about "Spironolactone" patented technology

The invention relates to the technical field of biological medicine, and discloses a preparation method and application of a novel spironolactone derivative based on intestinal fungus biotransformation, and the method comprises the following steps: S1, screening an intestinal fungus Syncephalasetum monosporium as a transformation strain; s2, carrying out in-vitro fermentation culture on the screened strains; s3, extracting metabolites in the fermentation liquor; s4, identifying and separating the novel spirolactone derivative by combining mass spectrometry and a chromatographic separation technology; and S5, verifying the aldosterone receptor antagonistic activity of the derivative through molecular docking simulation. A novel spirolactone derivative is identified and separated through strain screening, fermentation condition optimization, multi-stage purification and mass spectrometry and chromatographic separation technologies, the enzyme activity of the strain is activated through shake culture in a culture medium to promote metabolism, the product purity is improved through inactivation, extraction and chromatographic purification, and the problems that a product is single and low in purity in a traditional method are solved.

The invention provides a sustained-release medicinal preparation for preventing and treating alopecia as well as a preparation method and application of the sustained-release medicinal preparation, and belongs to the technical field of biological medicines. The medicine for preventing and treating alopecia is prepared from the following components: 1 to 2.5 mg of finasteride, 4 to 6 mg of minoxidil, 20 to 60 mg of spirolactone, 10 to 20 mg of isotretinoin, 3 to 8 mg of vitamin B5, 50 to 100 mg of zinc and 5 to 10 mg of vitamin b6. The components cooperate with one another to activate hair follicle stem cells, increase the number of hair follicles and synergistically enhance the ability of promoting hair regeneration, so that a better alopecia prevention and treatment effect is achieved; the pharmaceutical preparation prepared by selecting a specific filler, an adhesive, a sustained-release framework material and a lubricant in a reasonable proportioning range has good sustained-release performance, the dosage and frequency of the medicine are greatly reduced, and the side effect is far lower than that of an oral medicine in a common dosage form.

The invention relates to a material in the field of medical supplies, in particular to an easy-to-desorb wound dressing with controllable adhesion, near-infrared light response and antioxidant and antibacterial properties and a preparation method of the easy-to-desorb wound dressing. The wound dressing is of a double-layer integrated hydrogel structure, the upper layer is a photo-thermal hydrogel layer with near-infrared light response and constant-temperature photo-thermal performance, and the wound dressing is formed by compounding and curing core-shell microspheres containing spironolactone photo-thermal molecules, GelMA and PEGDA; the lower layer is a controllable adhesion hydrogel layer based on lipoic acid and is formed by curing components such as LA / LANa, GelMA and NIPAm. The wound dressing can achieve stable constant-temperature photo-thermal antibacterial treatment under irradiation of near-infrared light, meanwhile, the adhesion strength of the wound dressing can be regulated and controlled through temperature, the wound dressing can be firmly attached to a wound surface in the using process, mild and low-damage desorption is achieved during replacement, and the wound dressing has good antibacterial performance, oxidation resistance and biocompatibility and is suitable for being used in the field of medical treatment. The device is suitable for safe treatment and nursing of infected wounds.

The present invention provides a combination comprising niclosamide and spironolactone for use in the treatment of diseases caused by RNA virus in a subject in need thereof. The present invention further provides a combination comprising niclosamide and spironolactone for simultaneous, separate, or sequential use.

The invention relates to a cyclic preparation method of a spirolactone key material, and belongs to the technical field of medicines. According to the method, resource utilization is carried out on a byproduct compound 2 generated in the production process of a spirolactone intermediate 1, and the byproduct compound 2 is converted into a spirolactone key material compound 1 under the acidic condition. The reaction is carried out in an organic solvent or an aqueous medium, the acidic aqueous solution is selected from hydrochloric acid, sulfuric acid, trifluoroacetic acid, acetic acid, nitric acid or phosphoric acid, the concentration range is 0.1-6 mol / L, the reaction temperature is 0-100 DEG C, the reaction time is 0.5-96 hours, and the feeding molar ratio of the compound 2 to the acid is 1: 0.5-1: 10. The organic solvent can be selected from ethers, alcohols, esters or haloalkanes. The obtained compound 1 can be used as a raw material for preparing spirolactone, and a final product is obtained through an oxygen bridge reaction, an esterification reaction, a decarboxylation reaction, an etherification reaction, a dehydrogenation reaction and a thioation reaction. The method provided by the invention realizes cyclic utilization of production byproducts, improves the utilization rate of raw materials, reduces the production cost, reduces waste discharge, and has a good industrial application prospect.

There are provided a composition for preventing and treating heart disease due to pulmonary hypertension, and a functional preparation containing the same. The composition includes pimobendan, enalapril, torsemide, and spironolactone, and is thus effective in preventing and treating heart disease and pulmonary hypertension of animals.

The invention relates to the technical field of traditional Chinese medicines, and particularly discloses a traditional Chinese medicine formula for treating haemorrhoids and a preparation method thereof. The formula comprises ephedra, semen brassicae, cinnamon, rhizoma zingiberis, antler slices, bombyx batryticatus, smoked plum, catechu, golden cypress, coix seeds, peach kernels, snakegourd seeds, sanguisorba officinalis, hairyvein agrimony, radix angelicae, purslane, red halloysite, dragon's blood, gallnut, andrographolide extract and carboxymethyl pachymaran, and preferably comprises sophora flowers and fructus aurantii. The preparation method comprises the following steps: firstly, carrying out physical field auxiliary activation on animal and mineral medicinal materials in the formula, carrying out synergistic aging on high-tannin medicinal materials, and carrying out co-crushing pretreatment on sophora flowers and fructus aurantii; carrying out alternating magnetic field assisted dynamic countercurrent extraction on the pretreated medicinal materials; carrying out membrane separation and refining on an extracting solution, and carrying out oriented assembly on the refined extracting solution, an andrographolide extract and carboxymethyl pachymaran; and finally carrying out programmed molding according to the requirements of oral solid preparations or decoctions. The composition can be used for treating haemorrhoids, and has the advantages that multiple components have a synergistic effect, and related symptoms of the haemorrhoids can be conditioned in a targeted manner.

The invention relates to a hypertension implant rod and a preparation method thereof, and relates to the technical field of hypertension implant rods, the hypertension implant rod comprises a quick release layer, a slow release layer and a long-acting regulation and control layer from outside to inside, the quick release layer comprises, by mass, 60-70% of bacterial cellulose (BC), 15-25% of polydopamine (PDA), 3-8% of ciprofloxacin, 3-8% of protamine and 4-6% of indapamide, the slow release layer comprises, by mass, 20-30% of a long-acting regulation and control layer, and the long-acting regulation and control layer comprises, by mass, 20-30% of a slow release layer and 20-30% of a long-acting regulation and control layer. The sustained release layer is prepared from 55 to 65 percent of polylactic acid-glycolic acid copolymer, 20 to 30 percent of cross-linked gelatin, 8 to 12 percent of lacidipine and 4 to 6 percent of spirolactone, and the long-acting regulation and control layer is prepared from 65 to 75 percent of L-polylactic acid, 20 to 30 percent of beta-glycine crystal, 3 to 5 percent of silk fibroin (SF), 0.5 to 1.0 percent of calcitonin gene related peptide CGRP and 0.1 to 0.3 percent of neuropeptide Y. The hypertension implant rod can be matched with various treatment cycles through gradient degradation, realizes'on-demand treatment ', is high in biocompatibility, is suitable for subcutaneous implantation, and is convenient and safe to operate.

