45 results about "Mycophenolic acid" patented technology

The invention discloses application of an active compound in an anti-cataract drug, and particularly relates to the field of drugs. The active compound is lenalidomide, mycophenolic acid, glycyrrhetinic acid or bromfenac sodium hydrate. Through a solution based on a CRYAB structure and animal experiment screening, it is found that the active compound can serve as an effective component of an anti-cataract drug, the progress of cataract can be remarkably relieved or inhibited, and a new strategy and potential drug selection are provided for treatment of cataract.

The application discloses a kind of rice mycotic acid hapten and antigen preparation application, it is related to antigen preparation technical field, introduce sulfydryl in the 2 of rice mycotic acid, and obtain rice mycotic acid antigen by coupling with protein through connecting arm, rice mycotic acid hapten and antigen preparation application include the following specific flow: S1, the synthesis of rice mycotic acid hapten;S2, the preparation of rice mycotic acid immunogen;S3, the preparation of rice mycotic acid coating original;S4, the preparation of rice mycotic acid monoclonal antibody;S5, the preparation of rice mycotic acid immunofluorescence detection card;S6, rice mycotic acid detection in food;S7, detection limit experiment;S8, false positive rate, false negative rate experiment.The rice mycotic acid hapten retains the structural characteristics of rice mycotic acid, better exposes rice mycotic acid structural characteristics, improves the immunity and immune recognition ability of antigen, lays foundation for preparing specific, high sensitivity antibody, and improves its rapid detection ability.

The application belongs to the field of medicine and chemical industry, and discloses a mycophenolic acid medicine co-crystal and a preparation and application thereof. The co-crystal is prepared from mycophenolic acid and 4,4-bipyridine as raw materials. The co-crystal is a stoichiometric ratio diversity co-crystal. In the molecular structure of the co-crystal, the amount of substance of mycophenolic acid and 4,4-bipyridine is 1:1 or 2:1. The two kinds of mycophenolic acid medicine co-crystals prepared by a grinding method, a room temperature evaporation method or a slurry method are diversity co-crystals, and the diversity of the mycophenolic acid co-crystal has never been reported. The application solves the problems of poor stability and high hygroscopicity of mycophenolic acid, and the prepared co-crystal has low hygroscopicity and good stability.

The fermentation medium for producing mycophenolic acid comprises methionine, a carbon source and a nitrogen source, and the nitrogen source does not comprise a composite organic nitrogen source. According to the fermentation medium and the fermentation method disclosed by the invention, the titer of producing mycophenolic acid by utilizing penicillium brevicompactum is obviously improved, especially when the concentration of methionine is 1.5 g / L, the fermentation titer can be improved to 9214 mu g / mL, and the fermentation titer can reach 13506 mu g / ml due to the development of a feeding process.

The invention provides a genetic engineering strain of high-yield immunosuppressant mycophenolic acid as well as a preparation method and application of the genetic engineering strain. The invention firstly provides a method for constructing the penicillium with the effect of high yield of mycophenolic acid. The method comprises the step of replacing an indigenous promoter of acyl-coenzyme A oxidase PbACOX323 protein participating in beta oxidation in peroxisome of a penicillium strain with a promoter PgpdA of 3-phosphoglycerol dehydrogenase with an amino acid sequence of SEQ ID NO: 1. According to the method disclosed by the invention, the genetically engineered bacterium with high yield of mycophenolic acid is constructed, the yield of mycophenolic acid is positively increased by replacing a promoter of acyl-coenzyme A oxidase PbACOX323, and the method has a good industrial application value.

The present invention belongs to the field of detection of mycophenolic acid blood drug concentration, and specifically relates to a method for quantitatively detecting mycophenolic acid in trace blood by high performance liquid chromatography-tandem mass spectrometry, which comprises the following steps: after adding an internal standard solution to the plasma sample to be tested, adding a mixed solution of KH2PO4 and EDTA, the pH value of the mixed solution is 8-9, and mixing evenly; adding a propionic anhydride solution to the evenly mixed system, oscillating and reacting, centrifuging, and taking the supernatant for LC-MS / MS detection. Mycophenolic acid has a phenolic hydroxyl group, and under certain pH value and temperature, it undergoes an esterification reaction with propionic anhydride, and the derivative product is [M + CH3CH2CO] + peak, which simultaneously solves the problem that the sample volume is too low to affect the sensitivity, and reduces the interference of other substances.

Provided is a means for quantitative analysis of an analyte including mycophenolic acid and one or more other immunosuppressants using a whole blood fraction without requiring separation of a blood sample. One embodiment of the present invention relates to a method for quantifying an analyte including mycophenolic acid and one or more other immunosuppressants in a blood sample of a subject, the method comprising: an analyte concentration measurement step for measuring the concentration of the analyte; measuring the concentration of an analyte including mycophenolic acid and one or more other immunosuppressants in the whole blood fraction of the blood sample; a hematocrit value acquisition step for acquiring the hematocrit value of the target blood sample; and a mycophenolic acid concentration conversion step for converting the concentration of mycophenolic acid in the whole blood fraction of the blood sample into the concentration of mycophenolic acid in the plasma fraction of the blood sample on the basis of the hematocrit value.

Disclosed herein are pharmaceutical compositions in the form of a suspension for oral delivery. Some embodiments provide a pharmaceutical composition in the form of a suspension for oral delivery comprising an active pharmaceutical ingredient; water, a suspending agent; a buffering agent; and one or more of a wetting agent and a binder / filler. In some embodiments, the active pharmaceutical ingredient is selected from quetiapine, sildenafil, tadalafil, cinacalcet, ticagrelor, mycophenolate, aprepitant, zonisamide, and primidone.

The present application relates to a kind of mycophenolic acid detection reagent and its preparation and detection method, specifically a kind of mycophenolic acid chemiluminescence immunoassay reagent and its preparation and detection method, comprising: anti mycophenolic acid specific antibody, for detecting the indicating reagent of anti mycophenolic acid specific antibody-mycophenolic acid combination;The above anti mycophenolic acid specific antibody is obtained by mycophenolic acid immunogen immunization animal.The present application has the advantages that: the mycophenolic acid immunogen of the present application is specific, and immunogenicity is high, and the prepared anti mycophenolic acid specific antibody is specific, and titer is high;Chemiluminescence immunoassay reagent containing the above anti mycophenolic acid specific antibody can determine the mycophenolic acid content in sample conveniently, quickly and accurately, and multiple samples can be simultaneously determined on full-automatic chemiluminescence immunoassay analyzer, realize the high-throughput rapid determination of mycophenolic acid, and the accuracy is high, and the specificity is strong, and accuracy and detection efficiency have been greatly improved.

The application provides a preparation method of sodium mycophenolate, which comprises the following steps: mixing mycophenolic acid crystals and first methanol, and obtaining first filtrate after first filtration treatment; mixing the first filtrate and a solid acid catalyst, and reacting at 50-55 DEG C until the content of mycophenolic acid is lower than 1%, and obtaining second filtrate after second filtration treatment; obtaining third filtrate after decolorization treatment and third filtration treatment of the second filtrate; obtaining first crystalline body after first crystallization treatment of the third filtrate; mixing the first crystalline body and second methanol, then adding sodium hydroxide and water, and reacting at 60-64 DEG C until the content of mycophenolate methyl ester is lower than 0.5%, and obtaining sodium mycophenolate concentrate after second crystallization treatment and reduced-pressure drying. By controlling the reaction degree of esterification and hydrolysis reactions and reasonably matching each step, the purity and yield of sodium mycophenolate can be improved.

The invention provides application of mycophenolic acid methyl ester in preparation of antithrombotic drugs, and belongs to the technical field of antithrombotic drugs. The antithrombotic activity of the compound mycophenolic acid methyl ester is found for the first time, and experimental support and theoretical basis are provided for developing novel drugs for treating or preventing thrombus.

The culture medium comprises methionine, a carbon source, a nitrogen source and a phosphorus source, and the contents of the methionine, the carbon source, the nitrogen source and the phosphorus source in the culture process are 0.3-0.5 g / L, 180-230 g / L, 19-27 g / L and 3-5 g / L respectively. The optimized culture medium for improving the yield of the intracellular antibiotics can be used for fermenting penicillium brevicompactum to produce mycophenolic acid, and the titer of the penicillium brevicompactum for producing the mycophenolic acid can be obviously improved in a short time by utilizing the optimized culture medium and the fermentation method which are prepared by the invention; by utilizing the culture medium prepared by the invention, the activity of the mycophenolic acid produced by the mould in the penicillium brevicompactum can be improved.

The application discloses a kind of compositions for inhibiting uridine diphosphate glucuronosyltransferase 1A9 activity and application thereof, belong to medical technology field.The composition includes two kinds or more in alpha-antiarol, beta-antiarol, gamma-antiarol, garcinia C, garcinia D, 8-deoxy-garcinol, garcinol and 3-isoantiarol.The application verifies by experiment that the extract of fruit mountain bamboo has higher affinity and stronger inhibitory activity to UGT1A9 in alpha-antiarol, beta-antiarol, gamma-antiarol, garcinia C, garcinia D, 8-deoxy-garcinol, garcinol and 3-isoantiarol, and the components have higher biological activity and safety, can be used as the selective inhibitor of UGT1A9, to inhibit the metabolism of clinical immunosuppressive drug mycophenolic acid, increase mycophenolic acid exposure, prolong the half-life of mycophenolic acid, improve mycophenolic acid efficacy.

The invention provides a construction method of a precise medication model for mycophenolic acid drugs, a prediction device and electronic equipment. Belongs to the cross technical field of precision medicine and pharmacology. The construction method of the precise medication model for the mycophenolic acid drugs comprises the following steps: S1, acquiring clinical data of a patient; s2, collecting blood samples at different time points after the patient takes the medicine, and detecting the blood concentration of the mycophenolic acid medicine; s3, the non-atrioventricular model is used as a basic model, multiple linear regression analysis is carried out, a precise medication model for the mycophenolic acid drugs is established, and a mathematical model of the precise medication model for the mycophenolic acid drugs is shown as a formula (1). By the adoption of the accurate medication model for the mycophenolic acid drugs, the blood sampling frequency for monitoring the blood concentration of the mycophenolic acid drugs can be reduced, the workload of medical workers is reduced, the pain of patients is relieved, and the compliance of the patients is improved.

Method to remove mycophenolic acid (MPA) from an alkaline MPA-containing antibiotic mycelial fermentation residue (AMFR), includes: subjecting an alkaline MPA-containing AMFR to a heat treatment in pr

A combination comprising tilorone / nelfinavir; tilorone / molnupinavir; tilorone / remdesivir; tilorone / alfacalcidol: tilorone / clofazimine; tilorone / danazol; tilorone / manidipine; tilorone / sertraline; tilorone / trifluoperazine; remdesivir / hexachlorophene; remdesivir / mycophenolate; mycophenolate / hexachlorophene; mycophenolate / nelfinavir; or mycophenolate / nitazoxanide. This combination can be used for blocking the replication of a coronavirus in a coronavirus-infected cell, for treating an infection by a coronavirus in a subject, for treating a coronavirus-related disease in a subject, and / or for reducing the risk of developing a coronavirus-related disease or the severity of a coronavirus-related disease in a subject.

This invention discloses the application of fluorescent carbon dots for mycophenolic acid detection, relating to the field of drug content detection technology. The carbon dot preparation method includes the following steps: adding β-cyclodextrin and L-phenylalanine to deionized water, ultrasonically mixing, and performing a hydrothermal reaction to obtain a reaction solution; cooling to room temperature, and then sequentially filtering, dialyzing, and freeze-drying to obtain fluorescent carbon dots for mycophenolic acid detection. This invention uses water as the reaction solvent and employs a one-step hydrothermal method to synthesize fluorescent carbon dots, which have been successfully applied to the sensing and determination of mycophenolic acid with good results. It offers advantages such as convenient construction, high sensitivity, good specificity, and ease of use. This invention solves the problems of complex operation, high cost, and low accuracy in existing methods for mycophenolic acid content detection.

The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, and relates to a nano preparation for targeting glioblastoma, and preparation and application thereof, in particular to a nano preparation of chlorambucil-mycophenolic acid prodrugs for targeting glioblastoma, especially temozolomide drug-resistant glioblastoma, and preparation and application thereof. According to the invention, firstly, a chlorambucil-mycophenolic acid prodrug or a pharmaceutically acceptable salt thereof is constructed, and then on the basis, a prodrug co-assembled nano preparation capable of realizing synergistic delivery of three drugs, namely chlorambucil, mycophenolic acid and MHY1485, is constructed. Meanwhile, the prodrug co-assembled nano preparation is subjected to targeted modification, so that the prodrug co-assembled nano preparation is endowed with the capability of crossing a blood brain barrier. A targeting peptide modified nano-drug delivery system is constructed through a prodrug co-assembly technology, blood brain barrier crossing and accurate delivery of drugs to tumor sites are achieved, and the synergistic anti-tumor effect of a drug combination is remarkably improved.

