86 results about "Mesylate" patented technology

The invention relates to the technical field of medicines, in particular to a sustained-release coating as well as a preparation method and application thereof. The coating adopts a three-layer gradient structure design and comprises an inner layer coating, a middle layer coating and an outer layer coating, and the layers are compounded and matched through ethyl cellulose and hydroxypropyl methylcellulose with different molecular weights and are combined with talcum powder filling amount with gradient decreasing and a triethyl citrate plasticizer, so that accurate regulation and control of drug release are realized. Through hierarchical swelling-diffusion dynamic balance, burst release is inhibited, the inner layer has high talcum powder content to resist initial swelling stress, the outer layer has low filling amount to maintain hydrophobic continuity, interface defects are reduced in combination with high-temperature curing, and the release stability and long-term storage performance of drugs such as dihydroergoline mesylate are remarkably improved; the problems of sudden release, damp-heat sensitivity, impurity generation and the like of a traditional single-layer coating are solved.

The present invention discloses a method for preparing a linker-drug conjugate and its intermediates. Specifically, a method for preparing compound LE14 is provided, which comprises subjecting an intermediate compound of formula II to an amide condensation reaction with a compound of formula III or its mesylate in the presence of a condensing agent, a base, and a solvent to obtain a compound of formula I. This method can produce a high-purity intermediate II, which is directly condensed with isotecan mesylate to obtain compound I, and then subjected to subsequent reactions to obtain the final product LE14. The preparation method of the present invention has one or more of the following advantages: using intermediate II as the starting material for the production process reduces process steps, facilitates product quality control, significantly reduces impurities in the final product, and improves purity. Furthermore, using the more economical isotecan for the condensation reaction significantly reduces production costs, making it more suitable for industrial production.

The invention relates to the technical field of pharmaceutical preparations, in particular to a solid dispersion-based sustained-release drug composite carrier as well as a preparation method and application thereof. The preparation method comprises the following steps: carrying out synergistic spray drying on double polymers (hydroxypropyl methylcellulose acetate succinate and polyvinylpyrrolidone-vinyl acetate copolymer) to form a solid dispersion; compounding with mesoporous silica and calcium silicate for localization, and spraying ethanol to activate pores; calcium stearate and magnesium stearate are sequentially added for lubrication; prefabricating a sustained-release skeleton master batch; and finally, mixing, rolling and forming. According to the method, through hierarchical structural design, the drug stability, the powder fluidity and the release controllability are remarkably improved, the method is suitable for industrial production of the dihydroergoline mesylate sustained release preparation, and a release curve is smooth and reliable.

The invention provides a bromocriptine mesylate enteric-coated tablet and a preparation method thereof. Specifically, the bromocriptine mesylate enteric-coated tablet comprises a tablet core and an enteric coating layer wrapping the tablet core. The enteric-coated tablet disclosed by the invention is simple in process, good in stability and small in gastrointestinal side effect, the bioavailability of the enteric-coated tablet is more than two times that of a common tablet sold in the market, the dosage is expected to be reduced, the side effect is further reduced, and the enteric-coated tablet has excellent clinical value.

The invention discloses treatment of EGFR mutation positive non-small cell lung cancer brain metastasis by administering an effective dose of an EGFR inhibitor. The EGFR inhibitor is N-(2-((2-(dimethylamine) ethyl) (methyl) amine)-4-methoxy-5-((4-(1-deuterated methyl-1H-indol-3-yl) pyrimidine-N '-2-yl) amine) phenyl) acrylamide mesylate.

The invention belongs to the technical field of chemical analysis, and particularly relates to a method for separating and determining a rucotinib mesylate intermediate Z1 and related impurities thereof. The impurities comprise any one or more of an impurity SM2a, an impurity SM1d, an impurity Z1c, an impurity Z1b, an impurity Z1a, triphenylphosphine oxide, an impurity SM2, an impurity SM1 and an impurity Z1d. Octadecylsilane chemically bonded silica is adopted as a chromatographic column filling agent; a monopotassium phosphate buffer solution is used as a mobile phase A, a mixed solution of methanol and acetonitrile is used as a mobile phase B, and main components are separated from impurities through gradient elution; and detecting in a detector to obtain a chromatogram. The method is high in specificity, short in separation time, high in sensitivity and good in durability, and has important significance on quality control of rukotinib mesylate bulk drugs and preparation products.

