47 results about "Mesalazine" patented technology

The invention discloses application of scylla serrata antibacterial peptide Scycin in preparation of an anti-inflammatory composition and a preparation method of the scylla serrata antibacterial peptide Scycin. The nucleotide sequence of the scylla serrata antibacterial peptide Scycin is shown as SEQ ID NO.01. The invention further discloses a preparation method of the scylla serrata antibacterial peptide Scycin. In an LPS (lipopolysaccharide)-induced RAW 264.7 macrophage inflammation model, the recombinant expression plasmid vector containing the scylla antibacterial peptide Scin remarkably inhibits an inflammation cascade reaction by down-regulating expression of proinflammatory factors such as TNF-alpha (tumor necrosis factor-alpha) and IL-6 (interleukin-6), the anti-inflammatory effect of the recombinant expression plasmid vector is equivalent to that of a mesalazine positive control group, and obvious cytotoxicity is not observed.

The invention discloses a capsule medicament for endoscopic treatment of ulcerative colitis and a preparation method thereof, and belongs to the technical field of biological medicine, the capsule medicament is composed of a capsule matrix and a drug matrix; by adopting a dual control mechanism of an enteric layer coating and a pH response layer coating, accurate release of a medicine at a colon diseased region is ensured, medicine waste of the stomach and the small intestine is reduced, the medicine concentration at a focus is improved, mesalazine or budesonide is combined with the composite composition for treatment, inflammatory response is rapidly inhibited, acute symptoms are controlled, and the curative effect is good. A multi-mechanism synergistic treatment mode is adopted, the anti-inflammatory and repairing effects are enhanced, the clinical remission rate and the mucous membrane healing rate are remarkably improved, the pH response layer is dissolved in a colon alkaline environment, and the MMP-9 peptide cross-linking agent is subjected to enzymolysis at an inflammation part, so that the medicine is continuously released at a focus, the administration frequency is reduced, the compliance of a patient is improved, and the curative effect is good. In addition, the spherical gel particles in the medicament can prevent the medicament from being disintegrated too early in the intestinal tract, and the long-acting effect can be maintained.

The invention relates to betulinic acid type saponin derivatives as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The structural general formula of the betulinic acid type saponin derivative is # imgabs0, R1 is selected from hydroxyl or-O-G, and G is monosaccharide; r2 is selected from dopamine, 5-aminovaleric acid, 4-aminobutyric acid or 3-aminopropionic acid and the like and salts thereof. The betulinic acid type saponin derivative does not show obvious cytotoxicity to THP-1 macrophages, and can obviously reduce the release of IL-6 and IL-1beta in the THP-1 macrophages induced by LPS (lipopolysaccharide). Compared with betulinic acid and positive control medicine mesalazine, the pharmaceutical composition has better anti-inflammatory activity, has the treatment effect of improving diarrhea and hemafecia of mice with colitis remarkably superior to those of betulinic acid and positive control medicine mesalazine, has the treatment effect of dermatitis superior to that of positive control medicine dexamethasone, and does not have obvious toxic or side effects such as weight loss and immunosuppression. Therefore, the betulinic acid type saponin derivative has good in-vivo and in-vitro safety and druggability.

The invention belongs to the technical field of biological medicines, and particularly relates to application of a traditional Chinese medicine composition in preparation of a medicine for preventing or treating colitis. The invention provides application of a traditional Chinese medicine composition in preparation of a medicine for preventing or treating colitis. The traditional Chinese medicine composition is prepared from red ginseng, fructus aurantii stir-fried with bran and rabdosia amethystoides. The active ingredients of the traditional Chinese medicine composition disclosed by the invention highly coincide with related targets of colitis, so that a potential treatment mechanism is prompted. The traditional Chinese medicine composition can significantly improve weight loss and colon length shortening caused by colitis, recover colon crypt structure and reduce inflammatory factor level, and has an effect superior to that of mesalazine. The traditional Chinese medicine composition disclosed by the invention is suitable for various dosage forms to enhance the clinical applicability, and especially has relatively small toxic and side effects and good state recovery of treated individuals when being developed into a novel colon-targeted dosage form. The traditional Chinese medicine composition can be used as an important evidence for developing new clinical indications of the traditional Chinese medicine composition and treating colitis, and the clinical application value of the traditional Chinese medicine composition is expanded.

