102 results about "Ciclosporins" patented technology

The present invention provides novel cyclosporin analogue compounds, pharmaceutical compositions comprising these compounds and methods of using these compounds for the treatment of disorders and diseases, including immune disorders, inflammatory disorders and viral infections.

A capsule of cyclosporin A and semi-solid skeleton is proportionally prepared from cyclosporin A, oil phase, emulsifier, emulsifying aid, and semi-solid carrier through fusing them except cyclosporin A in water bath at 60 deg.C, stirring, adding cyclosporin A, stirring for full dissolving, cooling and loading it in capsules.

The invention discloses primers for detecting polymorphism of CYP3A4, CYP3A5 and MDR1 genes with an ARMs-PCR (amplification refractory mutation system-polymerase chain reaction) method and a prepared kit. Primer sequences are shown in SEQ 1-SEQ 18. The primers can perform typing testing on CYP3A4, CYP3A5 and MDR1 genes of humans quickly and accurately through specific amplification after primer combination. Genetic typing or preparation of the typing kit can be performed according to the primers and the primers are used for detecting metabolic capacity of Chinese people for related drugs such as tacrolimus, cyclosporine A and the like, so that a reference basis can be provided for special doctors who determine optimal drug dosage and individual drug use, and drug use risks are reduced.

The invention relates to the medical technology field, and particularly relates to a solid self-microemulsion based on a spherical crystallization technique and a preparation method thereof. The solid self-microemulsion is characterized in that: with the use of the spherical crystallization technique, the solid self-microemulsifying micoparticles are prepared from poorly water soluble drugs in a liquid phase by one step. The solid self-microemulsion with the poorly water soluble drugs comprises the components, by weight: 0.1 to 1.5 g of the poorly water soluble drugs, 4.0 g of a polyoxyethylene hydrogenated castor oil, 2.0 g of capric caprylic triglyceride, 2.0 g of tpropylene glycol, 1.0 ml of ethanol, 4.0 ml of dichloromethane, 0.5 to 1.1 g of ethylcellulose (or Eudragit RS100, RL100), 0.05 g of PEG4000, and 0.5 g of colloidal silicon dioxide. The poorly water soluble drugs include cyclosporine A, fenofibrate, glimepiride, cilnidipine, isradipine, simvastatin, baicalein, neogambogic acid, puerarin, cyclovirobuxine D, silymarin and the like.

The invention relates to a Cyclosporin A rapidly releasing solid dosage forms in the medicine technical field and the preparation method. The components weight contents of the solid dosage forms of the invention are that: 0.5 to 5 percent CyA, 5 to 75 percent lipide, and 5 to 70 percent porosint. The invention adopts CyA as the medicine activity component which is dissolved in the heating meltdown lipid material and added with the porosint in order to be richly adsorbed, then solid combined powder is prepared to be further suppressed to tablet or filled into capsule. The moisture content of the invention permeates into the porosint as meeting with water so as to make the wrapped medicine-lipide dispersoid inflate by absorbing water, pile out the gape structure and the medicine can be released. The invention can amplify the solubility and stripping speed of CyA, is useful for the absorption of medicine, has good stability, prevents the uses of organic solvent and polyoxyethylene castor oil, has safe operation, reduces the poison as well as side effects of medicine and has immunological rejection resisting function.

The present invention relates to compositions in the form of a clear solution comprising ciclosporin with low residual water content and 1-perfluorobutylpentane. The compositions may be used for topical administration to the eye.

The invention discloses a whole blood type freeze-dried powder immunosuppressant quality control substance as well as a preparation method and application thereof. The substance is a freeze-dried product mainly prepared from human whole blood serving as a matrix and an immunosuppressant. The immunosuppressant comprises one or more of tacrolimus, sirolimus, everolimus and cyclosporin A, or furthercomprises glucocorticoid immunosuppressants: one or more of hydrocortisone, cortisone, prednisolone, prednison and mycophenolic acid ester immunosuppressants for blood detection. The substance has theadvantages that the uniformity and the stability are good, low-temperature storage at -70 DEG C is not needed, and the substance can be used as a calibration product of immunosuppressant kits of different methodologies and can also be used as a quality control product for clinically monitoring an immunosuppressant detection system.