Low viscosity pharmaceutical compositions and methods for treating ocular disorders in a subject, which include mycophenolic acid or a pharmaceutically acceptable salt thereof at a concentration of 0.05% wt / wt to 0.30% wt / wt, a glucosaminoglycan at a concentration of 0.1% to 2.5% wt / wt, and optionally a betamethasone at a concentration of 0.01% to 0.08% wt / wt.

The invention discloses a method for rapidly and quantitatively detecting mycophenolic acid (MPA) in a trace serum sample by high performance liquid chromatography-tandem mass spectrometry, which comprises the following steps: pretreating the trace serum sample by a protein precipitation method, separating MPA from interference components in a serum matrix by high performance liquid chromatography, detecting MPA by mass spectrometry, and quantifying by an isotope internal standard method. The horizontal axis is the concentration of the mycophenolic acid standard solution, and the longitudinal axis is the peak area ratio of the mycophenolic acid to the internal standard of the mycophenolic acid, constructing a calibration curve, obtaining a regression equation and a correlation coefficient, and calculating the content of MPA. The method for quantitatively detecting mycophenolic acid in serum, provided by the invention, has the advantages of low venous blood sampling amount, trace serum detection, low detection cost, simplicity and rapidness in operation and accurate result, and solves the problems of low removal efficiency of impurities such as protein and the like and unstable matrix effect or recovery rate.

Disclosed herein are pharmaceutical compositions in the form of a suspension for oral delivery. Some embodiments provide a pharmaceutical composition in the form of a suspension for oral delivery comprising an active pharmaceutical ingredient; water, a suspending agent; a buffering agent; and one or more of a wetting agent and a binder / filler. In some embodiments, the active pharmaceutical ingredient is selected from quetiapine, sildenafil, tadalafil, cinacalcet, ticagrelor, mycophenolate, aprepitant, zonisamide, and primidone.

The application discloses a fluorescence resonance energy transfer probe system and a method for high-sensitivity homogeneous immuno-detection of mycophenolic acid in whole blood. The application uses NaYbF4:Tm nanocrystals marked with BA monoclonal antibody on the surface as a donor probe, NaDyF4 nanocrystals marked with BA antigen on the surface as an acceptor probe, and constructs a fluorescence resonance energy transfer probe system. The probe system is used for qualitative and quantitative detection of mycophenolic acid in whole blood. The donor probe is incubated with a whole blood sample to be detected, and the fluorescence intensity emitted at 800 nm is tested. Then, the acceptor probe is added for joint incubation, and the fluorescence intensity emitted at 800 nm is tested. The ratio of the fluorescence intensity of the two times is compared with a control group or a standard curve, so that the mycophenolic acid in the whole blood can be qualitatively or quantitatively detected. The probe system can effectively overcome the background interference of the whole blood sample, and realize high-sensitivity homogeneous immuno-detection of BA in the whole blood.

The present application relates to the field of drug delivery technology and chronic kidney disease treatment, in particular, a kidney tissue targeted chronic kidney disease treatment drug nano delivery system, which solves the problems of poor targeting, low bioavailability, obvious side effects of existing chronic kidney disease treatment drugs, and insufficient responsiveness and poor safety of existing nano delivery systems. The system comprises a double-responsive nano carrier, an anti-kidney fibrosis drug and a targeting mediation layer. The double-responsive nano carrier is based on methoxy polyethylene glycol modified chitosan-polylactic acid copolymer, contains pH-sensitive hydrazone bonds and redox-sensitive disulfide bonds, and has a core-shell structure. The surface of the carrier is covalently connected with CD13 receptor affinity peptides, and is coated with a polylysine modified hyaluronic acid targeting mediation layer. The drug is pirfenidone or mycophenolate mofetil, which is covalently combined with the carrier through a disulfide bond. The system can realize precise enrichment of kidney lesions and double-responsive controlled drug release, improve the treatment effect, and reduce systemic and local toxicity.

The invention provides a genetic engineering strain for fermenting immunosuppressant mycophenolic acid as well as a preparation method and application of the genetic engineering strain, and the method is characterized in that a promoter PgpdA of 3-phosphoglycerol dehydrogenase is used, the amino acid sequence of the promoter PgpdA is SEQ ID NO: 1, and an indigenous promoter of peroxisome biogenic protein PbPex337 of a penicillium strain is replaced. According to the genetically engineered bacterium for high yield of mycophenolic acid, the yield of mycophenolic acid is effectively increased by replacing a promoter of the peroxisome biogenic protein PbPex337 gene, and the genetically engineered bacterium has positive industrial application value.