A use of oleanolic acid-28-O-β-D-glucopyranoside in the preparation of an anti-colitis drug is provided. The oleanolic acid-28-O-β-D-glucopyranoside has significant anti-ulcerative-colitis activity compared with parent nucleus oleanolic acid and other analogues, and has equivalent efficacy compared with Mesalazine, a first-line drug for the clinical treatment of inflammatory bowel disease, and can also avoid salicylic acid anaphylaxis possibly caused by Mesalazine western medicine treatment, thereby achieving a good application prospect.

The invention relates to the technical field of medicines, in particular to a budesonide-loaded oral colon targeting delivery system, a preparation method and application. According to the delivery system, budesonide entrapped by Pickering emulsion serves as a core, and a low-ester pectin-calcium ion cross-linked inner layer and a low-ester pectin-chitosan polyelectrolyte composite outer layer are sequentially wrapped on the outer layer; the preparation process is realized by combining an emulsion template method with a layer-by-layer self-assembly technology, the obtained microcapsule is of a uniform spherical structure, the particle size is about 400 microns, and the microcapsule has a double-layer three-dimensional network structure. The delivery system is kept stable in the gastrointestinal environment and releases drugs rapidly only under the colon pH condition, in-vitro simulation experiments show that the drug release rate in the stomach / small intestine stage is lower than 5%, and the drugs are released rapidly in the colon stage. Animal experiments prove that the effect of treating ulcerative colitis is equivalent to that of mesalazine, the toxicity of the whole body is remarkably reduced, the residence time of the medicine at the colon part exceeds 24 hours, and the medicine is not accumulated in a non-target organ.

The invention discloses preparation and application of a liquid metal micro-nano robot for treating colitis, and belongs to the technical field of biomedical materials and micro-nano robots. The liquid metal micro-nano robot is prepared by taking liquid metal micro-droplets as a core, coating the surface of the liquid metal micro-droplets with a polyelectrolyte multilayer film through a layer-by-layer self-assembly technology, and loading a medicine (such as mesalazine) for treating colitis in the polyelectrolyte multilayer film. The liquid metal micro-nano robot realizes colon targeted aggregation after oral administration, and can generate autonomous movement and photothermal effect under the irradiation of near-infrared light, thereby realizing phototropic targeted aggregation, photothermal triggering of drug release, and drug delivery and drug delivery. The problems that an existing mesalazine preparation is low in targeted delivery efficiency and a chemically-driven micro-nano robot is low in targeted delivery efficiency in a colon area are solved.

The invention relates to the technical field of pharmaceutical preparations, in particular to a mesalazine enteric-coated sustained-release tablet and a preparation process thereof. The preparation method comprises the following steps: S1, uniformly mixing mesalazine, a pH regulator, modified hydroxypropyl methyl cellulose, a filler and an adhesive, carrying out wet granulation, drying, carrying out size stabilization, adding a lubricant and a flow aid, uniformly mixing, and tabletting to obtain a tablet core; s2, uniformly mixing hydroxypropyl methyl cellulose and deionized water to obtain an isolation coating solution; spraying the isolation coating liquid onto the tablet core to form an isolation coating layer so as to obtain an isolation coating tablet core; s3, uniformly mixing a methacrylic acid-ethyl acrylate copolymer dispersion liquid, a modified polyacrylate emulsion, an ethanol water solution, Tween 80, a plasticizer and talcum powder to obtain an enteric coating liquid; and spraying the enteric coating liquid onto the isolation coating tablet core to form an enteric coating layer, thereby obtaining the mesalazine enteric sustained-release tablet.