Mesylates of heterocyclic cytokinins of general formula I:wherein R is selected from the group comprising C3-C15 cycloalkyl, furfuryl, allyl, 4-hydroxy-3-methylbut-2-en-1-yl, 3-methylbut-2-en-1-yl, 4-hydroxy-3-methylbutyl, 4-hydroxy-1,3-dimethylbut-2-en-1-yl, 4-hydroxy-1,3-dimethylbutyl, benzyl, wherein the cycloalkyl, allyl, benzyl and furfuryl may be unsubstituted or optionally substituted with 1 to 3 substituents selected from the group containing hydroxy, halogen, methyl, hydroxymethyl and methoxy, and salts, solvates and addition salts thereof. These compounds are particularly suitable for agricultural and biotechnological use, and their great advantage is increased water solubility as compared to the corresponding free bases of heterocyclic cytokinins.

The invention discloses a salt form of a coronavirus 3CL protease inhibitor PLC-01 as well as a preparation method and application of the salt form, and belongs to the technical field of medicinal chemistry. Salt types of PLC-01 comprise inorganic acid salt, organic acid salt, sodium salt and a free state. According to the present invention, various organic acids, inorganic acids and solvents are mainly screened so as to obtain the PLC-01 hydrochloride Pattern A, the PLC-01 mesylate Pattern A, the PLC-01 sodium salt Pattern C and the PLC-01 free state Pattern A, wherein the PLC-01 hydrochloride Pattern A, the PLC-01 mesylate Pattern A, the PLC-01 sodium salt Pattern C and the PLC-01 free state Pattern A have characteristics of high purity and good stability; the invention also discloses a pharmaceutical composition of the salt form of the compound shown in the formula I. All salt forms of PLC-01 in the invention have strong inhibition efficacy on 3CL protease, and are expected to become novel active pharmaceutical ingredients for preventing or treating novel coronavirus infection.

The present disclosure relates to a pharmaceutically acceptable salt and a crystal form of a fused pyridine ring derivative and a preparation method therefor. Specifically, the present disclosure relates to a choline salt, sodium salt, potassium salt, calcium salt, arginine salt, lysine salt, meglumine salt, ethanolamine salt, hydrosulfate, hydrochloride, tartrate, maleate, citrate, malate, p-toluenesulfonate, and mesylate, and a crystalline form of a compound as represented by formula (I).

1. Name of the designed product: packaging box (veterinary fleroxacin mesylate injection); 2. Use of the designed product: veterinary drug packaging; 3. Design points of the design: the pattern of the product; 4. Picture or photo best indicating the design points: front view.

The invention discloses a mesoporous polydopamine (MPDA) nanoparticle which is loaded with a CeO2 nano enzyme and mitoxantrone mesylate (MitoQ) and is released by an intestinal tract, a preparation method of the mesoporous polydopamine (MPDA) nanoparticle, and an application of the mesoporous polydopamine (MPDA) nanoparticle, the preparation method of the mesoporous polydopamine (MPDA) nanoparticle, the preparation method of the mesoporous polydopamine (MPDA) nanoparticle and the preparation method of the mesoporous polydopamine (MPDA) nanoparticle, the preparation method of the mesoporous polydopamine (MPDA) nanoparticle, and the preparation method of the mesoporous polydopamine (MPDA) nanoparticle. The mesoporous polydopamine nanoparticle loaded with the CeO2 nano enzyme and the mitoxantrone mesylate and released by the intestinal tract comprises mesoporous polydopamine loaded with the CeO2 nano enzyme and MitoQ, and an enteric coating of chitosan and sodium alginate. The preparation method comprises the following steps: synthesizing mesoporous polydopamine by adopting a triblock copolymer as a template, then loading a small molecular drug MitoQ into MPDA through ultrasonic waves, and loading CeO2 nano-enzyme on the surface of MPDA through metal coordination to form MPDA (at) CeO2-MitoQ. And finally, coating chitosan and sodium alginate on the surfaces of the nanoparticles through electrostatic adsorption to obtain the final MPDA (at) CeO2-MitoQ (at) SA / CS. The drug-loaded nano-particles prepared by the preparation method disclosed by the invention have a good treatment effect on ulcerative colitis.