The invention discloses a ciclosporin A proliposome for oral administration, a pharmaceutical composition and a preparation method thereof. The ciclosporin A proliposome comprises the following pharmaceutical active ingredients and non-active ingredients by weight percent: 1-25% of ciclosporin A, 2-40% of lecithin, 0.5-12.5% of cholesterol, 21-96.45% of polyol and 0.05-1.50% of vitamin E. The proliposome is prepared from the ciclosporin A, a lipid membrane material, a hydrophilic matrix and the like through the ultrasonic dispersion method and the reverse phase evaporation method, and a liposome is formed spontaneously after the dispersion in water. The proliposome can improve the dispersity and the oral bioavailability of ciclosporin A which is an insoluble drug, lead the stability to be good and be more applicable to industrial production in comparison with the ordinary liposome.

The invention provides hydrogel with excellent antibacterial performance for burn wound healing and a preparation method of the hydrogel. The hydrogel is an ABA type triblock reticular copolymer formed by polymerizing a polyethylene glycol monomer and an N-isopropylacrylamide monomer, wherein the copolymer comprises a mussel bionic tissue bonding group and a nanoparticle anchoring group; the hydrogel is loaded with silver nanoparticles and zinc nanoparticles, and cyclosporine A is carried on the surface and the interior of the hydrogel. The hydrogel material prepared by the invention has the characteristics of high strain, biocompatibility, adhesiveness, heat sensitivity, injectability, microbial resistance and the like, and can promote the healing speed of full-thickness burn wounds. Meanwhile, the antibacterial activity is excellent.

The present invention provides a method for expanding PGC/PGCLC, including culturing PGC/PGCLC in the presence of a phosphodiesterase 4 (PDE4) inhibitor and/or cyclosporine A, further in the presence of forskolin, and a method for inducing oocytes from PGC/PGCLC, including culturing PGC/PGCLC in the presence of bone forming protein (BMP) and retinoic acid (RA).

The invention provides an in-situ gel containing cyclosporin micelles as a sustained release ophthalmic drug delivery system. The in-situ gel contains 0.01 wt% to 5 wt% of an aqueous ophthalmic formulation of cyclosporin present in the form of a micelle with the particle size of no greater than 20 nm.

The cyclosporin eye emulsion is prepared from the following components in percentage by mass: 0.01 to 0.05 percent of cyclosporin, 1.5 to 3 percent of collagen, 1.2 to 1.5 percent of castor oil, 1.8 to 2.5 percent of glycerol, 0.04 to 0.08 percent of anthocyanin, 0.8 to 1.2 percent of polysorbate 80 and the balance of double distilled water. The cyclosporin ophthalmic emulsion is prepared throughhigh-speed dispersion and shear emulsification, and collagen and anthocyanin in the emulsion are combined for use, so that the slow-release effect of the medicine can be effectively enhanced, and theresidual quantity of the medicine in corneas is increased.

The invention discloses an application of kaempferol in medicines for inhibiting rejection reaction of a receptor on organ transplantation. The invention discloses pharmacological effects of kaempferol in inhibiting rejection reaction of organ transplantation in the body of a receptor for the first time; and moreover, optimal effects can be achieved when kaempferol is combined with low-dose cyclosporin for a short time, and long-term survival of an islet graft in the receptor can be induced, so that various side effects caused by using full-dose cyclosporin for a long time can be avoided, the economic burden of patients brought by long-term anti-rejection treatment can also be lightened, and the long-term high-quality life of organ transplantation patients can be further facilitated. The invention also discovers an immune adjustment action mechanism of kaempferol, namely that kaempferol can be used for significantly increasing the number of regulatory T lymphocytes in the body of the receptor and reducing the gene expression of an islet graft IL-6 in the body of the receptor, so that the effects of resisting inflammation and resisting rejection reaction can be achieved.