The invention discloses a method for synthesizing mesalazine and application of mesalazine. The method comprises the following steps: introducing p-nitrophenol, formic acid and a Cu-Co-coated MFI-NS molecular sieve catalyst into a continuous flow reaction zone, and sequentially carrying out electrophilic substitution and nitro hydrogenation cascade reaction at normal pressure and 50-70 DEG C; the catalyst has a micropore-mesopore stepped pore channel, and contains a Cu0 metal cluster and a framework Co < 2 + > acid site. And separating, acidifying and crystallizing the reaction liquid to obtain a finished product. According to the invention, the shape-selective selectivity and difunctional synergistic effect of the molecular sieve are utilized, high conversion rate (gt, 98%) and high selectivity (gt, 94%) under mild conditions are realized, the product purity is greater than or equal to 99.5%, and the Cu / Co residue meets the ICHQ3D standard. The catalyst can be recycled for 10 times or more, the yield is reduced by 5% or less, iron mud pollution of a traditional iron powder method and the metal leaching risk of a noble metal catalyst are thoroughly eliminated, and the method has the remarkable advantages of being environmentally friendly, efficient, low in cost, easy to industrially amplify and the like and is suitable for preparing the medicine for treating the inflammatory bowel disease.

The invention discloses a preparation method of a mesalazine intermediate, which comprises the following steps: carrying out nitration reaction by using 2-chlorobenzoic acid as an initial raw material, and hydrolyzing in an alkaline aqueous solution to obtain a synthetic intermediate 5-nitrosalicylic acid of mesalazine. The method is mild in process condition, the used raw materials are cheap and easy to obtain, dangerous and toxic reaction conditions are not involved, the content of 3-site isomer impurities in the intermediate 5-nitrosalicylic acid product is 5% or below, and the total content of other impurities is lower than 0.5%.

The invention discloses a mesalazine microcrystalline capsule and a preparation method thereof, and belongs to the technical field of microcapsules. The mesalazine microcrystal capsule comprises an HPMCAS shell, and mesalazine microcrystals are loaded in the HPMCAS shell. The preparation method comprises the following steps: dissolving mesalazine in dimethyl sulfoxide to obtain a medicine solution, dissolving HPMCAS in ethyl acetate to obtain an anti-solvent, adding the medicine solution into the anti-solvent, and carrying out ultrasonication to obtain mesalazine microcrystals; the preparation method comprises the following steps: dissolving HPMCAS in ethyl acetate to obtain a shell material solution, dispersing mesalazine microcrystals in the shell material solution to obtain an oil phase, and dispersing the oil phase in a water phase by adopting a microfluidic technology to prepare the mesalazine microcrystal capsule. The mesalazine microcrystal is good in monodispersity and can release a large number of drugs in a concentrated mode. In the preparation process, the organic solvent in the oil-phase liquid drops is continuously diffused into the external continuous-phase fluid, the concentration of the shell material is increased until the shell material is cured into a shell, and the microcapsules with uniform particle sizes are prepared.

The present application relates to a new use of halogenophenol compound 4,5,2'-trihydroxy-2,5'-dibromobenzophenone, in particular in the preparation of a drug for treating inflammatory bowel disease. The halogenophenol compound of the present application can significantly alleviate the weight loss and colon shortening of the colonitis model, reduce the disease activity index of the colonitis model, reduce the inflammatory cell infiltration of the colonitis model, reduce the expression of inflammatory factors, has an immune regulation function on the intestinal tract, and is superior to the clinical first-line drug mesalazine in most indicators, and has application prospects in the treatment of inflammatory bowel disease.

The invention discloses a composition and application thereof in treating inflammatory bowel disease, and belongs to the technical field of medicine. The composition is prepared from N-acetylglucosamine and mesalazine. The N-acetylglucosamine and mesalazine in the composition provided by the invention have a synergistic anti-colitis effect, so that the recurrence rate of the inflammatory bowel disease (IBD) is reduced. The experimental result of the invention provides a theoretical basis for clinical drug combination of N-acetylglucosamine and mesalazine and an effective scheme for treating colitis, and has a wide application prospect in the field of medicine and pharmacology.

The invention discloses a preparation method and application of stable slow-release hydrogel, and belongs to the technical field of medical biological materials. An ammoniated polycaprolactone-polyethylene glycol carboxyl block copolymer (PCL-PEG-COOH) is self-assembled in a water-absolute ethyl alcohol system to form micelles, uniform catalytic sites are provided for tetraethyl orthosilicate, slow hydrolytic polycondensation of the tetraethyl orthosilicate is regulated and controlled, oriented deposition of silicon dioxide on the surface and cavities of the hydrogel is achieved, and the hydrogel is prepared. And constructing the composite hydrogel with a rigid structure and controllable pores. The hydrogel can efficiently load mesalazine and is stable and slow-released. The technical problems that traditional hydrogel is poor in mechanical stability and burst in drug release are solved, the accuracy and safety of ulcerative colitis treatment are improved, and the hydrogel has good clinical transformation potential.