The invention provides a design method and application of a DNA aptamer based on a directional optimization strategy. The method combines methods of OpenMM molecular dynamics simulation, directional point mutation, directional cutting assembly and the like for the first time. Through a directional optimization platform, aptamer sequences of immunosuppressant tacrolimus and mycophenolic acid with higher binding force and specificity are screened out, and an SPR verification technology platform is established. On the basis, a GO load platform is constructed, and simultaneous sensing of tacrolimus and mycophenolic acid is realized. In conclusion, according to the oriented optimization strategy, the selectivity of the aptamer in a complex biological sample can be improved by changing the structure and the function of the aptamer. The proposal and application of the method are expected to provide reference for finding more aptamers for reducing the cost and improving the detection sensitivity and specificity and the like.

The invention relates to a mycophenolic acid derivative and a pharmaceutical composition containing the mycophenolic acid derivative. The mycophenolic acid derivative has a structure as shown in a formula (I), or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the structure as shown in the formula (I). The compound or the composition provided by the invention can be used for preparing medicines for preventing, treating, treating or relieving eye diseases of patients.

This blood inspection method comprises a preparation step for preparing whole blood collected from a subject, a pretreatment step for pretreating the whole blood to prepare an analysis sample, a separation step for separating the analysis sample into individual components by liquid chromatography, and an analysis step for analyzing each of the separated components with a mass spectrometry device. The subject has undergone the administration of a first immunosuppressive agent and a second immunosuppressive agent, the first immunosuppressive agent comprising at least one component selected from the group consisting of tacrolimus, ciclosporin A, everolimus and sirolimus, and the second immunosuppressive agent comprising at least one component selected from the group consisting of mycophenolic acid and metabolites thereof. The separated components include the first immunosuppressive agent and the second immunosuppressive agent. With respect to the method, in the analysis of the components with the mass spectrometry device, the analysis is performed in a positive mode when the first immunosuppressive agent is analyzed as a target component, and the analysis is performed in a negative mode when the second immunosuppressive agent is analyzed as a target component.

The application discloses a fengycin mimotope peptide which can be specifically combined with fengycin antibody, and a sensitive and rapid competitive enzyme-linked immunoassay method can be established by using the phage displaying the mimotope peptide or the mimotope peptide. 50 The IC50 is 0.30 ng / mL, and the LOD is 0.02 ng / mL, and the sensitivity of the method is improved by 60 times compared with the sensitivity of a traditional enzyme-linked immunoassay method based on a hapten; the competitive immunoassay method based on the mimotope peptide has good cross reactivity to other common structural analogues.

Pharmaceutical formulations comprising mycophenolic acid or pharmaceutically acceptable salts or prodrugs thereof are disclosed. Methods of making the formulations and methods of using them to treat, manage or prevent disease and disorders associated with undesired immune response are also disclosed. The formulations include a core comprising mycophenolic acid, microcrystalline cellulose, povidone, and talc surrounded by a seal coat comprising a polymer, plasticizer and talc which is surrounded by a sustained release layer comprising cellulose, dibutyl sebacate, and talc.

The present invention provides an enzymatic synthesis method for the immunosuppressant mycophenolic acid and its derivatives. This method utilizes a multi-enzyme, multi-cycle cascade reaction strategy to catalyze the conversion of the substrates 4-dienodecanoic acid-3-hydroxy-5-hydroxymethyl-6-methylphthalide or 4-dienodecanoic acid-3,5-dihydroxy-6-methylphthalide into mycophenolic acid and its derivatives. The multi-enzyme combination comprises an acyl-CoA ligase, an FAD-dependent oxidase, a 2,4-dienoyl-CoA reductase, an enoyl-CoA isomerase, a bifunctional enzyme with hydratase and dehydrogenase functions, and a thiolase; in addition, a CoA hydrolase and an oxygen-methyltransferase. This method, for the first time, achieves the in vitro enzymatic synthesis of (M)FDHMP-3C to MPA, fully elucidating the mycophenolic acid oxidative degradation synthesis pathway and the catalytic sequence of the catalytic enzymes.