10 results about "Esomeprazole" patented technology

The present application relates to a kind of sulfide monooxygenase mutant and its application in esomeprazole synthesis.The sulfide monooxygenase mutant, its encoding gene, the preparation method of the recombinant expression vector containing the gene sequence, co-expression recombinant vector and recombinant expression transformant, and the application of the recombinant sulfide monooxygenase mutant catalyst in esomeprazole synthesis are specifically disclosed.Compared with other sulfide monooxygenases, the sulfide monooxygenase mutant obtained by the present application can efficiently utilize the coenzyme NADH with lower cost and higher stability to catalyze the asymmetric oxidation reaction of omeprazole sulfide, prepare esomeprazole, has the advantages of high substrate concentration, mild reaction condition, environment-friendly, simple operation, high yield, low production cost and good industrial application prospect.

The invention belongs to the crossing field of chemical biology and green catalysis, and particularly relates to application of an artificial photoenzyme as a catalyst to synthesis of an esomeprazole compound. The artificial photoenzyme is constructed by inserting non-natural amino acid containing a benzophenone structure into a protein skeleton; the invention aims to realize in-situ generation and chiral control of singlet oxygen by introducing a benzophenone photosensitive group into a protein skeleton at a fixed point, and solves the technical problems of need of expensive renewable coenzyme, poor enzyme stability, high loading capacity and low yield in the existing esomeprazole enzyme method process.

The application discloses a sequential anti-tumor strategy based on improvement of tumor microenvironment (TME) combined with CAR T and application thereof, and belongs to the technical field of biological medicine, which simultaneously improves tumor fibrosis and acid microenvironment by applying tumor-related fibroblast (CAF) targeting drugs and proton pump inhibitors, and sequentially injects CAR T combined therapy for solid tumors, wherein the CAF targeting drugs are selected from tretinoin, calcipotriol, losartan and minnelide, the proton pump inhibitors are selected from lansoprazole, omeprazole, pantoprazole, rabeprazole and esomeprazole, and the CAR T receptor or ligand is selected from mesothelin, protein tyrosine kinase 7, NKG2D, CD47, B7-H3, MUC1 and HER2; the sequential administration strategy first destroys the dense physical barrier of the tumor microenvironment, improves the acidity of the tumor site, ensures the infiltration, survival and proliferation of CAR T at the tumor site, and then targets and inhibits the growth of solid tumors, especially high-malignancy triple-negative breast cancer, by using the specificity of CAR T.

The present application provides a method for quantitatively analyzing acid-suppressing drugs by a high-performance liquid chromatography-tandem mass spectrometry device, comprising: preparing a sample solution containing the acid-suppressing drug; injecting the sample solution into the high-performance liquid chromatography-tandem mass spectrometry device to obtain a mass chromatogram; and quantitatively analyzing the acid-suppressing drug using an internal standard method according to the mass chromatogram, wherein the acid-suppressing drug is selected from: esomeprazole, rabeprazole, ilaprazole, lansoprazole, pantoprazole and vonoprazan fumarate; using a mixed mobile phase consisting of mobile phase A and mobile phase B for gradient elution in the high-performance liquid chromatography, wherein mobile phase A is an acetonitrile solution containing formic acid or a water-acetonitrile mixture containing ammonia and ammonium acetate (water: acetonitrile volume ratio: 1:99-10:90); and mobile phase B is selected from an aqueous solution containing ammonium acetate, an aqueous solution containing formic acid and ammonium acetate, an aqueous solution containing ammonia and ammonium acetate, and an aqueous solution containing ammonia and ammonium formate.

The invention relates to a preparation method and application of 5-(1H-pyrrole-1-yl)-2-mercaptobenzimidazole, according to the preparation method, key parameters such as an ester extraction solvent, a pH adjusting range, a pulping solvent, a ratio of a concentrated solution to the pulping solvent and the like are determined to cooperate with each other, and efficient separation and purification of a product are realized. And the synergistic improvement of economy, environmental protection, high yield and high content is realized. The solvents and reagents selected in the whole process are conventional chemical raw materials, are low in price and easy to obtain, and the solvents and mother liquor can be recycled and reused, so that the production cost is further reduced; the operation process is simplified, the production cost and the environmental protection pressure are reduced, and the environmental protection requirement of industrial production is met; the yield of the target product can be stably kept at 74% or above, the purity can reach 99% or above, and the content is higher than 97%. The prepared product can be applied to preparation of ilaprazole, meets the quality requirement for preparation of qualified ilaprazole bulk drugs, and has important industrial application value.

Embodiments herein provide a pharmaceutical formulation comprising an anti-inflammatory antipyretic agent with reduced side effects, addressing gastric problems. An enteric-coated tablet of the present invention comprises esomeprazole, aceclofenac, and paracetamol, along with maize starch, microcrystalline cellulose, povidone K30, colloidal anhydrous silica, and magnesium stearate.

The present invention relates to a pharmaceutical composition in the form of bilayer tablet comprising a) first layer comprising granules or powder containing Naproxen and at least one pharmaceutically acceptable excipient, and b) second layer comprising dry granulated granules containing Esomeprazole and its pharmaceutically acceptable salt and at least one pharmaceutically acceptable excipient. The invention further relates to a process for the preparation of said pharmaceutical composition.

The application provides a preparation method of crystalline form B of ilaprazole. The application provides a preparation method of crystalline form B of ilaprazole, which comprises the following steps: mixing a solution or slurry of ilaprazole raw materials and a good solvent with an anti-solvent, and crystallizing to obtain the crystalline form B of ilaprazole. The preparation method of the application has the advantages of good stability, high yield, good purity, low solvent residue, compliance with the standard of raw materials, and suitability for industrial production.

The present disclosure provides a kind of ilaprazole freeze-dried enteric-coated tablets and its preparation method.The above-mentioned ilaprazole freeze-dried enteric-coated tablets include tablet core and coating layer, tablet core includes ilaprazole, tablet core also includes disintegrating agent, freeze-drying protective agent and pharmaceutical excipient, the tablet core after freeze-drying treatment is formed with loose porous structure, and the moisture content of tablet core is <5%.The above-mentioned ilaprazole freeze-dried enteric-coated tablets, since the tablet core after freeze-drying treatment is formed with loose porous structure, and the moisture content of tablet core is <5%, both can improve the long-term storage stability of tablet core, effectively avoid the increase of related substances in long-term storage process, to improve the efficacy of ilaprazole and the safety of drug;It can also speed up the rapid release of tablet core in the intestine, improve the absorption efficiency of ilaprazole in the intestine, to enhance the curative effect of drug.

The embodiment of the invention provides an application of a proton pump inhibitor or a derivative thereof, or a compound thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof in preparation of anti-xerophthalmia drugs. The proton pump inhibitor is prepared from any one or a combination of at least two of omeprazole, lansoprazole, pantoprazole, rabeprazole, reminoprazole, esomeprazole or tenatoprazole. According to the application, the proton pump inhibitor is loaded on the self-assembled nucleic acid, so that the composite material has efficient corneal cell membrane penetrating capacity, and can remarkably inhibit expression of inflammatory factors and improve the ocular surface inflammation microenvironment; in addition, the compound also has relatively good biological safety, shows an excellent treatment effect on in-vivo and in-vitro xerophthalmia models, and provides a new choice for clinical xerophthalmia treatment.