The invention belongs to the technical field of mesalazine controlled-release preparations, and particularly relates to a mesalazine oral controlled-release pharmaceutical composition and a preparation method thereof.The mesalazine oral controlled-release pharmaceutical composition comprises a tablet core part and a coating part and is characterized in that the outer layer of the tablet core part is wrapped with the coating part, the tablet core part is composed of mesalazine and auxiliary materials, and the auxiliary materials are added into the tablet core part. The auxiliary material components comprise a matrix material, a filler, an adhesive and a lubricant, and the coating part is composed of an acid-resistant material, a plasticizer and a light shielding agent. According to the tablet core particle screening device, dried tablet core particles can be rapidly screened through the arranged vibration screening assembly, power of the vibration screening assembly can be transmitted through the arranged transmission assembly so that the transverse moving screening assembly can be driven, and the phenomenon that screening holes are blocked can be effectively reduced through the arranged transverse moving screening assembly; and therefore, the screening efficiency of the tablet core particles and the subsequent production efficiency can be improved.

The invention belongs to the technical field of mesalazine controlled-release preparations, and particularly relates to mesalazine colon-targeted controlled-release tablets and a preparation method thereof.The mesalazine colon-targeted controlled-release tablets comprise a tablet core layer and a controlled-release layer, the controlled-release layer wraps the tablet core layer, the tablet core layer is composed of mesalazine and an auxiliary material pyrodextrin, and the auxiliary material pyrodextrin is a mixture of mesalazine and pyrodextrin. The controlled release layer consists of pyrodextrin, a plasticizer and a pore-foaming agent. By arranging the power assembly, the two efficient stirring assemblies and the two cleaning assemblies can be driven at the same time, attachments on the inner wall of the equipment can be treated while efficient stirring is achieved, by arranging the efficient stirring assemblies, a starch aqueous solution and hydrochloric acid can be mixed more sufficiently and evenly, and the efficiency of the equipment is improved. And through the arrangement of the cleaning assembly, materials attached to the inner wall of the equipment can be scraped away, resources are saved, waste is reduced, and meanwhile the labor intensity of follow-up equipment cleaning is reduced.

This invention discloses a traditional Chinese medicine composition for treating ulcerative colitis, its preparation method, combined drugs, and applications. The traditional Chinese medicine composition for treating ulcerative colitis of this invention is made from the following raw materials in parts by weight: Astragalus membranaceus 13-26 parts, Lonicera japonica 10-20 parts, Sargentodoxa cuneata 10-20 parts, Prunus mume 8-16 parts, Agrimonia pilosa 8-16 parts, Allium macrostemon 6-12 parts, Platycodon grandiflorus 6-12 parts, Coptis chinensis 3-6 parts, and Panax notoginseng powder 1-3 parts. An animal model of ulcerative colitis was constructed using DSS induction, and the results showed that the traditional Chinese medicine composition of this invention has a certain therapeutic effect on ulcerative colitis. Clinical studies showed that the traditional Chinese medicine composition of this invention, used in combination with mesalazine enteric-coated tablets, can reduce the modified Mayo score and serum inflammatory markers in patients with active ulcerative colitis, improve colonic mucosal inflammation and gastrointestinal symptoms, and effectively treat active ulcerative colitis of the damp-heat type.

The invention belongs to the technical field of biological medicines, and particularly relates to application of mesenchymal stem cells combined with mesalazine in preparation of an anti-IBD (infectious bursal disease) medicine. The mesenchymal stem cells are mesenchymal stem cells from human umbilical cord; the human umbilical cord mesenchymal stem cells highly express CD73, CD90 and CD65, and low express CD34, CD45 and HLA-DR (Human Leukocyte Antigen-DR). The research finds that the hUC-MSCs has a remarkable treatment effect on a chronic IBD mouse model when being singly used or combined with 5-ASA for treatment, the hUC-MSCs and drug combination can restore the intestinal microecological balance by adjusting the composition of intestinal flora so as to improve the symptoms of IBD, and the hUC-MSCs and the drug combination have a synergistic effect when being combined with 5-ASA for treatment. The invention provides a new thought and experimental basis for clinical treatment of IBD.

The present invention relates to the technical field of medical, dental or cosmetic preparations, and in particular to a mesalazine enteric-coated sustained-release micro-pill and a preparation method thereof. The mesalazine enteric-coated sustained-release micro-pill comprises the following components: mesalazine, microcrystalline cellulose, a modified guar gum inclusion agent, a binder, and ethyl cellulose. The present invention also provides a preparation method thereof. Compared with the prior art, the enteric-coated sustained-release micro-pill prepared by the present invention has the advantages of intestinal directional release, mildness and no irritation, etc.

A use of oleanolic acid-28-O-β-D-glucopyranoside in the preparation of an anti-colitis drug is provided. The oleanolic acid-28-O-β-D-glucopyranoside has significant anti-ulcerative-colitis activity compared with parent nucleus oleanolic acid and other analogues, and has equivalent efficacy compared with Mesalazine, a first-line drug for the clinical treatment of inflammatory bowel disease, and can also avoid salicylic acid anaphylaxis possibly caused by Mesalazine western medicine treatment, thereby achieving a good application prospect.

The invention discloses a traditional Chinese medicine composition for treating ulcerative colitis, the traditional Chinese medicine composition for treating ulcerative colitis comprises an oral traditional Chinese medicine composition and an enema traditional Chinese medicine composition, and by optimizing the components and the content proportioning relationship among the components and simultaneously matching the components for use, ulcerative colitis ineffective in mesalazine can be improved, and the ulcerative colitis can be effectively treated. The traditional Chinese medicine composition especially improves clinical symptoms and enteroscopy performance of refractory ulcerative colitis, and is remarkable in curative effect, few in side effect and low in recurrence rate.

The invention relates to the field of pharmaceutical preparations, in particular to a preparation process of mesalazine enteric-coated sustained-release granules. The invention discloses a preparation process of mesalazine enteric-coated sustained-release granules. The preparation process comprises the following steps: preparing hydrophobic starch from octenyl succinic anhydride modified starch; chitosan quaternary ammonium salt and starch are used as raw materials to prepare chitosan quaternary ammonium salt modified starch; mixing hydrophobic starch, starch and polyvinyl alcohol to prepare adhesive slurry; loading mesalazine with chitosan quaternary ammonium salt modified starch, adding the adhesive slurry, extruding, rolling, and drying to obtain spherical dry pills; and coating the spherical dry pills to obtain the mesalazine enteric-coated sustained-release granules.

The application belongs to the technical field of medicine synthesis and specifically relates to a preparation method of mesalamine. In the application, ethylene glycol is used to replace water as a reaction solvent in a substitution reaction, the reaction temperature can be increased to 130-140 DEG C, the reaction time is shortened to 3-4 hours, after the substitution reaction is completed, direct cooling and crystallization are carried out, 5-nitrosalicylate is separated, and the mother liquor can be directly used for the next batch of substitution reaction after adding alkali, so that the ethylene glycol and excess alkali can be reused, no waste water and waste liquid are generated, the production cycle is short, the process is simple, the operation is simple, the "three wastes" are less, and the application is green and environmentally friendly.

The present application relates to a kind of pump control administration system and its execution method for mesalamine enema preparation, belong to the technical field of drug delivery and intelligent administration control. Among them, system includes holding / adapting component, drive assembly, controller, user interaction unit;Holding / adapting component is used to position commercial packaging container, so that commercial packaging container is in sealing communication with output passage, and commercial packaging container is in the driving range of drive assembly, drive assembly is used to apply action to commercial packaging container to output liquid medicine;At least one set of candidate delivery parameter set associated with mesalamine enema preparation is stored or called in controller, and a set of target delivery parameters in candidate delivery parameter set is determined, and local safety check is carried out on target delivery parameter;After local safety check passes and user actively confirms, control drive assembly executes output operation according to target delivery parameter. Pumping execution control to mesalamine enema preparation existing commercial package is realized.