The present invention relates to an aqueous ophthalmic composition comprising spirolactone, cyclodextrin and tromethamine, preferably for topical application to the human eye. The present inventors advantageously dissolve spirolactone in the HP-gamma cyclodextrin excipient at a concentration of 0.1%, which dose has been demonstrated to be effective in the treatment of ocular surface defects. They also have successfully demonstrated that the spirolactone eye drops are stable for up to 9 months at 4 DEG C and achieve its efficacy within at least 6 months, and the formulation is well tolerant after multiple daily instillations within 7 days. In addition, the spirolactone eye drops provided by the invention accelerate healing of corneal wounds of rats, reduce corneal edema and inflammation, enhance epithelial integrity and improve nerve regeneration, and prompt recovery of corneal homeostasis. Thus, the invention also relates to the use of an aqueous ophthalmic composition for the treatment of ocular diseases and disorders.

The invention relates to the technical field of pharmaceutical preparations. The invention provides a sustained-release capsule containing minoxidil and dutasteride and a preparation method of the sustained-release capsule, the sustained-release capsule is composed of a capsule shell and content, and the content comprises minoxidil, dutasteride, spirolactone, isovitamin A, a traditional Chinese medicine composition, a sustained-release material, a filling material, an adhesive, a lubricant, a traditional Chinese medicine solubilizing dispersant and a stabilizer. According to the sustained-release capsule, through the synergistic effect of chemical components and traditional Chinese medicine components, the medicine components are better and more stable, the duration time of the medicine effect is prolonged, and the side effects of hirsutism, edema and the like caused by minoxidil and the side effects of transaminase abnormality and the like caused by dutasteride are reduced; meanwhile, by means of the liver protecting and blood nourishing effects of the traditional Chinese medicine components, the liver metabolism pressure is better reduced, and the long-term medication safety is improved; the hair regeneration capability is enhanced, and a better alopecia prevention and treatment effect is achieved.

The invention relates to a traditional Chinese medicine composition for treating psoriasis, which is prepared from the following traditional Chinese medicines in parts by weight: 5-25 parts of cornu bubali, 5-25 parts of purslane, 5-25 parts of radix curcumae, 1-20 parts of radix isatidis, 1-20 parts of rhizoma dryopteris crassirhizomae, 1-20 parts of fructus forsythiae, 1-20 parts of rhizoma smilacis glabrae, 1-20 parts of fructus gardeniae and 1-20 parts of raw flos sophorae. The traditional Chinese medicine composition comprises, by weight, 1-20 parts of Chinese trumpet creeper, 1-20 parts of artemisia apiacea, 1-20 parts of folium mori, 1-20 parts of roasted rhizoma atractylodis macrocephalae and 1-10 parts of radix sophorae flavescentis. The traditional Chinese medicine composition is based on the traditional Chinese medicine theory, aims at the core pathogenesis of the psoriasis blood-heat syndrome, is rigorous in formula and clear in monarch, minister, assistant and guide, can remarkably improve the skin lesion symptom of progressive psoriasis, and is small in side effect and good in patient compliance.

The application discloses a kind of external use traditional Chinese medicine preparation for treating cold blood stasis type granulomatous lobular mastitis and preparation method, and external use traditional Chinese medicine preparation is made of the raw materials including the following medicinal materials: prepared rhizome of rehmannia, antler slice, cassia, gunpowder ginger, chuanxiong, safflower, golden cypress, radix angelicae pubescentis, spironolactone, white and so on.The external preparation formula of the application is warm and blood tonic, blood-activating and skin-regenerating, has better clinical effect of treating cold blood stasis type granulomatous lobular mastitis, can effectively reduce the size of mass in clinical test, improve patient life treatment score, reduce the pain of patient, and has greater popularization and application value.

Disclosed are methods, compositions, and kits for treating pediatric cancers using hydroxyureamethyl acylfulvene (LP-184) or pharmaceutically acceptable salts / solvates thereof. The methods include monotherapy and combination regimens for pediatric sarcoma, medulloblastoma, glioma (including DIPG), hepatoblastoma, Wilms tumor, and related malignancies. Combination therapies include LP-184 with vincristine, topoisomerase I poisons (topotecan or irinotecan), PARP inhibitors (e.g., rucaparib), or spironolactone, yielding additive or greater-than-additive reductions in tumor growth or cell viability.

