22 results about "Methylprednisolone" patented technology

The present disclosure relates to the use of cortisol, cortisone, cortisone acetate, hydrocortisone, fludrocortisone, prednisolone, prednisone, methylprednisolone, Dehydroepiandrosterone (DHEA), dexamethasone, betamethasone, adrenocorticotropic hormone (ACTH), ganaxolone, tetracosactide or combinations thereof for preventing and / or reducing the risk of Sudden Unexpected Death in Epilepsy (SUDEP). The disclosure further provides pharmaceutical compositions and methods for preventing and / or reducing the risk of SUDEP, particularly in Dravet Syndrome patients.

The present invention discloses the use of combined GC triamcinolone enema in the treatment of immune checkpoint inhibitor-related immune enteritis. The present invention proves through clinical trial cases that intravenous administration of GC methylprednisolone combined with (triamcinolone) enema administration is beneficial to the improvement of the condition of immune checkpoint inhibitor-related immune enteritis. Therefore, combined GC (triamcinolone) enema can be used in related fields such as immune checkpoint inhibitor-related immune enteritis. The present invention provides a new drug and treatment idea for the treatment of immune checkpoint inhibitor-related immune enteritis; the present invention opens up a new use for GC (triamcinolone) enema administration and provides a new treatment method for immune checkpoint inhibitor-related immune enteritis, having good clinical application prospects. The combined medication scheme provided by the present invention has been fully clinically verified in terms of its effectiveness and safety; it is easily acceptable to patients and has unique advantages.

The invention discloses an efficient mouse small intestine epithelial cell isolated culture method. The method comprises the steps of fetal mouse small intestine tissue obtaining, flushing digestion, sediment obtaining through centrifugal separation, density gradient centrifugal purification, differential adhesion method purification, inoculated culture and culture medium replacement for further culture. During culture, a first culture medium and a second culture medium based on William's E basic culture media are sequentially used, and the first culture medium comprises fetal calf serum, EGF, L-glutamine, mannitol, methylprednisone, bovine insulin and double antibodies; the second culture medium is prepared from fetal calf serum, vitamin C, L-glutamine, resveratrol, sodium pyruvate, bovine insulin and double antibodies. The rapid adherent proliferation and long-term stable culture of the mouse small intestine epithelial cells on the 2D surface are realized through mutual cooperation of the two culture media, so that the separation and in-vitro culture method of the mouse small intestine epithelial cells, which is simple, easy to operate, stable and efficient, is established, and convenience is provided for metabolic research of various in-vitro drugs and inflammatory factors.

The invention provides a double-acting phase-change carrier-free nanoparticle based on L-menthol and a preparation method and application thereof.According to the nanoparticle, a solution of lauric acid mixed with methylprednisolone and L-menthol is dripped into a heated hydrogenated lecithin dispersion liquid, the self-assembly process of the nanoparticle is carried out, and the nanoparticle is prepared. The preparation method comprises the following steps: firstly preparing nano-particles, then rapidly cooling to quench the reaction, then removing the nano-particles which are not successfully assembled in a rewarming stirring manner to obtain the required nano-particles, and regulating a spinal cord injury immune microenvironment and repairing a blood spinal cord barrier in an in-situ injection manner to achieve the effect of treating the spinal cord injury.

The present invention discloses a steroidal dihydropyrazole thiazoline derivative, 3β-hydroxy-pregnane-5-en-17β-yl-5'-(substituted phenyl)-1'-(4''-phenyl-[1'',3'']-thiazol-2''-yl)-4',5'-dihydropyrazole-3'-yl. The present invention also discloses the use of the steroidal dihydropyrazole thiazoline derivative. The steroidal dihydropyrazole thiazoline derivative of the present invention has a strong inhibitory effect on nitric oxide (NO) production in RAW 264.7 mouse peritoneal macrophages induced by lipopolysaccharide (LPS), especially compound 4 in the prepared steroidal dihydropyrazole thiazoline derivative has an IC of 0.05. 50 The value is better than that of the positive control methylprednisolone, and the toxicity to cells is low. The steroidal derivative containing a dihydropyrazole thiazoline heterocycle provided by the present invention is a new structural compound, which shows higher activity than existing first-line anti-inflammatory drugs.

