74 results about "Ciclosporins" patented technology

The invention relates to the technical field of aplastic anemia (AA) treatment research, discloses a biomarker method for predicting the curative effect of cyclosporine on aplastic anemia, and aims to detect plasma differential metabolites of patients with aplastic anemia by adopting a metabonomics technology, find potential biomarkers for treating AA patients and find the curative effect of cyclosporine on the AA patients. CsA) is used for treating the in-vivo metabolism of AA. The method is based on liquid chromatography-mass spectrometry (LC-MS) and gas chromatography-mass spectrometry (GC-MS) technologies, and comprises the following steps: collecting 5 plasma samples of AA patients, 5 plasma samples of healthy people and 5 plasma samples of patients in a stable period after treatment for comparative analysis; and screening differential compounds by adopting a multivariate statistical method, and further performing enrichment analysis on differential metabolites. Research of the method shows that in-vivo metabolites of AA patients and healthy people are obviously different, and the way related to immunity and energy metabolism may be a key target for treating AA; csA intervenes the occurrence and development of AA by regulating and controlling immune-related metabolic ways.

The invention discloses a method for detecting the concentration of cyclosporine in blood through fluorescence and electrochemical double signals, and belongs to the technical field of biochemical analysis and medical detection. Aiming at the technical problems of insufficient sensitivity and high false positive rate of traditional single-signal detection of blood concentration of cyclosporine, the method comprises the following steps: activating carboxyl microspheres by a coupling agent, fixing double-stranded DNA (deoxyribonucleic acid) formed by a cyclosporine aptamer and an initiator chain, inducing the initiator to release by using a cyclosporine sample, realizing strand displacement through an A2-PEI composite system, and detecting the blood concentration of cyclosporine by using an A < 2 >-PEI composite system. DNA modified cadmium telluride quantum dots are respectively adopted to detect fluorescence signals, eATRP electrochemical signal amplification is carried out to detect electrochemical signals, concentration values obtained by the two signals are verified, and an average value is taken as a result. The method can accurately capture low-concentration cyclosporine signals in blood, eliminates interference of a single method, is mainly used for accurately monitoring the blood concentration of cyclosporine, and provides a reliable detection means for medication safety and curative effect control of cyclosporine in clinical scenes such as organ transplantation.

The invention relates to the field of biological medicine, in particular to a carrier-free nanoparticle which is formed by self-assembly of cyclosporine A and costunolide through intermolecular weak interaction. The invention also provides a preparation method of the traditional Chinese medicine composition and application of the traditional Chinese medicine composition in preparation of medicines for treating xerophthalmia. The carrier-free nano eye drops based on the synergistic effect of Chinese and western medicines are used for anti-inflammatory treatment of the xerophthalmia, a new strategy is provided for precise diagnosis and treatment of the xerophthalmia, the problems of single target spot, limited curative effect and the like in traditional treatment are solved, and more efficient inflammation control is expected to be achieved. While the curative effect is improved, the tolerance risk caused by long-term use is reduced, double optimization of the curative effect and safety is realized, and the limitation of traditional single drug treatment is broken through. By adopting the carrier-free nano preparation, the delivery efficiency of the medicine on the ocular surface is effectively improved, the bioavailability is enhanced, powerful support is provided for improving the curative effect of the medicine, and the carrier limitation bottleneck is broken through.

The invention provides pharmaceutical compositions comprising about 0.05 to 0.1% (w / v) cyclosporine dissolved in 1-perfluorobutyl-pentane for use in the topical treatment of dry eye disease and provides for dosing and treatment methods thereof. The invention further provides kits comprising such compositions.

The invention relates to an ophthalmic composition in an aqueous solution form. The ophthalmic composition consists of cyclosporine, medium chain triglyceride, polyoxyethylene (40) hydrogenated castor oil, polyethylene glycol 400, glycerol, sodium acetate and water. The pH value of the ophthalmic composition is close to that of tears, and the ophthalmic composition is good in medication comfort and good in stability during storage.

The invention discloses difunctional nano drug-loaded eye drops for xerophthalmia and a preparation method of the difunctional nano drug-loaded eye drops, and belongs to the field of pharmaceutical preparation technologies and ophthalmology pharmacy. The core of the invention is to construct a composite nanoparticle which has a core-shell structure and has long-acting adhesion lubrication and targeted control drug release functions. The preparation method comprises the following steps: firstly, encapsulating a hydrophobic immunosuppressant such as cyclosporine A in a biodegradable pad polymer matrix such as polylactic acid-glycolic acid copolymer (PLGA) by an emulsification-solvent evaporation method to form a drug-loaded polymer nano core; through the exquisite integrated design of the structure and the function, collaborative targeted therapy of two core pathological links of'tear film instability 'and'immune inflammation' of xerophthalmia is achieved, the bioavailability of the medicine is remarkably improved, the medication frequency and eye irritation are reduced, and the curative effect of xerophthalmia is improved. A more efficient and safer administration scheme with better patient compliance is provided for clinical treatment of xerophthalmia.

Compositions are disclosed that include acridinium esters of cyclosporin A or C. Kits containing same, as well as methods of making and using same, are also disclosed.

The present disclosure relates to oral compositions of Compound I or its derivatives. Several dosage ranges are disclosed, along with SAD, MAD, and PK data. Comparative data between Compound I, tofacitinib, ritrecitinib, and cyclosporin A are also disclosed. Methods of use for treating inflammatory conditions are also disclosed.

The invention relates to the technical field of hematopoietic reconstruction, in particular to application of costal cartilage derived stem cells and costal cartilage derived stem cells combined with pluripotent progenitor cells, hematopoietic stem cells or cyclosporine in preparation of a preparation for hematopoietic reconstruction. The costal cartilage derived stem cells (CD45-CD51 +) are derived from costal cartilage and have remarkable ecological niche recovery capability. When the cells are used alone or combined with hematopoietic stem cells and pluripotent progenitor cells, the hematopoietic function can be enhanced. The costal cartilage-derived stem cells are directionally differentiated into important supporting cells forming bone marrow ecological niche, secrete hematopoietic cell factors and protect hematopoietic stem / progenitor cells. In treatment of aplastic anemia, costal cartilage-derived stem cells and cyclosporin A have a synergistic effect, and immune-mediated bone marrow failure is improved through dual mechanisms. According to the technical scheme, the technical problem that the effect of treating bone marrow failure and promoting hematopoietic reconstruction by hematopoietic stem cell transplantation is not ideal is solved, and a new way is opened up for treating bone marrow failure and blood system diseases.

A method of preparing an implantable biomaterial includes combining a polymer with a neuro-regenerative agent or immunosuppressive agent selected from a group comprising at least one of: rapamycin, cyclosporine A, or analogs thereof, melting the polymer, and extruding the polymer and the neuro-regenerative agent or immunosuppressive agent to form the implantable biomaterial.

The present invention aims to provide a cyclosporine self-microemulsion preparation, its preparation method and application. The preparation is composed of cyclosporine, α-tocopherol, amino acids, a solvent, a surfactant, and a co-surfactant. This cyclosporine preparation has good stability and palatability. While effectively improving the bioavailability of the active ingredient, it also improves the stability and palatability of the cyclosporine preparation. After oral administration, under the action of the gastrointestinal tract, the preparation is first dispersed and diluted by gastric juice to form a microemulsion, and then digested by digestive enzymes, etc., and has obvious effects in the treatment of canine and feline atopic dermatitis or allergic dermatitis, etc.

The invention provides a medicine for preventing or treating enteritis. Hamp is adopted; and E, dyeing, determination of IL-6 factors in serum of each group of animals and the like are used for researching the influence of the vocyclosporine on intestinal tissues, mucosal barriers and immune systems of DSS or TNBS-induced mouse colitis models. Experimental basis is provided for clinical application of the vocyclosporine in preparation of the colitis treatment medicine, and the vocyclosporine has good application prospects and huge potential value and social significance.

The present disclosure relates to solid state forms of Voclosporin and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof.

The utility model relates to the technical field of mass spectrometers, and discloses a mass spectrometer for detecting the concentration of cyclosporine A in human whole blood, which comprises a sampler, a fixed box is fixedly mounted at the bottom of an inner cavity of the sampler, a through hole is formed in the upper part of an inner cavity of the fixed box, a motor is fixedly mounted at the rear part of the inner cavity of the fixed box, and a through hole is formed in the inner cavity of the fixed box. A first gear is fixedly connected to an output shaft of the motor in a sleeving mode, a gear ring is meshed with the outer edge of the first gear, edge rings are fixedly installed on the upper portion and the lower portion of the gear ring respectively, a sliding groove is formed in an inner cavity of the fixing box, a tooth groove is formed in an inner cavity of the gear ring, second gears are evenly meshed with the outer edge of the tooth groove, and a rotating shaft is fixedly connected to the middle of the second gears in a sleeving mode; the stroke of a motor is adjusted through a pressure sensor, sample bottles are fixed through a clamping plate, the device can conveniently fix the sample bottles with different sizes, the practicability of the device is improved, the situation that the air tightness is affected by shaking of the sample bottles is avoided, and the accuracy of a detection result is guaranteed.

The invention discloses a stable cyclosporine ophthalmic ultra-micro emulsion, which comprises 0.1% of cyclosporine, 1%-2% of medium chain triglyceride, 0.4%-0.8% of an emulsifier, 2%-3% of glycerol, 0.0005%-0.005% of sitaammonium chloride and sodium hydroxide with a required amount for adjusting the pH value of the emulsion to 6.1-7.9, and the emulsifier is a combination of teloxaben and poloxamer in a weight ratio of 3: 1. The cyclosporin ophthalmic ultra-micro emulsion provided by the invention is smaller in droplet particle size and higher in Zeta potential, is basically not changed after being placed for a long time, and has better stability and better expected drug effect.

Methods, compositions, and kits suitable for use in the prevention, treatment, or recovery of fibrosis are disclosed. [Solution] The above problems are solved by a method comprising administering a composition comprising a cyclosporine analog (e.g., CRV431) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof to a subject requiring prevention, treatment, or recovery from fibrosis, and by compositions and kits for the prevention, treatment, or recovery from fibrosis comprising a cyclosporine analog (e.g., CRV431) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.

To provide novel cyclosporin derivatives.SOLUTION: Provided is a compound having the following structure or a pharmaceutically acceptable salt thereof. Also provided are a pharmaceutical composition comprising the same, and a method that uses the same for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, lung, liver, and kidney diseases, and hair loss.SELECTED DRAWING: None

The invention relates to the field of pharmaceutical preparations, in particular to a cyclosporine ophthalmic preparation and a preparation method and application thereof. The preparation comprises cyclosporin, an oil phase, a surfactant, a cosurfactant, a thickening agent, an osmotic pressure regulator and water for injection. By controlling the peroxide value ratio of the oil phase to the cosurfactant or the pH value of the cosurfactant, the ophthalmic preparation containing high-concentration cyclosporin is controllable in quality, stable and feasible.

The invention discloses a composition. The composition is a combination of any two or three of cyclosporine A, allipovir, allipovir and [MeIle] 4-cyclosporine. The invention also discloses the cyclosporin A, the allipovir, the allipovir, the [MeIle] 4-cyclosporin and the application of the composition in preparation of a preparation for inhibiting proliferation of the African swine fever virus. The medicine has an application prospect.

The application belongs to the field of ophthalmic nano-preparations, and particularly relates to an ophthalmic poly-nitrogen-oxygen amphoteric nano-drug carrier, an ophthalmic nano-preparation and a use. The nano-drug carrier is prepared by using a random copolymer of 2-(N-oxide-N,N-diethylamino)ethyl methacrylate and butyl methacrylate, has an average particle size of 7-12 nm, and can be used for loading ophthalmic drugs such as cyclosporine A. Research shows that the nano-drug carrier has good corneal retention characteristics and corneal permeability, and after loading cyclosporine A, has a good relieving effect on corneal damage and local inflammation of dry eye model animals, and the safety of the nano-drug carrier is good, and the nano-drug carrier has a good application prospect.