The present invention relates to a process for the preparation of belumosudil mesylate and its crystalline form. Further, the present invention relates to a 10 pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of belumosudil mesylate obtained by the process of the present invention.

The present invention relates to the field of medical intermediates, and provides a preparation method for a key intermediate tert-butyl (3aR,5S,6aS)-5-(methylamino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxylate mesylate of a JAK kinase inhibitor. The method comprises: reacting tert-butyl cis-5-oxohexahydrocyclopenta[C]pyrrole-2(1H)-carboxylate as a raw material with a methylamine equivalent to obtain intermediate A; and then carrying out a reduction reaction in metallic sodium and isopropanol to obtain a crude product, adding L-DBTA to form a salt, removing isomers, and then carrying out re-liberation and salt formation with methanesulfonic acid to obtain a purified product. The method significantly reduces reaction steps, reduces raw material costs, has a simple and reliable process, and is easy for industrial production.

The invention discloses a synthesis method of 3-amino-2-(tert-butyldimethylsilyl) phenyl trifluoromethanesulfonate, which is characterized in that a compound 2-bromo-3-nitrophenol is used as a raw material, and the target compound 3-amino-2-(tert-butyldimethylsilyl) phenyl trifluoromethanesulfonate is obtained through four-step reaction. According to the synthesis method disclosed by the invention, tert-butyllithium which is commonly used in the prior art is not used in key steps, and bis (trimethylsilyl) amino lithium (LiHMDS) is adopted to convert a compound 3, namely, 2-bromo-3-((tert-butyldimethylsilyl) oxy) aniline into a compound 4, namely, 3-amino-2-(tert-butyldimethylsilyl) phenol; the reaction risk is greatly reduced, meanwhile, the reaction effect is remarkably improved, no by-product is generated, post-treatment and purification are simple, and the yield is ideal.

The invention belongs to the technical field of medicinal chemistry, and relates to a novel crystal form of Lanziatinib mesylate and a preparation method thereof, in particular to a crystal form Q1, a crystal form Q3 and a crystal form Q6 of Lanziatinib mesylate.

The invention belongs to the technical field of environmental protection, and provides a composite particle for treating water floating algae and a preparation method and application thereof, the preparation method comprises the following steps: a, preparing intranuclear active Gemini type biquaternary ammonium cationic polymer mesylate; b, preparing a coating material; c, preparing composite particles: mixing the coating material in the step b with castor oil and sodium bicarbonate, heating and stirring to obtain a coating solution, and adding the Gemini type biquaternary ammonium cationic polymer mesylate prepared in the step a to obtain the composite particles; and d, evaluating the performance of the composite particles. According to the invention, a biodegradable and non-toxic natural polymer material is used as an outer coating, so that slow release and targeted release of quaternary ammonium salt are realized. Quaternary ammonium salt is coated in a compound formed by PVA and chitosan, the release rate of the quaternary ammonium salt is controlled, floating or suspension is realized through density adjustment, and targeted treatment of blue-green algae on the water surface is realized.

Provided herein are salts and solid forms of 1-((S)-4-((R)-7-(6-amino-4-methyl-3-(trifluoromethyl)pyridin-2-yl)-6-chloro-8-fluoro-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)quinazolin-4-yl)-3-methylpiperazin-1-yl)prop-2-en-1-one, including adipate, fumarate, ethylenesulphonate, besylate, and mesylate salts thereof.

