49 results about "Indometacin" patented technology

The invention discloses a phlebitis treatment gel containing a coptis chinensis-wine-treated rhubarb compound component and a preparation method of the phlebitis treatment gel. The active ingredients of the gel are coptis chinensis, rheum officinale and wine-treated rheum officinale in a mass ratio of (1.5-2.5): (1.5-2.5): 1, preferably 2: 2: 1. Lavender essential oil, tea tree essential oil, folium eucalypti essential oil and vinegar frankincense, radix trichosanthis and other traditional Chinese medicine auxiliary materials are used as auxiliary materials. The preparation method comprises the following steps: extracting twice with ethanol, mixing extracting solutions, adding borneol, menthol and essential oil, and finally gelling with carbomer. The phlebitis gel can be independently used or combined with indometacin to form dual-channel anti-inflammation, and the defects of skin atrophy, toxicity accumulation and the like of traditional phlebitis gel are overcome. The traditional Chinese medicine composition is clinically expanded and applied to first-stage pressure sores (without skin damage), acnes and mosquito bites, red and swollen of the first-stage pressure sores fade away within 3-5 days, red and swollen of the acnes are relieved by more than or equal to 60% when the traditional Chinese medicine composition is combined with oral medicine for 48 hours, the itching relieving effect on the mosquito bites is less than or equal to 30 minutes, and the curative effect on phlebitis is remarkably superior to that of 50% magnesium sulfate (Plt;

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an anti-inflammatory analgesic indometacin long-acting suppository and a preparation method thereof.The suppository is composed of indometacin sustained-release microspheres and a modified fatty matrix; eudragit RS100 / RL100 is used as a compound framework of the sustained-release microspheres, the sustained-release microspheres are prepared through a spherocrystal granulation process, the modified fatty matrix is prepared from a mixed fatty glyceride compound matrix sustained-release aid, a three-dimensional suspending dispersant and the like through melting, pre-crystallization and high-speed homogenization processes, and the three-dimensional suspending dispersant contains modified nano silicon dioxide, glycerin monostearate and beewax. According to the invention, a microsphere-matrix dual controlled release system is constructed, so that burst release of drugs is eliminated, and long-acting stable release is realized; the microspheres are prevented from settling and agglomerating through a physical locking mechanism, and the storage stability of the preparation is improved by matching with a dual anti-oxidation system; meanwhile, rectal mucosa stimulation is reduced, the preparation process is simple, the quality is controllable, and the composition is suitable for anti-inflammation and analgesia of various diseases and has a wide clinical application prospect.

Described are synthetic compounds having anti-inflammatory properties and optionally analgesic properties. These compounds are derivatives of FDA-approved anti-inflammatory, such as ibuprofen and indomethacin, and can be formed using reactions under microwave irradiation. Generally, the compounds contains a moiety of the parent drug, a triazolyl heterocycle, and a substituted or unsubstituted aryl group. In some forms, the compounds show anti-inflammatory properties and optionally analgesic properties with similar or higher efficiencies compared with their respective parent drugs, with additional advantages including no or reduced adverse effects (e.g., without ulcerogenic liability in the gastric) and / or selective inhibition of COX-2 over COX-1. Pharmaceutical compositions suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical formulation can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. Methods for preventing or treating an inflammatory disease or disorder in a subject are also disclosed.

The invention relates to the technical field of organic synthesis, in particular to a method for synthesizing a chiral allene compound from aromatic hydrocarbon and alkyne. A simple aromatic hydrocarbon compound and thianthrene-S-oxide are designed to construct an aryl thianthrene salt in situ under the action of an electrophilic activation reagent, then the aryl thianthrene salt constructed in situ under catalysis of a palladium catalyst and a chiral ligand is subjected to an asymmetric Heck reaction with alkyne, and the tri-substituted chiral allene compound is rapidly and efficiently constructed. The method is mild in condition, wide in substrate range and excellent in enantioselectivity and yield, and meanwhile, chiral allene fragments can be introduced into salicin and indometacin which have anti-inflammatory and analgesic activities.

The application discloses a stomach-derived limosilactobacillus fermentum LAF-09 and application thereof, and the preservation number of the stomach-derived limosilactobacillus fermentum LAF-09 is GDMCC No. 65656. The inventor of the application screens a stomach-derived limosilactobacillus fermentum LAF-09 from stomach mucosa tissue of healthy people, the strain has strong acid resistance and high proliferation capacity in the stomach, has strong adhesion properties to stomach epithelial GSE-1 cells, can be effectively applied to prevent and treat gastric ulcers caused by indomethacin, and has no obvious side effects.

The present invention discloses a pterostilbene chalcone compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. The compound has a strong inhibitory effect on LPS-induced NO production in RAW264.7 cells, significantly superior to indomethacin, and can be developed into a new anti-inflammatory drug. The preparation method of the compound of the present invention is characterized by readily available raw materials, simple operation, and high yield.

A 2,3-fused quinazolinone derivative, its preparation method, and application are disclosed. A 2,3-quinazolinone derivative was synthesized using a simple method with high yield and low production cost. At a concentration of 5 µM and an LPS concentration of 1 µg / mL, compounds 1e and 1f exhibited superior NO release inhibition compared to the anti-inflammatory drugs indomethacin and evodiamine, while compounds 1g and 1q were comparable to indomethacin, and compounds 1w and 1m were comparable to evodiamine. Compounds 1e, 1f, 1g, 1q, and 1m, which exhibited strong NO release inhibition, exhibited less cytotoxicity against RAW264.7 cells than the anti-inflammatory drugs indomethacin and evodiamine. The derivative exhibited significant anti-inflammatory effects and low toxicity. The derivative can be formulated into various dosage forms of anti-inflammatory drugs, possessing high medical value and broad market prospects.

The invention provides an umbilical cord mesenchymal stem cell adipogenic induced differentiation culture medium and a culture method, and belongs to the technical field of stem cell induced differentiation. Comprising a DMEM culture medium, fetal calf serum, dexamethasone, insulin, indometacin, IBMX, Zardaverine and glabridin. Zardaverine and glabridin are added into an umbilical cord mesenchymal stem cell adipogenesis induced differentiation culture medium according to a certain concentration, and the synergistic effect of Zardaverine, glabridin and other components can better induce the umbilical cord mesenchymal stem cells to differentiate into adipocytes, increase the number of lipid droplets, increase the volume of the lipid droplets, enhance the lipid storage capacity of the adipocytes, and improve the adipogenesis of the umbilical cord mesenchymal stem cells. The adipogenic differentiation induction period is shortened, and the problems of low adipogenic differentiation rate, long induction time, few and small lipid droplets, unstable adipogenic effect and the like in the three-dimensional differentiation identification of the umbilical cord mesenchymal stem cells are solved.

The invention belongs to the technical field of medicines, and particularly relates to a preparation method and application of a self-assembled conjugate of a non-steroidal anti-inflammatory drug and irinotecan. Water-insoluble non-steroidal anti-inflammatory drugs (ibuprofen, oxaprozin, naproxen, indometacin and the like) are introduced into a water-soluble anti-tumor drug irinotecan through esterification reaction and are self-assembled into nano particles in an aqueous solution, and then the self-assembled nano conjugate with an anti-tumor effect is formed. The inhibition activity of the nano particles prepared by the method on tumor cells is far better than that of irinotecan and a corresponding physical mixture of a non-steroidal anti-inflammatory drug and irinotecan, cancer cell proliferation can be accurately blocked by synergistically inhibiting protein expression of COX-2 and Topo I, particularly, the inhibition effect on Topo I is better, the anti-tumor treatment effect is greatly improved, and the nano particles have good application prospects. And a more efficient scheme is provided for tumor treatment.

An improved process for the preparation of Indomethacin of formula (I):is provided by means of the precipitation, crystallization, re-crystallization or re-slurry of the intermediate 4-chloro-N-(4-methoxyphenyl)benzohydrazide in a mixture containing tetrahydrofuran and a C1-C4 linear or branched alkyl alcohol.

The invention discloses an adhesive hydrogel microneedle as well as a preparation method and application thereof, belongs to the technical field of biological materials, and solves the problem that the curative effect of a drug delivery system applied to gout treatment in the prior art is not ideal enough. The hydrogel microneedle based on the dithiolane carboxylic acid derivative, provided by the invention, is prepared by mixing the dithiolane carboxylic acid derivative with tea polyphenol nanoparticles and passing through a silica gel microneedle mold through an ultraviolet irradiation crosslinking effect. The hydrogel microneedle based on the dithiolane carboxylic acid derivative, provided by the invention, can be used for treating gouty arthritis by cooperating with the effects of the tea extract and the indometacin medicine.

The invention discloses indometacin dry particles and a preparation method and application thereof, and the indometacin inhalable dry particles comprise: L-amino acid; indometacin and / or a pharmaceutically acceptable derivative thereof; the mass ratio of the L-amino acid to the indometacin and / or the pharmaceutically acceptable derivative of the indometacin is 1.0: (0.1-1.0). The indometacin inhalable dry particles have excellent solubility and air properties, the deposition effect of indometacin in the lung can be effectively improved, and the effective deposition rate of the indometacin inhalation powder inhalation is effectively increased.

The present invention discloses a co-amorphous compound containing olaparib, a preparation method, and a pharmaceutical composition thereof. The co-amorphous compound is formed by combining olaparib with a nonsteroidal anti-inflammatory drug. The nonsteroidal anti-inflammatory drug in the co-amorphous compound includes component A: diclofenac or a pharmaceutically acceptable salt thereof; component B: ibuprofen or a pharmaceutically acceptable salt thereof; component C: flurbiprofen or a pharmaceutically acceptable salt thereof; component D: ketoprofen or a pharmaceutically acceptable salt thereof; and component E: indomethacin or a pharmaceutically acceptable salt thereof. The co-amorphous compound of olaparib and the nonsteroidal anti-inflammatory drug disclosed herein has one or more advantages, including significantly improved solubility, significantly improved dissolution rate, good physical stability over three months under long-term conditions, and significantly enhanced antitumor activity. Therefore, the co-amorphous compound of olaparib and the nonsteroidal anti-inflammatory drug is expected to become a new compound solid preparation for the treatment of related cancers.

The invention provides a neocadinane type sesquiterpene compound fisduterpene and application thereof in preparation of anti-inflammatory drugs, the compound is extracted from dry stems of fissistigma oldhamii, the structural formula of the compound is determined through spectrum analysis, the molecular formula of the compound is C15H22O3, and the compound belongs to neosesquiterpenes. The preparation method comprises the following steps: extracting stems with 60-80% ethanol, carrying out vacuum concentration, extracting with petroleum ether and ethyl acetate, and carrying out silica gel column chromatography, Sephadex LH-20 column chromatography and high performance liquid chromatography purification. Pharmacological experiments show that the compound has a remarkable inhibiting effect on LPS-induced BV2 cell NO release, IC50 is 5.63 + / -0.22 mu M, the activity is superior to that of indometacin, and the compound can be used as a candidate component of anti-inflammatory drugs and provides a material basis and an application prospect for research and development of novel anti-inflammatory drugs.

The present invention provides a nucleoside derivative for preventing and treating inflammation and an application thereof in the preparation of a drug for preventing and treating inflammatory diseases. The nucleoside derivative for preventing and treating inflammation provided by the present invention can significantly ameliorate conditions of pancreatitis, hepatitis, arthritis and the like, ameliorate organ injury and inflammatory indexes, and have better effects than positive control drug, indometacin. Compared with the conventional anti-inflammatory drugs, aspirin, ibuprofen, indomethacin, phenylbutazone, diclofenac, piroxicam and glucocorticoids, the nucleoside derivative for preventing and treating inflammation provided by the present invention has the advantage of significantly fewer side effects.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an indometacin liniment for external use and a preparation process thereof, the indometacin liniment is prepared by compounding indometacin, a composite solubilizer, a composite stabilizer, a penetration enhancer, a humectant, a pH regulator and a solvent; wherein the composite solubilizer is a compound system of ethanol, N-sodium methyl taurate, lauroyl lysine and propylene glycol, the composite stabilizer is a compound system of ethylene diamine tetraacetic acid, acetylcysteine and dithiothreitol, the penetration enhancer is peppermint oil, the humectant is glycerol, the pH regulator is triethanolamine / citric acid, and the solvent is purified water. Through the specific compounding design of the components and the precise control of the preparation process, the obvious improvement of the water solubility of the indometacin and the effective guarantee of the content stability of the preparation are synchronously realized.

The application belongs to the technical field of medicine, and particularly discloses a small-molecule indometacin hydrogel and a preparation method thereof. The small-molecule hydrogel is obtained by mixing indometacin and a small-molecule ligand, adding a small amount of deionized water, and oscillating. The small-molecule hydrogel has the advantages of solubility and permeability, with the small-molecule ligand as a matrix. The formed small-molecule hydrogel can significantly improve the solubility and dissolution / release rate of indometacin. Compared with indometacin crystals, the water solubility of the two small-molecule hydrogels of indometacin-meglumine and arginine is increased by 506 times and 479 times, respectively, and the cumulative release rate at 2h is increased by 2.67 times and 3.05 times, respectively. Meanwhile, the small-molecule hydrogel significantly promotes the membrane permeability of indometacin, enhances the development potential of indometacin in oral and transdermal applications, and provides a new preparation idea for solving the solubility and permeability defects of non-steroidal anti-inflammatory drugs and other poorly soluble drugs.

The invention relates to the technical field of biological culture, and particularly discloses a culture medium for improving synthesis of unsaturated fatty acid in cell culture fat, which is used for solving the problem that the content of unsaturated fatty acid in the culture fat is not satisfactory. The differentiation culture medium comprises the following components: a basic culture medium, a specific porcine adipose-derived mesenchymal stem cell differentiation induction factor and an unsaturated fatty acid additive. Wherein the specific induction factors comprise but are not limited to factors such as insulin, dexamethasone, indometacin, 3-isobutyl-1-methylxanthine, rosiglitazone and the like. The unsaturated fatty acid additive comprises alpha-linolenic acid, and by adding the substances into the culture medium, the differentiation efficiency of the porcine adipose-derived mesenchymal stem cells and the directional synthesis of the unsaturated fatty acid in the cells can be improved. According to the improved differential culture medium, cell differentiation and unsaturated fatty acid synthesis are effectively promoted by optimizing components and proportions, and the improved differential culture medium has an important application prospect.

The invention discloses a squalene type triterpenoid compound, a preparation method thereof and application of the squalene type triterpenoid compound to anti-inflammatory drugs. According to the invention, the irpolacrin C with remarkable anti-inflammatory activity is separated from a rice solid fermentation culture of a casuarina equisetifolia endophytic fungus Irpus lactus SC4004, and the irpolacrin C is as shown in a formula (I) which is described in the specification. The irplacrin C is a novel squalene type triterpenoid compound, the half inhibitory concentration (IC50) of the irplacrin C is 32.53 mu M, and the IC50 value of the positive control indometacin is 29.44 mu M. The irplacrin C is a novel squalene type triterpenoid compound. The invention provides a candidate drug for research and development of novel anti-inflammatory drugs, and provides a scientific basis for development and utilization of casuarina equisetifolia endophytic fungus resources.

The invention discloses a quinoline-malononitrile derivative, a preparation method thereof and application of the quinoline-malononitrile derivative as a near-infrared AIE fluorescent probe targeting COX-2, and belongs to the technical field of fluorescent probes. According to the quinoline-malononitrile derivative, quinoline-malononitrile serves as a fluorophore, thiophene and triphenylamine are introduced, a fluorescent parent nucleus of a strong D-pi-A structure is formed through conjugate connection, on the basis, an alkyl chain is connected with celecoxib or indometacin, and the quinoline-malononitrile derivative is a near-infrared AIE fluorescent probe, has good biocompatibility and stability, and can be used as a fluorescent probe for detecting the fluorescence intensity of a human body. The quinoline-malononitrile derivative has a targeting property on COX-2, shows bright fluorescence in MCF-7, shows weak fluorescence in HUVEC, can generate fluorescence response according to COX-2 fluctuation and can realize accurate imaging of a tumor microenvironment, and the structure of the quinoline-malononitrile derivative is as follows: # imgabs 0 # or # imgabs 1 #.

To provide a topical pharmaceutical composition containing indomethacin, diclofenac sodium, felbinac, salicylic acids, or heparins, wherein irritation to the application site is reduced. [Solution] A topical pharmaceutical composition that contains component (A) and component (B) below, wherein component (A) is one or more selected from the group consisting of components (A-1) to (A-5) below, and which reduces irritation to the application site. Ingredient (A-1): Indomethacin Ingredient (A-2): Diclofenac sodium Ingredient (A-3): Felbinac Ingredients (A-4): Salicylic acids Ingredient (A-5): Heparinoid Ingredient (B): One or more selected from the group consisting of loxoprofen, its salts, and their hydrates.

The invention relates to an inducer and an induction method for adipose differentiation of mesenchymal stem cells, and the inducer for adipose differentiation of mesenchymal stem cells is characterized in that 3-isobutyl-1-methylxanthine IBMX, insulin, indometacin, fetal calf serum, dexamethasone sodium phosphate, astragaloside, resveratrol and iridoside A are contained in a DMEM (dulbecco's modified eagle medium) high glucose culture medium. When the mesenchymal stem cells are cultured, only the inducer is used, and different proportions of inducers do not need to be added into a culture medium like the prior art; moreover, the adipose differentiation induction time is shortened, the adipose differentiation induction rate is not lower than 91.3% after culture is carried out for 15 days, and the adipose differentiation induction rate is not lower than 94.8% after culture is carried out for 21 days.