The invention relates to the technical field of biological medicine, in particular to a pharmaceutical composition for preventing or relieving sperm motor dysfunction caused by fenvalerate, and the pharmaceutical composition comprises N-acetylcysteine and / or cyclosporin A. Based on the discovery that fenvalerate induces rise of reactive oxygen species (ROS) to cause mitochondrial dysfunction and destroy a cAMP / PKA signaling pathway so as to inhibit sperm motility and induce mitochondrial apoptosis. An in-vitro rat sperm model proves that NAC and CsA can effectively reverse sperm motility reduction, ATP / cAMP level reduction, mitochondrial membrane potential dissipation and cell apoptosis caused by fenvalerate. The invention provides a new prevention and treatment strategy for treating male reproductive function damage caused by exposure of pyrethroid pesticides.

The invention discloses a programmed controllable slow-release bionic spinal cord graft and a preparation method and application thereof, and belongs to the field of medical biomaterials.The preparation method comprises the steps that a micro-nano oriented fiber scaffold with a groove is synthesized on the basis of recombinant NT3, silk fibroin, bovine collagen and a neurotrophic factor NGF; the programmed controllable slow-release bionic spinal cord graft is jointly constructed by combining an acellular matrix and an exosome derived from human umbilical cord mesenchymal stem cells with a programmed slow-release system of GelMA drug-loaded microspheres containing cyclosporine a; multiple technologies such as bionic tissue engineering, a micro-fluidic technology, a drug-loaded microsphere controllable slow-release technology, an acellular matrix and exosome are combined, spinal cord injury repair is facilitated, good biocompatibility is achieved, nerve axons are promoted to grow in an oriented mode, immune regulation can be given in the early stage of spinal cord injury, the nerve regeneration microenvironment after spinal cord injury is improved, and the nerve regeneration effect is improved. The method is beneficial to nerve regeneration and functional reconstruction after spinal cord injury.

To provide a topical ophthalmic preparation containing cyclosporin, and a method for producing the preparation.SOLUTION: A topical ophthalmic preparation contains 0.087 to 0.093 wt.% of cyclosporin. In some aspects and embodiments, the preparation may contain polyoxyl lipid or fatty acid and / or polyalkoxylated alcohol, and may contain nanomicelle.SELECTED DRAWING: Figure 1

Disclosed herein include methods, compositions, and kits suitable for use in preventing, treating or reverse fibrosis. The methods comprise administering to a subject in need thereof a composition comprising a cyclosporine analogue (for example, CRV431), or a pharmaceutically acceptable salt, solvate, stereoisomer thereof. The compositions and kits comprise a cyclosporine analogue (for example, CRV431), or a pharmaceutically acceptable salt, solvate, stereoisomer thereof.

The invention relates to a method for detecting related substances of cyclosporine eye drops, which is characterized in that a chromatographic column (Aurashell C18 4.6 * 150mm, 2.7 mu m) taking octadecylsilane bonded (fully porous) silica gel as a filler is adopted as a chromatographic condition, a mobile phase is composed of a mobile phase A and a mobile phase B, an acetonitrile-water-methanol-phosphoric acid system is selected as the mobile phase A, an acetonitrile system is selected as the mobile phase B, and gradient elution is adopted; the main detected impurities comprise degradation impurities: iso-cyclosporine A, and relatively large process impurities, namely dihydrocyclosporine A, cyclosporine B, cyclosporine C, cyclosporine U, cyclosporine D, cyclosporine G and cyclosporine H. The related substance analysis method provided by the invention has the advantages that the specificity is strong, and the accuracy and reproducibility of each impurity are good; (2) the method provided by the invention is relatively mild in mobile phase and solvent, and has less influence on a chromatographic column and an instrument.