The present invention relates to the field of pharmaceutical preparations, and specifically to a preparation process of mesalazine enteric-coated sustained-release granules. The present invention discloses a preparation process of mesalazine enteric-coated sustained-release granules, which uses octenyl succinic anhydride modified starch to prepare hydrophobic starch; uses chitosan quaternary ammonium salt and starch as raw materials to prepare chitosan quaternary ammonium salt modified starch; mixes hydrophobic starch, starch and polyvinyl alcohol to prepare an adhesive slurry; loads mesalazine with chitosan quaternary ammonium salt modified starch, and then adds the adhesive slurry to extrude, spheronize and dry to obtain spherical dry pellets; coats the spherical dry pellets to obtain mesalazine enteric-coated sustained-release granules.

The invention discloses a mesalazine colon-targeted drug delivery transfer system as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The transfer system comprises a mesalazine drug carrier skeleton, an enzyme sensitive component and a pH sensitive coating, the enzyme-sensitive component wraps the outer layer of the mesalazine drug carrier skeleton or is mixed with the mesalazine drug carrier skeleton; the pH-sensitive coating wraps the outer layer of the enzyme-sensitive component or the outer layer of the mixture of the enzyme-sensitive component and the mesalazine drug carrier skeleton. A unique enzyme-sensitive and pH-sensitive double-layer coating technology is adopted, so that enzymatic degradation of mesalazine in a gastric acid environment and the upper section of a small intestine is effectively protected, and early release and whole-body absorption of drugs are remarkably reduced; it is ensured that mesalazine is efficiently and intensively released in the colon environment; the bioavailability of mesalazine in a colon focus is improved, and the local treatment effect is enhanced; the systemic exposure of mesalazine is reduced, and potential systemic adverse reactions are reduced.

The invention relates to carbon monoxide releasing molecules, and methods, compositions and uses relating thereto. Provided is a compound representing a carbon monoxide (CO) releasing variant of Mesalazine (MesaCORM) having a structure according to Formula Ia or Ib; or a pharmaceutically acceptable salt thereof.

This application belongs to the field of biotechnology, and specifically relates to a method for improving the efficacy of wolfberry puree by fermentation with kefir grains and the application of kefir-grain-fermented wolfberry puree in alleviating and treating colitis. The fermented wolfberry puree prepared in this application can significantly improve the inflammatory symptoms and various inflammatory indicators of colitis, and its efficacy is close to or even better than that of the existing mesalazine.

The present invention discloses a mesalazine-tetrandrine hydrochloride drug cocrystal and its preparation method and application, belonging to the technical field of drug crystallization. The structural unit of the drug cocrystal contains mesalazine molecules and tetrandrine hydrochloride molecules, the molar ratio of the two is 1:1, and the molecular formula is [C7H7NO3]·[C 21 H 22 ClNO4]. The present invention mixes mesalazine and tetrandrine hydrochloride hydrate in a solvent at a molar ratio of 1:1, and prepares mesalazine-tetrandrine hydrochloride drug cocrystals through evaporation, mechanical grinding, or suspension stirring. The preparation method is simple and has a high cocrystal yield. The prepared mesalazine-tetrandrine hydrochloride cocrystal has significantly reduced solubility in a pH 1.2 simulated gastric fluid medium and exhibits sustained release behavior in a pH 6.8 simulated intestinal fluid medium. It can effectively increase the contact time of mesalazine and tetrandrine hydrochloride with the inflamed intestinal mucosa and exhibits good inhibitory activity against human colon cancer cells.

The present invention relates to a betulinic acid saponin derivative, a preparation method and an application thereof, and belongs to the field of biomedicine technology. The betulinic acid saponin derivative of the present invention has the general structural formula: 1 Selected from hydroxyl or -O-G, G is a monosaccharide; R 2 Selected from dopamine, 5-aminovaleric acid, 4-aminobutyric acid or 3-aminopropionic acid and their salts. The betulic acid saponin derivative did not show obvious cytotoxicity to THP-1 macrophages, and could significantly reduce the release of IL-6 and IL-1β in LPS-induced THP-1 macrophages. It also has better anti-inflammatory activity, and its therapeutic effect on improving diarrhea and bloody stools in colitis mice is significantly better than that of betulic acid and the positive control drug mesalazine, while its therapeutic effect on dermatitis is better than that of the positive control drug dexamethasone, and there are no obvious toxic side effects such as weight loss and immunosuppression. This shows that the betulic acid saponin derivative has good in vitro and in vivo safety and drugability.