The invention discloses indometacin emulsifiable paste and a preparation method thereof, and aims to solve the problems that the existing oral indometacin is large in gastrointestinal irritation, and an external preparation is low in solubility, poor in transdermal permeability and insufficient in stability. The emulsifiable paste comprises the following components in parts by weight: an oil-phase matrix consisting of indometacin, dimethyl sulfoxide, liquid paraffin, white vaseline, octadecanol and hexadecanol, and a water-phase matrix consisting of lauryl sodium sulfate, urea and the like. The emulsifiable paste is high in indometacin solubility, excellent in transdermal efficiency, good in stability and free of gastrointestinal tract irritation, is suitable for the elderly, special crowds with hepatic and renal insufficiency and the like, and is suitable for industrialization and clinical application.

The invention discloses preparation of an indissolvable drug solubilizing system and application of the indissolvable drug solubilizing system in drug solubilization, and belongs to the technical field of medicines.The solubilizing system uses dendritic mesoporous silica as a carrier of an indissolvable drug, and the carrier plays a role in solubilizing and protecting the indissolvable drug; the oral bioavailability of insoluble drugs is increased; the indissolvable drugs refer to BCS II type drugs, such as indomethacin, magnolol and carvedilol. The preparation method of the system comprises the following steps: adding distilled water into triethanolamine, carrying out ultrasonic dispersion, adding hexadecyl trimethyl ammonium bromide and sodium salicylate into a reaction system, continuously stirring, dropwise adding tetraethoxysilane into the reaction system, continuously reacting, cooling a product to room temperature, centrifugally washing, drying, and calcining to obtain the high-temperature-resistant graphene oxide. The dendritic mesoporous silica carrier is obtained. Adding the medicine into methanol, dissolving the medicine under an ultrasonic condition, adding the dendritic mesoporous silica, ultrasonically stirring, evaporating methanol, drying and collecting.

The invention discloses a quinolyl fluorescent probe containing indometacin as well as a preparation method and application of the quinolyl fluorescent probe. The structural formula of the probe is shown in the specification. According to the probe constructed by the invention, a quinoline fluorophore is coupled with a COX-2 targeting group indometacin through a variable-length carbon chain connector, so that the fluorescent probe has relatively large Stokes shift gt; and the wavelength is 160 nm. Wherein the probe ICP-1 shows excellent environmental sensitivity due to limited intramolecular rotation, selectivity and open-type fluorescence detection on COX-2 can be realized, and the probe successfully visualizes RAW 264.7 macrophages induced by lipopolysaccharide, PC12 neuronal cells stressed by glutamic acid and COX-2 up-regulation in an AD zebra fish model. Besides, ICP-1 is effectively used for screening the COX-2 inhibitor to confirm the neuroprotective effect of hararine, and it is indicated that ICP-1 is a powerful tool for real-time neuroinflammation imaging and has application value in neurodegenerative disease research.

The application belongs to the technical field of anti-inflammatory drug development, and discloses an indometacin derivative containing 2-amino-1,3,4-thiadiazole and preparation and application thereof. The derivative is a compound with the structure shown in formula 2 or a pharmaceutically acceptable salt thereof. The application first designs and successfully synthesizes a novel indometacin derivative containing 2-amino-1,3,4-thiadiazole, and the structure is characterized. The preparation method of the indometacin derivative containing 2-amino-1,3,4-thiadiazole is simple, convenient to operate, and can quickly synthesize the compounds. Research shows that the indometacin derivative containing 2-amino-1,3,4-thiadiazole has good anti-inflammatory activity and good application prospect in inflammatory diseases.

The present disclosure in various aspects and embodiments provides formulations that solubilize and / or suspend poorly soluble active ingredients, such as but not limited to ketotifen and indomethacin, for use in coating processes to manufacture drug products. In other aspects, the disclosure provides spray-coated products with low impurities and high homogeneity and mass transfer efficiencies relative to products produced with conventional pan coating or spray-coating processes. In aspects, the disclosure provides pharmaceutical compositions and methods of treatment involving these spray-coated products.

The present application relates to a kind of evodia rutaecarpine analog and its preparation method and application, belong to the field of synthetic chemistry of medicine. With 4 (3H) -quinazolinone derivative as substrate, phthalocyanine iron as catalyst, evodia rutaecarpine analog is synthesized by intramolecular hydrogen transfer reaction, high yield, low production cost. When concentration is 25 μM, LPS concentration 1 μg / mL, compound 1c, 1t, 1u, 1v inhibit NO release ability is superior to anti-inflammatory drug indometacin, and 1a, 1b, 1i is equivalent to indometacin;Inhibit NO release ability stronger compound 1c, 1t, 1u and 1v are weak to RAW264.7 cell cytotoxicity;Anti-inflammatory effect is obvious, and toxicity is very small, has very high medical value and broad market prospect.