32 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 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 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 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 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.

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 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.

The application discloses a palmitoyl hydrochloride-indometacin pharmaceutical cocrystal as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical crystallization. 21 H 22 ClNO4]·[C 19 H 16 ClNO4]. The palmitoyl hydrochloride-indometacin pharmaceutical cocrystal is prepared by mixing palmitoyl hydrochloride hydrate and indometacin in a solvent system according to a molar ratio of 1:1 and through stirring treatment in a suspended state. The process flow is simple, the operation is convenient, and the cocrystal has a high yield. In a pH 6.8 simulated intestinal fluid medium, the dissolution rate of palmitoyl hydrochloride in the pharmaceutical cocrystal is obviously lower than that of pure palmitoyl hydrochloride, and the pharmaceutical cocrystal presents a sustained-release behavior. On the contrary, the dissolution rate of indometacin in the pharmaceutical cocrystal is obviously improved, which is beneficial to the improvement of the bioavailability of indometacin. The palmitoyl hydrochloride-indometacin pharmaceutical cocrystal also has good human colon cancer cell inhibition activity.

The invention provides a superoxide anion free radical activated indometacin-transretinoic acid prodrug, a preparation method of an albumin compound of the superoxide anion free radical activated indometacin-transretinoic acid prodrug and application of a composition prepared from the compound and an antitumor drug. The prodrug compound and an anti-tumor drug are prepared into the composition, the prodrug is activated by superoxide anion free radicals overexpressed in a tumor microenvironment, prototype drugs of indometacin and transretinoic acid are released, the damage effect of the transretinoic acid on a Golgi apparatus structure of a tumor cell is remarkably enhanced, and excellent broad-spectrum applicability is shown; and the device can be adapted to various drug delivery systems and disease models.

The invention discloses a stomach-derived lactobacillus fermentum LAF-09 and an application of the stomach-derived lactobacillus fermentum LAF-09, wherein the preservation number of the stomach-derived lactobacillus fermentum LAF-09 is GDMCC (China General Microbiological Culture Collection Center) No.65656, and the preservation number of the stomach-derived lactobacillus fermentum LAF-09 is GDMCC No.65656. The invention further discloses a preparation method of the stomach-derived lactobacillus fermentum LAF-09 and application of the stomach-derived lactobacillus fermentum LAF-09. According to the present invention, the stomach-derived lactobacillus fermentum LAF-09 is screened from the gastric mucosa tissue of the healthy population, and the strain has characteristics of strong acid resistance and high intragastric proliferation capacity, has strong adhesion to the gastric epithelial cell GSE-1, can be effectively used for preventing and treating the gastric ulcer caused by indometacin, and does not have significant side effects. The invention further provides a preparation method of the stomach-derived lactobacillus fermentum LAF-09, and the stomach-derived lactobacillus fermentum LAF-09 can be used for preparing the stomach-derived lactobacillus fermentum LAF-09, such that the stomach-derived lactobacillus fermentum LAF-09 can be used for preparing the stomach-derived lactobacillus fermentum LAF-09, and the stomach-derived lactobacillus fermentum LAF-09,

The application discloses a kind of sorafenib co-amorphous drug and its preparation method and application.Co-amorphous drug is made of active ingredient sorafenib and ligand according to 1:1 mole ratio;Ligand is selected from any one of L-phenylalanine, L-proline, L-arginine and indometacin;Sorafenib and ligand form single homogeneous amorphous structure by intermolecular interaction.By X-ray powder diffraction, differential scanning calorimetry and infrared spectroscopy, the results show that sorafenib and ligand form single homogeneous amorphous structure by intermolecular hydrogen bond interaction.Compared with sorafenib crystalline raw material and physical mixture, the application improves the equilibrium solubility and dissolution rate of sorafenib in physiological medium, and shows excellent physical stability, can effectively inhibit the recrystallization of drug during storage, provides a new preparation strategy for improving the oral bioavailability of sorafenib.

The disclosure provides a high-dose dry powder inhaler formulation of a carrier-based formulation. Specifically, larger drug particles serve as the carrier for the smaller micronized drug particles such that an inhaled dose is combined with an oral dose. The coarse drug particles act as a carrier and allow improved powder flow and aerosol performance while also providing a potential secondary route of absorption of indomethacin; oral.

The application discloses a kind of stable indometacin tablets and its preparation process, belong to pharmaceutical preparation technical field.The tablet is composed of indometacin, hydroxypropyl beta-cyclodextrin, soybean phospholipid, composite stabilizer, binder and lubricant, and the composite stabilizer is compounded by succinylated c14-c18 alkyl sulfonate sodium, N-ethyl-L-glutamine and maltodextrin according to specific mass ratio.Preparation process includes liposome inclusion compound preparation, mixing granulation, drying whole particle, total mixing and tabletting.The application realizes the preparation of high drug loading design, and the composite stabilizer forms a multilayer coating protection system with hydroxypropyl beta-cyclodextrin and soybean phospholipid, which synergistically improves the dissolution performance and stability of the preparation, makes the dissolution rate of the preparation fast, and the content of the main component decreases little during long-term storage, solves the problems of low drug loading, poor stability and dissolution of existing indometacin tablets.