The invention relates to the technical field of medicines, in particular to a dihydroergoline mesylate sustained-release tablet containing an antioxidant synergistic system and a preparation method of the dihydroergoline mesylate sustained-release tablet. The preparation method comprises the following steps: firstly, preparing double-molecular-weight polyethylene glycol composite microspheres as a pore-foaming agent; preparing antioxidant regulation particles, forming a buffer microenvironment by tartaric acid, citric acid monohydrate, sodium citrate and the like, and adding a water-soluble antioxidant; then preparing a fat-phase antioxidant skeleton mixture, and loading a fat-soluble antioxidant; preparing drug-containing core particles from dihydroergoline mesylate and a part of the skeleton mixture; and after mixing and tabletting, sequentially carrying out bottom layer hydrophilic film coating, middle powder layer coating and outer layer functional film coating. The sustained release tablet is stable in release within 24 hours and good in batch-to-batch consistency, oxidation impurities in acceleration and long-term stability tests are remarkably reduced, and the medication safety and the long-term effect are effectively guaranteed.

The invention discloses a method for preparing a methanesulfonate product. The method comprises the following steps: in a dichloromethane system, the reaction temperature is controlled to be no higher than 40°C and the reaction rate is controlled, a mixed solution of methanesulfonyl chloride and methanesulfonic anhydride reacts with sodium alkoxide, after the reaction is completed, the reaction solution is cooled to room temperature, filtered, dried, and subjected to rotary evaporation to remove the solvent, and distilled to obtain the methanesulfonate product. The method has a simple synthesis route, does not use an acid binding agent, a phase transfer catalyst or an esterification catalyst, does not require heating, has a short reaction time, and greatly reduces the total production cost in terms of raw materials, production cycle, environmental protection, and the like. The yield and purity of the product prepared by the method are very high, with the yield reaching above 98.2% and the purity reaching above 99.9%. The moisture content of the obtained product is also very low, and the quality of the product obtained by the method far exceeds the product standard for use as an electrolyte.

This invention relates to the field of pharmaceutical technology, specifically to a sustained-release tablet of dihydroergot mesylate with composite network regulation and its preparation method. The sustained-release tablet comprises a composite structure consisting of a drug-resin composite core, an inner interface regulation structure, and an outer composite network. The key to its preparation lies in: forming a wet complex of dihydroergot mesylate with a strongly acidic cation exchange resin; sequentially introducing low-viscosity hydroxypropyl methylcellulose and a first portion of ethyl cellulose to construct the inner interface regulation layer; and after semi-drying, adding high-viscosity hydroxypropyl methylcellulose and a second portion of ethyl cellulose to form the outer composite network framework. This structure can significantly inhibit the burst release of the drug in gastric juice and achieve a stable and sustained release in intestinal juice, with stable tablet quality and good industrialization prospects.

The invention discloses a triazolo ring compound mesylate crystal form as well as a preparation method and application thereof. Specifically, the invention discloses a mesylate crystal form of a compound shown as a formula (I) and a preparation method and application thereof, the mesylate crystal form is selected from a crystal form A-I, the preparation method of the crystal form and a pharmaceutical composition containing the crystal form. The preparation method disclosed by the invention is simple and easy to implement and suitable for industrial large-scale production, and the prepared mesylate crystal form A-I of the compound shown as the formula (I) has good solubility and stability and is beneficial to preparation and storage of pharmaceutical preparations.

The invention relates to the technical field of pharmaceutical preparations, in particular to a lenvatinib mesylate capsule and a preparation method thereof. In order to overcome the problem of dissolution of the lenvatinib mesylate capsule, an aqueous solution of an alkaline anti-gel agent is adopted for granulation, and the water adding amount in the granulation process is controlled, so that on one hand, the particle size can be increased, the particle fluidity is further improved, and industrial production is facilitated; on the other hand, the dissolution rate of the lenvatinib mesylate capsule can be improved, so that the bioavailability is improved. The lenvatinib mesylate capsule preparation prepared by the method disclosed by the invention is high in dissolution rate, more controllable in product quality, simple in preparation process and suitable for industrial production.

