52 results about "Tacrolimus" patented technology

The present application relates to the technical field of pharmaceutical analysis, and in particular to a combined analysis method for exploring the effect of Huangkui capsules on improving chronic kidney injury of tacrolimus based on metabolomics and proteomics. The combined analysis method of the present application explores how Huangkui capsules improve the mechanism of chronic kidney injury of tacrolimus from multiple dimensions, which is beneficial to in-depth analysis of the specific effects of Huangkui capsules at the molecular, cellular and tissue levels, reveals the key path and regulation mechanism of kidney protection, and can also provide a scientific basis for optimizing clinical application, further promoting the modernization of traditional Chinese medicine and its wide application in the treatment of kidney disease.

The invention discloses a preparation method of tacrolimus capsules, and relates to the technical field of medicines. The preparation method comprises the following steps: S1, preparing a drug-loaded pellet core; s2, coating and curing a flexible buffer layer, namely curing for 8 hours under the conditions that the temperature is 100 DEG C and the relative humidity is 35%, so that the xanthan gum is in a swelling state; s3, coating with a high-barrier layer; s4, protective controlled release layer coating: preparing a coating solution from the third polymer grafted with the lipophilic bile salt derivative and phospholipid; and S5, capsule filling. Through functional gradient multilayer structure design and fine regulation and control of phospholipid composition and spatial distribution, multiple technical problems of poor chemical stability of tacrolimus, brittle rupture of a coating, burst drug release, dissolution and absorption disorder and release drift caused by individual difference of gastric emptying are synergistically solved; the excellent mechanical strength, stable and controllable release kinetics and obvious solubilization promoting effect of the pellet are realized. The method is clear in technological parameters and suitable for industrial production.

The invention discloses a tacrolimus-containing pellet pharmaceutical composition, the pharmaceutical composition is composed of an enteric pellet and a sustained-release pellet, the enteric pellet comprises 0.5-5% of tacrolimus, 10-80% of a filler, 2-10% of a disintegrating agent, 1-5% of an adhesive, 0.5-2% of a flow aid, 0.5-1% of a lubricant, and 5-13% of an enteric coating material; the sustained-release pellet comprises 0.5 to 2% of tacrolimus, 10 to 80% of a filling agent, 2 to 10% of a disintegrating agent, 1 to 5% of an adhesive, 0.1 to 1% of a flow aid, 0.1 to 1% of a lubricant, 5 to 15% of a sustained-release coating material and 0.1 to 0.5% of a plasticizer. The pellet pharmaceutical composition containing tacrolimus disclosed by the invention can maintain longer blood concentration and longer action time, so that the medicine taking frequency is reduced, the compliance of a patient is improved, the toxic and side effects are reduced, and the effectiveness and safety of medicine use are further ensured.

The invention relates to a nano antibody for specifically recognizing a tacrolimus-antibody compound and application of the nano antibody, and belongs to the technical field of biological detection. A variable region of the nano antibody has three complementary determining regions CDR1, CDR2 and CDR3, can specifically recognize a tacrolimus-antibody compound, and can be used for detecting drugs by a double-antibody sandwich method; the kit is widely suitable for various immunodetection technologies such as an enzyme-linked immunosorbent assay (ELISA), a chemiluminescence immunoassay (CLIA), an electrochemical luminescence immunoassay (ECLIA), a fluorescence immunoassay (FIA), an immunochromatography test strip method and the like. According to the method, the limitation of a traditional competition method is overcome, high-sensitivity, high-specificity and high-stability detection is realized, the method can be adapted to various detection platforms, and a portable pretreatment process without centrifugation can also be realized.