The invention provides a double-layer tablet and a preparation method thereof. The double-layer tablet comprises a quick-release layer and a slow-release layer, wherein the quick-release layer comprises an indometacin solid dispersion, a disintegrating agent, a filling agent and a lubricating agent; the sustained-release layer comprises an indometacin solid dispersion, a disintegrating agent, a filling agent, a high-molecular sustained-release polymer and a lubricating agent. The quick-release layer is prepared by adopting a direct powder compression method, and then the raw materials of the slow-release layer are mixed and compressed to the second layer to obtain the double-layer tablet. The preparation process is simple, the medicine is rapidly released to 45% at the initial stage of tablet release, the medicine is continuously and stably released after 20 min, the final release amount reaches 80% or above, no burst release phenomenon exists in the release process, and meanwhile good adhesion time and adhesion force are guaranteed.

The invention discloses diterpenoid compounds in honeycomb and a preparation method and application thereof.The preparation method comprises the steps that the honeycomb is dried in the air and then ground into powder, extraction is conducted through an organic reagent, purification is further conducted through macroporous resin, sephadex, normal-phase silica gel, reverse-phase silica gel and other column chromatography methods, and the diterpenoid compounds are obtained. A monomeric compound is prepared through semi-preparative high performance liquid chromatography, and finally three diterpenoid compounds with novel structures are obtained through structural identification such as one-dimensional nuclear magnetism, two-dimensional nuclear magnetism, ECD and X-single crystal diffraction. The three diterpenoid compounds provided by the invention can inhibit the generation of nitric oxide in a cell inflammation model, and the IC50 of the compound 1 is superior to that of a positive drug indometacin. In addition, the compound 1 can down-regulate gene expression of inflammatory factors IL-1beta and IL-6, has an inhibition effect stronger than that of indomethacin with the same concentration, has remarkable anti-inflammatory activity, and can be applied to development of drugs for treating gouty arthritis.

Composition, in particular pharmaceutical composition, especially for use in the prophylactic and / or therapeutic (symptomatic) treatment of veisalgia (alcohol intoxication, hangover), wherein the composition is in the form of a fixed dosage (fixed dosage form) for oral administration, and wherein the composition comprises an effective, in particular pharmaceutically and / or therapeutically effective, amount of active substances from the drug classes (i) non-steroidal anti-inflammatory drug (NSAID), (ii) H1 antihistamine and (iii) calcium channel antagonist, wherein the active substances are selected from Class (i): Acetylsalicylic acid, ibuprofen, dexibuprofen, flurbiprofen, naproxen, ketoprofen, tiaprofenic acid, diclofenac, indomethacin, acemetacin, flufenamic acid, mefenamic acid, piroxicam, tenoxicam, meloxicam, lornoxicam, nabumetone and / or mixtures thereof, Class (ii): Dimenhydrinate, and Class (iii): Cinnarizine.

The application discloses an anchor COX-2 protein responsive photosensitizer and a preparation method and application thereof, relates to the technical field of biological medicine and disease treatment. The compound IRID-SS shown in formula (I) prepared by the application is provided with a near-infrared cyanine as a photosensitive unit, an indomethacin as a COX-2 targeting ligand and a disulfide bond as a glutathione response unit. The compound can be activated under the condition of high glutathione in a tumor microenvironment, specifically anchors Golgi COX-2 protein, generates reactive oxygen species in situ through near-infrared laser irradiation, realizes irreversible oxidative damage of COX-2 protein, and induces pyroptosis of tumor cells through a Caspase-3 / GSDME channel. The compound has a simple synthesis method, does not introduce toxic reagents, does not have the problem of toxic reagent residue, has high biological safety, and therefore has good practical application value.

[Problem] To provide a pharmaceutical composition for external use, which comprises indomethacin, diclofenac sodium, biphenylacetic acid, a salicylic acid, or a heparin, and which alleviates irritation to a site to which the pharmaceutical composition is applied. [Solution] A pharmaceutical composition for external use, which is a composition that mitigates irritation to an application site, and which contains: one or more components (A) selected from the group consisting of the following components (A-1)-(A-5), and (B) one or more components (B) selected from the group consisting of the following components (A-1)-(A-5), the component (B) being one or more selected from the group consisting of the following components (A-1)-(A-5); component (A-1): indomethacin component (A-2): diclofenac sodium component (A-3): biphenylacetic acid component (A-4): salicylic acid component (A-5): heparin analogue component (B): one or more substances selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof.