39 results about "Spironolactone" patented technology

The invention relates to the technical field of biological medicine, and particularly discloses application of spirolactone in preparation of a synergist of an immune checkpoint inhibitor. The application finds that spirolactone can enhance the effect of the immune checkpoint inhibitor on treating liver cancer, has no toxic or side effect on animals, and improves the tumor killing ability of infiltrating NK cells. Animal experiments show that the progress of the liver cancer can be remarkably inhibited by combining the spirolactone with the immune checkpoint inhibitor, and the tumor killing capability of infiltrating NK cells can be improved by combining administration, so that the spirolactone can be used as an auxiliary medicine for clinically improving or enhancing the immune checkpoint to treat the liver cancer (HCC).

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 discloses a low-irritation policresulen flushing fluid 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 the policresulen to 55-65 DEG C, and then adding Kinan oil to form a mixture A; s2, quickly stirring the mixture A for 8-15 minutes until the mixture A is dissolved and clarified, then adding spironolactone, uniformly stirring, and cooling to 24-27 DEG C to form a mixture B; and S3, sequentially adding succinic anhydride and water into the mixture B, stirring for 10-20 minutes, filtering with a filter membrane, filling according to specifications, sealing, and carrying out terminal sterilization to obtain the policresulen flushing fluid. The prepared policresulen flushing fluid is good in clarity, low in irritation, high in stability, small in related substance increment, easy and convenient to operate and low in production cost.

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.

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 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 provides a polychlorinated spirolactonization reaction method of a phenolic compound. The polychlorinated spirolactonization reaction method is used for preparing a spirolactone compound. According to the method, 2-(3 '-hydroxyphenyl) benzoic acid and derivatives thereof are used as raw materials, trichloroisocyanuric acid is used as an oxidizing agent and a chlorine source, and the dearomatization polychlorinated spirolactonization reaction of phenolic compounds is realized through one-step operation. The key of the reaction lies in participation of halide, rapid construction of a plurality of C-Cl bonds is promoted, and spirolactone rings are formed through oxygen atom migration. The method is mild in reaction condition, simple and convenient to operate, wide in substrate application range, high in yield and selectivity, safe in preparation, low in cost, suitable for industrial production and capable of meeting the requirements of the market for wide range and large quantity.

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.

The invention discloses a large Stokes shift near-infrared fluorescent probe for detecting Hg < 2 + > as well as a preparation method and bioimaging application of the large Stokes shift near-infrared fluorescent probe. According to the invention, a conjugated system is expanded by introducing a quinoline structure, the emission wavelength is red-shifted to a near-infrared region (730nm), and the Stokes shift is up to 170nm, so that the interference of background fluorescence in bioimaging application can be greatly reduced. In the process of identifying Hg < 2 + > by the probe, S atoms in a sulfo-spirolactone structure are promoted to be combined with Hg < 2 + > to form HgS by virtue of the high sulfur-loving characteristic of Hg < 2 + >, so that a spirolactone ring is opened and fluorescence is generated. The probe has the advantages of fast response time (3s), low detection limit (53nM) and specific recognition capability on Hg < 2 + >. The fluorescent probe disclosed by the invention has relatively good biocompatibility and relatively low cytotoxicity, and can be applied to evaluating the drug effect of a mercury poisoning antidote in a 4T1 cell model and monitoring the change of the Hg < 2 + > level in an acute mercury poisoning mouse model in real time.

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 belongs to the technical field of medicine, and discloses a sparsentan crystal form, a preparation method thereof and a pharmaceutical composition, the crystal form is a crystal form A, and X-ray powder diffraction of the crystal form A has characteristic peaks at diffraction angles 2theta of 7.1 + / -0.2 degrees, 12.5 + / -0.2 degrees, 12.8 + / -0.2 degrees, 14.1 + / -0.2 degrees, 15.7 + / -0.2 degrees, 16.8 + / -0.2 degrees, 18.6 + / -0.2 degrees, 20.5 + / -0.2 degrees and 21.4 + / -0.2 degrees. According to the present invention, by reasonably designing the first solvent, adjusting the pH value of the system, the subsequent good solvent and / or poor solvent, the temperature and the time of cooling crystallization, and the like, the new sparsentan crystal form A is obtained, the purity of the obtained product is high, the product is in the crystalline state, and the stability is significantly improved. By adopting the crystallization method, the operation is simple, the amplification is easy, the production cost is greatly reduced, and the efficiency is greatly improved.

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 invention relates to a cell stress pulse detection ultrafast fluorescent probe group and application thereof, belongs to the field of organic fluorescent probes, and provides specific micromolecular fluorescent probes C1 and T1 for detecting Cu < 2 + > and tyrosinase of CSP, the probe C1 is designed based on a specific recognition group of Cu < 2 + >, and the probe T1 is designed based on an active cavity structure of tyrosinase and a specific recognition group of the tyrosinase. All the compounds have ultrafast response speed, excellent light stability, good pH stability and anti-interference ability to other ions and amino acids in cells. After the probe C1 reacts with Cu < 2 + >, a lactam spiro ring is opened to emit strong near-infrared fluorescence, similarly, after the probe T1 reacts with tyrosinase, a spirolactone ring is opened, and a near-infrared fluorescence signal is remarkably enhanced. The probe C1 and the probe T1 can specifically and rapidly detect the Cu < 2 + > content and the tyrosinase activity in vitro, and CSP detection is achieved by monitoring the changes of Cu < 2 + > and tyrosinase in cells under the stress condition in real time.

The invention provides a composition for preventing and treating heart diseases caused by pulmonary arterial hypertension and a functional preparation containing the composition. The composition comprises pimobendan, enalapril, torasemide and spirolactone, and can effectively prevent and treat animal heart diseases and pulmonary arterial hypertension.

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 present invention relates to an orodispersible tablet comprising spironolactone or pharmaceutically acceptable salts thereof, at least one diluent, a disintegrant, a binder, a solubilizer, a lubricant, and one or more pharmaceutically acceptable excipients. The orodispersible tablet of spironolactone or pharmaceutically acceptable salts thereof is formulated for acceptable palatability and taste-masking of the bitter drug, thereby enhancing patient compliance, especially among pediatric and geriatric individuals with dysphagia. The orodispersible tablet of spironolactone is manufactured by the wet granulation method to provide a faster disintegration and dissolution rate of said tablet.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a spirolactone composition for treating alopecia as well as a preparation method and application of the spirolactone composition. The spirolactone composition for treating alopecia is characterized by being prepared from the following raw materials in percentage by mass: 0.5 to 5 percent of spirolactone, 38 to 45 percent of ethanol, 10 to 15 percent of glycerol, 2 to 5 percent of hydroxypropyl chitosan and 32 to 47.5 percent of purified water. The spirolactone composition prepared by the invention is small in irritation, safe and free of toxic and side effects, and has a wide application prospect.