The invention discloses application of tetrahydronaphthalene [1, 2-b] furan-2 (3H)-ketone in preparation of drugs for treating inflammatory bowel diseases, and belongs to the field of drug synthesis. The tetrahydronaphthalene [1, 2-b] furan-2 (3H)-ketone and the mesylate thereof can remarkably improve disease symptoms of mice and rats with colitis, have a regulating effect on CD4 + T cell subgroups, reduce the proportion of Th1 and Th17 cells in mesenteric lymph nodes, up-regulate the proportion of Treg cells and recover the immune homeostasis mediated by the CD4 + T cells. The invention provides a new medicine choice for treating the inflammatory bowel disease.

The compound can be used for preparing an intermediate and related compounds of iprotecan mesylate. Further provided are methods for preparing these compounds. Also provided are improved, scalable synthesis of iprotecan mesylate using the provided intermediates. The synthesis of iprotecan mesylate utilizes a convergent pathway, includes fewer steps and utilizes fewer reagents and improves efficiency.

The present invention relates to an improved process for the preparation of Belumosudil mesylate compound of formula-1a and its intermediates which is represented by the following structural formula: Formula-1a.

The invention provides a crystal form of a compound shown in a formula I or a salt thereof. The crystal form is an equivalent mesylate crystal form A of a compound as shown in a formula I, a crystal form D of the compound as shown in the formula I, an equivalent maleate crystal form A of the compound as shown in the formula I, an equivalent tartrate crystal form C of the compound as shown in the formula I, an equivalent citrate crystal form B of the compound as shown in the formula I or an equivalent succinate crystal form D of the compound as shown in the formula I; the crystal form has one or more of the following advantages: high crystallinity, good stability, low hygroscopicity, high solubility and high bioavailability. # imgabs0 #

The present invention relates to the field of chemical pharmaceutical technology, and specifically discloses a preparation method of nafamostat mesylate. 6-amidino-2-naphthol mesylate, p-guanidinobenzoic acid hydrochloride and EDCI are added to a first solvent to carry out a condensation reaction; then a saturated sodium bicarbonate aqueous solution is added to obtain an intermediate; the intermediate is added to a second solvent, and then methanesulfonic acid is added to form a salt, and purified to obtain nafamostat mesylate. EDCI first reacts with the first solvent to be activated, and the oxygen atom on the carbonyl carbon of the carboxylic acid is positively charged in the activated EDCI, thereby increasing the electrophilicity of the carboxylic acid and forming an active intermediate, making it easier for it to undergo a nucleophilic substitution reaction with an alcohol, and undergoing dehydration condensation to form an ester bond. The present invention uses EDCI as a condensing agent, improves the production efficiency and yield of nafamostat mesylate, improves the purity of nafamostat mesylate, reduces the impurity content, and is low in cost and easy to industrialize.

The utility model discloses a nitrogen filling device for nafamostat mesylate for injection, including the cabinet body and setting in the cabinet body downside for the foot stand of mobile, the rear upper side four corners of cabinet body are provided with slide rod respectively, the upper side of slide rod is provided with nitrogen filling tank, the front lower side of nitrogen filling tank is provided with the air pump box, the front lower side of air pump box is provided with nitrogen filling pipe, the downside bottom of nitrogen filling pipe is provided with the sealing plug, the front upper side of cabinet body is provided with the placing tray, the upper side inside of placing tray is provided with a plurality of placing mouth with equidistance annular array, this novel mainly helps chuck, spring, trigger ball's mechanical linkage, and the whole process of " putting in - clamping - loosening - taking out " of the penicillin bottle does not need manual intervention. The chuck area opens automatically when placing, which is convenient for feeding. After rotating, it is automatically clamped to ensure process stability. After processing, it is automatically loosened to facilitate unloading, which greatly improves the production line turnover efficiency.