The invention discloses application of quercidic acid in preparation of a medicine or a medicine composition for preventing or treating diseases or symptoms related to excessive glucocorticoid. According to the application disclosed by the invention, the protective effect of the quercidic acid on the GIONFH is verified through a preclinical model, and evidence that the quercidic acid can be applied to prevention or treatment of the GIONFH is provided. Animal experiments prove that the quercidic acid can inhibit methylprednisolone-induced rat GIONFH, and the action mechanism is related to inhibition of osteoclasts. The medicine or the medicine composition described by the invention can obviously improve the formation of necrotic fossa in femoral head of GIONFH, bone loss of bone trabecula, CTSK positive cell expression, osteoclast formation, bone resorption protein expression and osteoclast overactivity at a lower dosage, and provides a potential prevention and treatment scheme for treatment of GIONFH.

The present invention discloses a carbonyl reductase mutant and its application in synthesizing 11β-hydroxysteroid compounds. Carbonyl reductase derived from Homo sapiens is modified by semi-rational design methods to provide a carbonyl reductase mutant. The mutant can efficiently catalyze the synthesis of 11β-hydroxysteroid compounds prednisolone, hydrocortisone and methylprednisolone using prednisone, cortisone and methylprednisolone as substrates.

The invention relates to the technical field of pharmaceutical preparations, in particular to a methylprednisolone pulse micro-tablet and a preparation method thereof. The methylprednisolone pulse microtablet comprises a quick release tablet core and a coating layer, the quick-release tablet core comprises methylprednisolone, a filler, an antistatic agent A, an antistatic agent B, an adhesive and a lubricant; the coating layer comprises a coating material and a plasticizer; wherein the antistatic agent A is selected from at least one of a combination of organic acid and bicarbonate or ammonium carbonate; the antistatic agent B is selected from at least one of polyoxyethylene, carbomer, high-expansion type pregelatinized starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, croscarmellose sodium and crospovidone. The antistatic agent A and the antistatic agent B have a synergistic effect, so that the electrostatic phenomenon can be effectively reduced, and particle adhesion and microchip agglomeration are avoided.

The invention relates to a preparation method of methylprednisolone or a derivative thereof, which comprises the following steps: mixing a compound 1, methanol, acetone cyanohydrin and a potassium carbonate solution, and reacting to obtain a compound 2; mixing the compound 2, dichloromethane, piperidine, imidazole and chloromethyl dimethyl chlorosilane, and reacting to obtain a compound 3; adding a lithium diisopropylamide solution into a mixed solution of a compound 3 and tetrahydrofuran, and reacting; adding into the mixed solution, keeping the temperature, heating, reacting and treating to obtain a compound 4; mixing the compound 4, N, N-dimethylformamide, potassium acetate, water and acetic acid, and reacting to obtain a compound 5; adding a liquid alkali solution into a mixed solution of the compound 5, dichloromethane and methanol, and carrying out heat preservation and reaction to obtain a compound I; according to the method disclosed by the invention, the cost of the raw materials is reduced, the pollution is reduced, and the yield and the purity of the product are improved.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a preparation method of methylprednisolone and an intermediate compound thereof. The preparation method comprises the following steps: by taking cortisone as a raw material, carrying out 17 and 21 site upper protecting groups and 3 site upper protecting groups, and carrying out reduction, so as to obtain a methylprednisolone intermediate compound shown as a formula V; and carrying out 5 and 6-site epoxidation, Grignard reaction, 3-site protecting group removal, 4 and 5-site dehydration elimination, 1 and 2-site dehydrogenation and 17 and 21-site protecting group removal on the compound in the formula V to obtain methylprednisolone. The structural formula of the compound of formula V is shown in the specification. The preparation process has the advantages of high yield, high purity, low cost, simplicity in operation and suitability for industrial production.

The invention belongs to the field of biological analysis of medicines, and particularly relates to a biological analysis method for determining concentrations of methylprednisolone aceponate and metabolites thereof in blood plasma, and the method is a liquid chromatography-tandem mass spectrometry method. The method for simultaneously detecting the plasma concentration of methylprednisolone aceponate and the metabolite 6 alpha-methylprednisolone 17-propionate thereof in the plasma is the only disclosed method at present, and can be used for supporting non-clinical and clinical research work of the medicine.

The invention provides an application of metformin in preparation of a medicine for preventing or treating immune checkpoint inhibitor related colitis. It is found through experiments that when the immune checkpoint inhibitor causes colitis, change of metabolic level represented by glycolysis caused by change of a PI3K / AKT / mTOR pathway in the colon is obviously accompanied, then Treg / Th17 steady state in the colon is affected, and a high inflammatory state is shown in the colon. According to the present invention, the influence on glycolysis and other metabolic pathways is achieved through the targeted interference of the metformin on the PI3K / AKT / mTOR pathway, the colitis caused by the immune checkpoint inhibitor can be significantly improved, the anti-tumor drug effect of the immune checkpoint inhibitor is not affected, and the method is generally superior to the original clinical methylprednisolone intervention scheme.

The invention discloses a methylprednisolone-loaded cell membrane bionic liposome atomization preparation. The atomization preparation comprises methylprednisolone-loaded cell membrane bionic liposome, a liposome membrane stabilizer and a buffer solution of a pH regulator, the invention also discloses a preparation method of the methylprednisolone-loaded cell membrane bionic liposome atomization preparation. The invention also discloses an application of the methylprednisolone-loaded cell membrane bionic liposome atomized preparation in preparation of drugs for treating acute lung injury or asthma, and an application of the methylprednisolone-loaded cell membrane bionic liposome atomized preparation as a carrier of targeted drugs in preparation of drugs for treating acute lung injury. The atomization preparation provided by the invention can realize local drug delivery so as to realize pulmonary drug delivery, and the drug action efficiency is improved.

This invention relates to a lipid nanoparticle delivery system, its preparation method, and its applications, belonging to the fields of biomedicine and vaccine technology. The lipid nanoparticles include immunomodulatory components, cationic lipids, helper phospholipids, sterol lipids, and polyethylene glycol-modified lipids, wherein the immunomodulatory component is methylprednisolone or squalene. When the immunomodulatory component is methylprednisolone, LNPs exhibit higher levels of cytokines related to the activation of innate immunity, suggesting enhanced humoral immune responses. When the immunomodulatory component is squalene, LNPs exhibit higher muscle retention, suggesting potentially higher biocompatibility, better immunogenicity, and enhanced T-cell responses.

The invention discloses a carbonyl reductase mutant and application of the carbonyl reductase mutant in synthesis of 11 beta-hydroxy steroid compounds, carbonyl reductase from Homo sapiens is modified by a semi-rational design means, the carbonyl reductase mutant is provided, prednisone, cortisone and methylprednisone are used as substrates, and the carbonyl reductase mutant is synthesized by a one-step method. And the 11 beta-hydroxy steroid compounds such as prednisolone, hydrocortisone and methylprednisolone are efficiently and catalytically synthesized.

The invention relates to the field of medicines, and particularly discloses a method for treating rheumatoid arthritis (RA) by combining statins and glucocorticoids. According to the method, statins (such as atorvastatin, rosuvastatin, simvastatin and the like) and glucocorticoids (such as prednisone, methylprednisolone, dexamethasone and the like) are jointly applied to RA patients, so that the anti-inflammatory and immunoregulation effects are enhanced, and meanwhile, the adverse reaction of the glucocorticoids is reduced. Animal experiments and clinical research show that the pharmaceutical composition can effectively inhibit an NF-kappa B signal channel, reduce the level of inflammatory factors (such as CRP and ESR), improve synovitis, reduce joint injury and reduce RA-related cardiovascular risks. In addition, the combined treatment can reduce the dosage of glucocorticoid, so that side effects (such as osteoporosis, hypertension, hyperglycemia and the like) caused by long-term use of the glucocorticoid are reduced. The invention provides a safe and effective RA combined treatment strategy which can be used for clinical treatment of RA and has important application value.