The invention relates to the technical field of bioinformatics, and provides an analysis method for treating aplastic anemia (AA) targets by cyclosporine, which comprises the following steps: collecting plasma samples from a preliminary diagnosis patient, a disease stable period patient and a healthy control group; the method comprises the following steps: based on a DIA quantitative proteomics method, analyzing proteins in a plasma sample by adopting a liquid chromatography-mass spectrometer (LC-MS) method, and screening differential expression proteins; carrying out enrichment analysis and pathway analysis on the differential expression protein; verifying the expression levels of the differential expression proteins in different groups by adopting an ELISA (Enzyme-Linked Immunosorbent Assay) method to obtain key differential expression proteins; a molecular docking technology is adopted to verify the binding capacity of cyclosporine and the differential expression protein, and the potential of the key differential expression protein as a therapeutic target is determined. Different differential proteins of AA patients and healthy people before and after treatment are successfully obtained, an experimental basis is provided for exploring a mechanism for treating AA by cyclosporine, and possibility is provided for searching a new treatment target.

The invention provides a cyclosporine bulk drug and a detection method of related substances of oil-in-water emulsion thereof, the method adopts an octadecyl silane bonded silica gel chromatographic column (the front of the column is connected with a stainless steel tube), a mobile phase A is a mixed solution of acetonitrile, a water phase, tert-butyl methyl ether and phosphoric acid in a ratio of 450-480: 490-540: 25-45: 1, and the water phase contains 0.1-0.4% of an ion pair reagent; a mobile phase B is a mixed solution of acetonitrile and 0.2% phosphoric acid water in a ratio of 70: 30-80: 20, and the cyclosporine and five impurities (impurity U, impurity H, impurity dihydroA, impurity D and impurity G) thereof can be distinguished and detected at the same time through specific gradient elution. The method has the advantages of strong specificity, high sensitivity and good repeatability, and can effectively control the content of related substances in the cyclosporine oil-in-water emulsion. The method can be used for detecting the cyclosporine ophthalmic preparation containing the teloxacin and the medium chain triglyceride.

The invention relates to the field of pharmaceutical preparations, in particular to an ophthalmic composition containing cyclosporine. The ophthalmic composition comprises a first component and a second component, wherein the first component is ciclosporin or a pharmaceutically acceptable salt or a pharmaceutically acceptable derivative thereof; and a second component, wherein the second component is selected from at least one of alkyl glycoside and polyethylene glycol-15-hydroxystearate. The cyclosporine composition disclosed by the invention is good in stability, and repeated administration results show that the composition is free from eye irritation, so that the safety and the patient compliance are greatly improved. Meanwhile, the preparation process of the cyclosporine composition is simple, batch production can be realized through a conventional ophthalmic preparation production line, and the cyclosporine composition is beneficial to popularization and application in actual production.

The invention relates to the technical field of pharmaceutical analysis, in particular to an ICP-OES (Inductively Coupled Plasma-Optical Emission Spectrometry) detection method for the content of carbomer in cyclosporine eye drops. The method comprises the following steps: fully dissociating carboxylic acid groups of carbomer under alkaline conditions, carrying out metering reaction on the carboxylic acid groups and added calcium ions, detecting the content of residual calcium elements in a solution after the reaction through ICP-OES (Inductively Coupled Plasma Optical Emission Spectrometry), and carrying out back calculation by combining with a metering relationship between the calcium ions and carbomer, so as to obtain the content of carbomer in the cyclosporine eye drops. Compared with an existing titration method, the method is easy and convenient to operate, high in detection efficiency and good in repeatability and accuracy, can effectively adapt to complex matrix systems such as cyclosporine eye drops and the like, and has good industrial application value.

The application discloses a new use of 4F dimer polypeptide and lipids thereof, and the 4F dimer polypeptide and lipids thereof are used for preparing a drug for treating dry eye syndrome. The application has the advantages that the application innovatively finds that pHDL has very good effects on dry eye syndrome, and has the advantages of synergistic treatment for the multi-factor pathological mechanism of dry eye syndrome. Therefore, compared with the existing single mechanism drug (such as cyclosporine eye drops for only inhibiting inflammation), the multi-dimensional action mechanism of pHDL precisely matches the complex pathological network of dry eye syndrome, and is expected to improve the coverage range of the curative effect on refractory dry eye syndrome.