The present disclosure provides methods for treating or alleviating symptoms of a disease, disorder, or condition related to excess androgen or stress-induced skin changes in a subject in need thereof by topically administering a pharmaceutical composition comprising a pharmaceutically effective amount of spironolactone to the subject. Other aspects relate to methods for providing anti-oxidative stress, anti-inflammatory and anti-aging benefits for the skin to a subject in need thereof by topically administering a pharmaceutical composition comprising a pharmaceutically effective amount of spironolactone to the subject. Surprisingly, it has been found that spironolactone may be topically administered with reduced adverse effect compared to systemic administration of the same medication.

A method for the treatment or prevention of the symptoms or effects of hair loss of an animal which comprises treating the animal with a therapeutically effective amount of a combination comprising 7α-Acetylthio-17α-hydroxy-3-oxopregn-4-ene-21-carboxylic acid γ-lactone or a physiologically functional derivative thereof, N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide or a physiologically functional derivative thereof, 17β-(N-tert-butylcarbamoyl)-4-aza-5α-androst-1-en-3-one or a physiologically functional derivative thereof, and 2,4-pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide or a physiologically functional derivative thereof. A pharmaceutical formulation comprising the same. A patient pack comprising at least one active ingredient selected from 7α-Acetylthio-17α-hydroxy-3-oxopregn-4-ene-21-carboxylic acid γ-lactone or a physiologically functional derivative thereof, N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide, 17β-(N-tert-butylcarbamoyl)-4-aza-5α-androst-1-en-3-one, and 2,4-pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide, and an information insert containing directions on the use of all three active ingredients together in combination.

The present application provides a dandruff-removing and itching-relieving essence liquid with anti-inflammatory and antibacterial effects, and relates to the field of cosmetics.The present application provides an essence liquid, components of which comprise spironolactone, 1,2-hexanediol, ethanol, propylene glycol, butanediol, p-hydroxyacetophenone, citric acid, sodium citrate, pyridoxine hydrochloride, sophora alkaloid, menthol lactate, PEG-40 hydrogenated castor oil, dipotassium glycyrrhizinate, sodium hyaluronate, essence and quaternary ammonium salt-73; the essence liquid has significant anti-inflammatory and itching-relieving effects when used for scalp care, and also has antibacterial and dandruff-removing effects, and has great application potential in the field of cosmetics.

Pharmaceutical compositions for the topical administration of spironolactone to the pilosebaceous unit and methods for administering the same. The pharmaceutical compositions comprise aqueous suspensions of submicron particles of spironolactone in water.

The invention relates to the technical field of biotransformation, and discloses a method for generating a novel antihypertensive metabolite through intestinal fungus mediated spirolactone biotransformation, and the method comprises the following steps: S1, screening a fungus strain with spirolactone transformation capability from intestinal microbiota; s2, carrying out biotransformation on spirolactone by using the screened fungus strain to obtain a transformed product; s3, separating and purifying the converted product; s4, identifying a metabolite structure in the converted product by adopting a mass spectrum-assisted structure mining technology in combination with a spectral analysis method; and S5, evaluating the potential antagonism of the metabolite on the aldosterone receptor through a molecular docking technology. According to the invention, intestinal fungus screening, biotransformation, separation and purification, structural identification and molecular docking technologies are integrated into a systematic method, so that the problems of low discovery efficiency and high synthesis cost of novel compounds caused by a chemical synthesis path adopted by most traditional drug development are improved.

The application discloses a low-irritation policresulen flushing solution and a preparation method thereof, and relates to the technical field of pharmaceutical preparations.The preparation method comprises the following steps: S1, pouring policresulen into a container, heating to a temperature of 55-65 DEG C, and then adding karanja oil to form a mixture A; S2, rapidly stirring the mixture A for 8-15 min until it is dissolved, then adding spironolactone, uniformly stirring, and reducing the temperature to 24-27 DEG C to form a mixture B; S3, sequentially adding succinic anhydride and water to the mixture B, filtering after stirring for 10-20 min, and performing filling, sealing and terminal sterilization according to specifications, so that the policresulen flushing solution is obtained.The policresulen flushing solution prepared by the application has the advantages of good clarity, low irritation, high stability, less increase of related substances, simple operation, and low production cost.

