68 results about "Indometacin" patented technology

The invention relates to the technical field of stem cell induced differentiation, and discloses an umbilical cord mesenchymal stem cell adipogenic induced differentiation culture medium and a culture method. The culture medium comprises the following substances: a DMEM (Dulbecco's Modified Eagle Medium) / F12 basal culture medium, fetal calf serum, insulin, penicillin, streptomycin, dexamethasone, 3-isobutyl-1-methylxanthine, indometacin, BMP-2 and FGF-1 (Fibroblast Growth Factor 1). The culture method comprises the following steps: (1) carrying out primary isolation culture on umbilical cord mesenchymal stem cells; (2) carrying out passage on the umbilical cord mesenchymal stem cells; and (3) inducing adipogenesis of the umbilical cord mesenchymal stem cells by using the adipogenesis induced differentiation culture medium. BMP-2 and FGF-1 are added on the basis of a traditional adipogenic induction culture medium to induce and promote the umbilical cord mesenchymal stem cells to be more efficiently differentiated into adipocytes under the combined action, so that the adipogenic differentiation time is shortened, and the adipogenic differentiation efficiency is improved; the umbilical cord mesenchymal stem cell adipogenic culture medium is stable in formula, simple and convenient in culture method and suitable for wide popularization.

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 a method for detecting nine antipyretic and analgesic drugs in feed, and belongs to the field of food safety detection. The method comprises the following steps: pretreating a feed sample to obtain a sample to be detected; detecting the nine antipyretic and analgesic drugs in the to-be-detected sample by adopting a liquid chromatography-mass spectrometry method; the nine kinds of antipyretic and analgesic medicines are antipyrine, phenylbutazone, acetaminophen, analgin, naproxen, diclofenac, indometacin, aspirin and ibuprofen. According to the pretreatment method provided by the invention, the problems of tedious steps, long consumed time and low accuracy of a detection result can be improved. By adopting liquid chromatography-mass spectrometry, simultaneous determination of multiple types of drugs can be realized, qualitative and quantitative analysis of multiple drugs can be rapidly and accurately completed in a short time, the timeliness requirement of actual detection is met, and the method can be used for feed quality safety monitoring.

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.

The present application relates to the technical field of pharmaceutical preparations, in particular to an indomethacin PLGA microsphere glass body injection with drug sustained release anti-inflammatory function and staining effect in vitreous cutting operation and application thereof, the injection comprises indomethacin and PLGA as a drug carrier and a physical dyeing agent. The PLGA provides vitreous cavity staining and intraoperative imaging on the one hand, assisting the operator to clearly identify the vitreous, proliferative membrane and the edge of the hole; on the other hand, the sustained release of indomethacin maintains the effective treatment concentration in the eye. Tests show that the effective concentration of the microsphere is maintained for about 3 times longer than that of free drugs, the inflammatory reaction is limited to the vitreous cavity, there is no lens toxicity, the safety is better than that of free drugs, the effect of inhibiting IL-1beta in the acute stage in the RRD-PVR model is significantly better than that of free drugs, and the retinal function is effectively protected. The present application realizes the diagnosis and treatment integration function of "one ball two use", and has good clinical transformation prospect.

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 relates to the technical field of gout treatment, in particular to a huperzine derivative, a preparation method of the huperzine derivative and application of the huperzine derivative in anti-gout drugs. In a first aspect, the present application discloses huperzine derivative compounds of general formula (I); on the second aspect, the invention discloses a preparation method of the huperzine derivative. On the third aspect, the huperzine derivative can be applied to gouty arthritis, the huperzine derivative represented by 3k and 3q remarkably inhibits release of IL-1beta induced by sodium urate at the concentration of 30 mu M, and compared with clinical anti-inflammatory drugs such as hydrocortisone, indometacin and colchicine, the huperzine derivative has the advantages that the anti-inflammatory effect is good, and the anti-inflammatory effect is good. The huperzine derivative disclosed by the invention well gives consideration to high inhibitory activity and low cytotoxicity, and has a good application prospect. # imgabs0 #

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.