The invention discloses a methylprednisolone dimer impurity and a separation and purification method thereof. The invention provides a compound as shown in a formula I and / or a compound as shown in a formula II. The two methylprednisolone dimer impurities provided by the invention are not reported, are detected in the product, and are of great significance to product quality control.

The invention provides an external parasite prevention and control agent for animals. The external parasite prevention and control agent comprises the following components in percentage by mass: 6-12% of fipronil; 1 to 5% of moxidectin; 1-3% of pyriproxyfen; 1-3% of a crystallization inhibitor; 0.3%-0.6% of an antioxidant; 3-5% of a main solvent; the total percentage is 100%. The fipronil is taken as a main effective component, and moxidectin and pyriproxyfen are cooperatively matched, so that the fipronil-containing insecticidal composition has a good insecticidal effect, and the problems that an existing insecticide is poor in insecticidal effect and cannot thoroughly kill ticks, mites and the like are solved; particularly, the animal external parasite control agent comprises 10% of fipronil, 1% of moxidectin, 1.8% of pyriproxyfen, 2% of propylene glycol, 0.1% of BHT, 0.2% of BHA, 3% of absolute ethyl alcohol, 2% of dimethyl sulfoxide and a proper amount of diethylene glycol monoethyl ether, and the insecticidal effect is particularly good.

The application discloses a traditional Chinese medicine composition for treating nodular erythema, which is prepared from the following raw materials in a proportion by weight: 3-15 parts of Bupleurum, 3-20 parts of Artemisia annua, 3-15 parts of Angelica sinensis, 3-15 parts of Radix Angelicae Pubescentis, 3-20 parts of Cynanchum, 3-15 parts of Notopterygium, 3-20 parts of Fructus Kochiae, 3-15 parts of Cnidium, 3-20 parts of Alnus, 3-10 parts of Glycyrrhiza, 3-20 parts of Salvia miltiorrhiza, 3-15 parts of Saposhnikovia divaricata, 3-15 parts of Paeonia suffruticosa, 3-10 parts of honeycomb, 3-12 parts of Tripterygium wilfordii, 5-30 parts of Crataegus pinnatifida, and 5-30 parts of Sorsastrum hemningsii. The composition can fade the skin rash and nodular erythema, has a low recurrence rate, and is superior to methylprednisolone which is commonly used in the clinic. The application can effectively treat the nodular erythema related to connective tissue disease, and has the clinical popularization and application value.

The invention discloses a preparation method of a composite scaffold for multi-period controlled release of methylprednisolone. The composite scaffold is composed of chitosan hydrogel loaded with methylprednisolone and a polycaprolactone fiber membrane loaded with methylprednisolone. The preparation method of the methylprednisolone-loaded polycaprolactone fiber membrane comprises the following steps: mixing polycaprolactone particles with methylprednisolone, dissolving by using a mixed solution of trichloromethane and methanol, and preparing the solution into the fiber membrane by using an electrostatic spinning technology. And mixing the chitosan hydrogel loaded with the methylprednisolone with a polycaprolactone fiber membrane to prepare the composite scaffold. The preparation method is simple in process and low in cost, in-vitro drug release experiment research shows that the controlled release effect of methylprednisolone can be used for marking a clinical treatment scheme, and cell experiments and animal experiments prove that the composite scaffold has the advantages of biocompatibility, inhibition of inflammatory factor release, inhibition of M1 type polarization of immune cells and the like.

The present invention discloses a dehydrogenase mutant and a method for preparing methylprednisolone dehydroproduct by using the same. The amino acid sequence of the dehydrogenase is shown as SEQ ID NO: 2; the dehydrogenase mutant has amino acid residue differences at one or more sites selected from the following positions in the amino acid sequence shown as SEQ ID NO: 2: position 315, position 330, or positions 452-463. The method for preparing methylprednisolone dehydroproduct by using the dehydrogenase mutant comprises one or more of the following steps: mixing an enzyme solution or pure enzyme containing the dehydrogenase mutant with methylprednisolone Grignard reagent; reacting at pH 7.5 and 35°C with stirring. The method provided by the present invention has the advantages of a simple reaction system, a short conversion period, few side reactions, and low cost.