The invention relates to the technical field of microbial conversion, and discloses a mass spectrum-assisted structure mining method for converting conehead monospora into spirolactone, which comprises the following steps: S1, screening intestinal fungus strains with spirolactone bioconversion capability through high performance liquid chromatography; s2, carrying out in-vitro fermentation on spirolactone by utilizing the concephalosporium monosporum, and carrying out acetonitrile inactivation and ethyl acetate extraction to obtain fermentation liquor containing metabolites; s3, identifying the metabolites by adopting an HPLC-MS / MS technology; s4, performing separation and structure verification on the metabolite in S3 by combining preparative high performance liquid chromatography and nuclear magnetic resonance technology; and S5, evaluating the binding capacity of the metabolite and an aldosterone receptor through a molecular docking technology, and screening the metabolite with potential antagonistic activity. The concephalosporium monosporum is determined to be a strain for efficiently converting the spirolactone through HPLC (High Performance Liquid Chromatography) screening, and various metabolites including three unreported novel metabolites are generated in the conversion process, so that a candidate compound library is enriched.

The application discloses a kind of acne-removing compositions, including Baiji, Huanglian, dandelion, spironolactone, borneol, alisma, purple flower diting, baiyan, the effective component extract of composition formed by white yam;Wherein the weight ratio of each component is: Baiji 10.0~12.0%, Huanglian 3.0~4.5%, dandelion 14.0~16.0%, spironolactone 14.0~16.0%, borneol 7.0~8.5%, alisma 7.0~8.5%, purple flower diting 14.0~16.0%, baiyan 14.0~16.0%, white yam 10.0~12.0%.The application compared with prior art has the advantages that: provide a kind of acne-removing compositions capable of repairing damaged skin, suitable for a variety of external preparation forms and preparation method and application.

The application discloses a kind of acne-removing compositions and its application on solid-state flash-release soluble microneedle, belong to daily-use cosmetics technical field.The acne-removing composition comprises 10-13 parts of dihydrofarnesic acid, 1-4 parts of spironolactone extract, 0.3-1 parts of yeast / zinc fermentation product and 2.0-2.6 parts of hamamelis virginiana extract by mass fraction, wherein the hamamelis virginiana extract is prepared by compound fermentation of cellulomonas huizhi and bacillus subtilis, secondary fermentation of streptomyces thermophilus and ethanol reflux extraction, and the utilization rate of active ingredients is high;The composition provided by the application can significantly inhibit lipid synthesis through the synergistic effect of multiple components, and effectively reduce the level of inflammatory factors.The composition is loaded in solid-state flash-release soluble microneedle, which can quickly dissolve and release active ingredients when used, achieve the effect of quickly removing acne, anti-inflammatory and detumescence, and has good safety without irritating reaction.

The invention discloses an acne-removing composition and application thereof to a solid-state flash-release soluble microneedle, and belongs to the technical field of daily cosmetics. The acne-removing composition is prepared from the following components in parts by mass: 10-13 parts of dihydroquecolic acid, 1-4 parts of a herba portulacae extract, 0.3-1 part of a saccharomycetes / zinc fermentation product and 2.0-2.6 parts of a witch hazel extract, and the witch hazel extract is prepared by carrying out compound fermentation on wet cellulomonas and bacillus subtilis, carrying out secondary fermentation on streptomyces thermophilus and carrying out ethanol reflux extraction. The active ingredient utilization rate is high; according to the composition provided by the invention, through the synergistic effect of multiple components, the synthesis of grease can be remarkably inhibited, the level of inflammatory factors is effectively reduced, the composition is loaded in a solid flash-release soluble microneedle, the composition can be quickly dissolved and release active ingredients during use, the effects of quickly removing acnes, resisting inflammation and diminishing swelling are achieved, and meanwhile, the composition is good in safety and free of irritant reaction.