Drug combinations, compositions including pharmaceutical compositions as well as methods of using and treating a viral infection, including one of the following: (1) atovaquone with a second group of substances consisting of ademetionine, albendazole, celastrol, cepharantine, chloroquine, cycloheximide, diethylstilbestrol, gemcitabine, homoharringtonine, hydroxy progesterone, imatinib, imipramine, indomethacin, ivermectin, niclosamide, raloxifene, sorafenib, and tipifarnib; or (2) cepharantine with a second group of substances consisting of ademetionine, albendazole, atovaquone, celastrol, chloroquine, cycloheximide, diethylstilbestrol, gemcitabine, homoharringtonine, hydroxy progesterone, imatinib, imipramine, indomethacin, ivermectin, raloxifene, sorafenib, and tipifarnib; or (3) one substance selected from a first group of substances consisting of ademetionine, albendazole, atovaquone, celastrol, cepharantine, chloroquine, cycloheximide, diethylstilbestrol, gemcitabine, homoharringtonine, hydroxy progesterone, imatinib, imipramine, indomethacin, ivermectin, raloxifene, sorafenib, tipifarnib in combination with a second group of substances selected from the group consisting of ademetionine, albendazole, celastrol, cepharantine, chloroquine, cycloheximide, diethylstilbestrol, gemcitabine, homoharringtonine, hydroxy progesterone, imatinib, imipramine, indomethacin, ivermectin, raloxifene, sorafenib, and tipifarnib.

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 present invention discloses a non-steroidal anti-inflammatory drug transdermal patch, which comprises a backing layer, a plaster layer and a release liner. The raw materials of the plaster layer are: indomethacin, amphiphilic cholesterol derivatives, isopropyl myristate, menthol, modified polyacrylate adhesive solution, tackifier, crosslinking agent, main drug solvent, wherein the modified polyacrylate adhesive solution uses ethyl acetate as a reaction solvent, and polyethylene glycol and zinc-based zeolitic imidazolate framework materials are respectively introduced during the polymerization of isooctyl acrylate, methyl acrylate and dimethylaminoethyl methacrylate; the present invention also discloses a preparation process of the non-steroidal anti-inflammatory drug transdermal patch. The non-steroidal anti-inflammatory drug transdermal patch of the present invention has air permeability, moderate adhesion, no skin irritation, can be administered locally, has a high transdermal permeation amount and a low residual drug amount, helps to improve the bioavailability and efficacy of the drug, and reduces the number of drug administrations and the drug dosage.

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 present invention belongs to the field of medical technology, and specifically discloses a novel scissoric terpenoid compound and a preparation method, a pharmaceutical composition and an application thereof. The scissoric terpenoid compound (±)-Cornuscone provided by the present invention has not been reported yet. Experimental results show that the scissoric terpenoid compound provided by the present invention has significant anti-inflammatory activity on lipopolysaccharide-induced RAW 264.7 cells, which is significantly better than the positive drug indomethacin, and can be used to develop drugs for the treatment of various inflammation-related diseases, including but not limited to arthritis, conjunctivitis, pneumonia, hepatitis, nephritis, gastroenteritis, metabolic syndrome, diabetes, cancer, etc.

The invention belongs to the technical field of biological medicines, and discloses application of indometacin combined with polymyxin in resisting salmonella infection. A checkerboard method minimum inhibition concentration test and an in-vitro time-sterilization curve test prove that the indometacin and colistin combined drug has an obvious synergistic effect on salmonella resistance, and the indometacin can enhance the antibacterial effect of the colistin drugs on salmonella standard strains and colistin-resistant salmonella. The invention provides a new drug combination strategy, and provides a new research thought and research and development direction for solving the increasingly serious drug resistance problem of polymyxin.

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 #.

The present invention relates to the preservation of collagenous connective tissue so as to achieve the structural integrality of the collagen fibers, rendering the tissue suitable for use in implants without causing immune and / or inflammatory rejection, comprising the steps of trimming the collagenous connective tissue in a buffer solution, washing the connective tissue with the buffer solution, stabilizing the tissue in an ethanol solution, treating the tissue with polyethylene glycol solution and hydrogen peroxide, washing and storing the tissue in ethanol, sterilizing the tissue with an ethanol and hydrogen peroxide solution and storing the tissue for transport in ethanol and indomethacin solution. The preferred use of the present invention is in surgical interventions for correcting various anomalies of the human body, where the graft is particularly required.