The invention provides a method for detecting a cyclosporine pharmaceutical preparation, which comprises the following steps of: 1) treating the cyclosporine pharmaceutical preparation with a diluent to obtain a cyclosporine pharmaceutical preparation solution to be detected; and (2) detecting the cyclosporine pharmaceutical preparation solution to be detected obtained in the step (1) through using a gel chromatography exclusion method, wherein a chromatographic column adopted in the gel chromatography exclusion method detection is formed by connecting at least two water-soluble GPC chromatographic columns in series. The method can effectively separate povidone, OP-40 and polyoxyethylene hydrogenated castor oil, has the outstanding advantages of being good in stability, easy and convenient to operate, rapid, high in efficiency, good in sensitivity and the like, can achieve effective separation when the concentration of povidone, OP-40 and polyoxyethylene hydrogenated castor oil is low, and can provide a basis for further research on specific properties of any two or three of povidone, OP-40 and polyoxyethylene hydrogenated castor oil, such as cyclosporin eye drops.

The invention discloses application of cyclosporine A in preparation of a medicine for improving the embryo implantation rate of a patient suffering from repeated embryo implantation failure. In the prior art, the cyclosporine A is used as an immunosuppressor or a medicine for preventing miscarriage and preventing abortion, the application proposes that the cyclosporine A can improve the embryo planting rate for the first time, and particularly discloses improvement of the embryo planting rate of secondary embryo transplantation of the patient suffering from the repeated embryo implantation failure, and the research result is different from that in the prior art. Specifically, according to the technical scheme, clinical application of the cyclosporine A can be effectively guided, and side effects caused by improper medication are avoided.

The invention provides a method for constructing an immune healthy synovial sarcoma xenograft mouse model; the method comprises cultivating a generation P0, to be specific, resuscitating a tumor tissue block of a synovial sarcoma patient stored in a liquid nitrogen environment, then transplanting the tumor tissue block into an immunodeficient mouse under a sterile condition, and pretreating a micewith normal immunity by cyclosporine; culturing a generation Px, to be specific, inoculating the tumor tissue block, grown in a mouse from any of the generations P0 to Px, into the mouse pretreated with cyclosporine to form a generation Px mouse; and culturing a generation Py, to be specific, inoculating a synovial sarcoma tumor tissue block, grown in a mouse from any of the generations Px to Py-1, into the mouse with normal immunity until tumor tissues grow in the mouse, so that culturing of the generation Py is completed. The invention solves the problem that the traditional PDX (patient-derived xenograft) model has no immune system, provides an in-vivo model for the research on tumor immunotherapy, and widens the application range of the PDX model.

Belonging to the field of chemical technologies, the invention relates to a preparation process for a cyclosporine A-pH sensitive nanoparticle, and more specifically relates to improvement of the preparation process of the cyclosporine A-pH sensitive nanoparticle. The preparation process for the cyclosporine A-pH sensitive nanoparticle is characterized by low cost and high synthesis rate, and the product has good intestinal absorption effect. The preparation process for the cyclosporine A-pH sensitive nanoparticle includes the steps of: weighing F68 and dissolving it in 125mL distilled water to serve as the water phase; dissolving 50mg of CyA and a proper amount of EudragitS100 in anhydrous ethanol to prepare an organic phase; injecting the organic phase into the water phase stirred at a speed of 400r.min with a No. 7 support marrow puncture needle quickly; and then conducting stirring continuously and transferring the mixture into 60DEG C water bath, and volatilizing the organic solvent completely, thus obtaining a CyA-NP colloidal solution.

The present invention relates to a composition comprising cyclosporine A (CsA) for use in the prevention of bronchiolitis obliterans syndrome (BOS) in a double lung transplanted patient, or for the treatment of BOS or for the prevention or delay of the progression of BOS in a double lung transplanted patient being diagnosed with BOS, wherein the composition is administered to said patient by inhalation of said composition in aerosolized form comprising a therapeutically effective dose of cyclosporine A.

The invention discloses an intestinal adhesion prevention membrane solution as well as a preparation method and application thereof. The membrane solution disclosed by the invention comprises a solution A and a solution B, wherein the solution A refers to a normal saline solution dissolved with carboxymethyl chitosan and ciclosporin A; the concentration of the carboxymethyl chitosan in the solution A is 10-40mg/ml; the concentration of the ciclosporin A is 1.0-1.8mg/ml; the solution B refers to a CaCl2 normal saline solution; the concentration of CaCl2 is 2.5mg/ml; and the volume ratio of the solution A to the solution B is (25:8)-(25:40). The membrane solution disclosed by the invention can effectively prevent postoperative intestinal adhesion and is convenient to use.