The application discloses a method for simultaneously and rapidly detecting the concentration of four immunosuppressants, comprising the following steps: mixing a blood sample with an internal standard solution containing ascomycin, cyclosporine-d4, sirolimus-d3 and everolimus-d4, adding a precipitant and centrifuging to obtain a sample to be detected; injecting into a liquid chromatography-tandem mass spectrometry system for analysis to obtain original data containing the retention time window and mass spectrum response signal of four analytes; searching the original data based on an interferent database, wherein the interferent database contains a plurality of compounds that can possibly generate mass spectrum signal interference and characteristic ion information thereof; inputting the original data and the searched potential interferent information into a machine learning model to output a net mass spectrum response value after interference correction; and calculating the concentration of tacrolimus, cyclosporine, sirolimus and everolimus in the blood sample according to the obtained net mass spectrum response value, the mass spectrum response value of the corresponding internal standard and a pre-established standard curve.

The invention discloses an immunosuppressant transdermal patch and a preparation method thereof, the transdermal patch is provided with a backing layer, an ointment-containing body and a protective layer, the backing layer is a polyester and ethylene-vinyl acetate copolymer film, the ointment-containing body is formed by mixing a main drug tacrolimus, a stabilizer, a matrix, a cross-linking agent and a pressure-sensitive adhesive, and the protective layer is a polyester and ethylene-vinyl acetate copolymer film. The protective layer is a polyethylene glycol terephthalate film, the protective layer is coated with the ointment-containing body, and then the backing layer is pressed and covered on the surface of the ointment-containing body. The immunosuppressant transdermal patch provided by the invention can be adhered to parts such as neck, shoulder, chest, arm memory and the like, can be freely adjusted in use duration according to different illness states, and is safe and free of toxic and side effects. In addition, the transdermal patch disclosed by the invention is good in stickiness, good in permeability, free of irritation and allergy phenomena, good in patient compliance and capable of being used for a long time. Meanwhile, the method has the advantages of low preparation cost, simple and reasonable preparation process and the like, and has wide application prospects.

The application belongs to the technical field of medicines, and discloses a tacrolimus microcrystal and a preparation method and application thereof. Compared with the raw medicine, the tacrolimus microcrystal has a significantly improved dissolution rate, cumulative dissolution rate, hydrophobicity and safety (non-irritation). Compared with the existing medicine preparation, the tacrolimus microcrystal has the advantages of long retention time and better treatment effect.

The invention discloses a fibroblast composite bone filling preparation as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The method comprises the following steps: specifically culturing fibroblasts by using Yoda1 and matrix I-type collagen, and activating the osteogenic differentiation capability of the fibroblasts; resuspending the finished product fibroblasts capable of activating the osteogenic differentiation capacity in a solution containing ginsenoside, tacrolimus and fibronectin to obtain a mixed solution; and finally, mixing the mixed solution with the bone filler to obtain the fibroblast composite bone filling preparation capable of promoting repair. The preparation can provide fibrosis support and promote vertebra fusion, does not cause inflammatory reaction, and has a large-scale application prospect.

The invention relates to a tacrolimus-loaded nano material as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention provides a preparation method of a tacrolimus-loaded nano material, which comprises the following steps: dispersing MnO2 nanosheets in water, carrying out ultrasonic treatment, and centrifuging to obtain a supernatant; mixing the supernate with dopamine hydrochloride, adjusting the pH value, stirring, centrifuging to obtain supernate, and dialyzing to obtain MnO2 / PDA NPs; and mixing a tacrolimus chloroform solution with the obtained MnO2 / PDA NPs, centrifugally collecting the precipitate, and washing to obtain the nano material loaded with tacrolimus. According to the method, MnO2 is subjected to ultrasonic treatment and then centrifuged, MnO2 / PDA NPs containing polydopamine is prepared from MnO2 and dopamine hydrochloride, polydopamine serves as a functional medium, tacrolimus is effectively loaded on a MnO2 substrate through coordination self-assembly, and the nano material loaded with tacrolimus is successfully synthesized.

The invention relates to an anti-immunological rejection FK506 (at) ZIF-8 / HTCC ophthalmic gel and a preparation method thereof, FK506 and a zeolite imidazole skeleton (ZIF-8) are combined to prepare FK506 loaded nanoparticles (FK506 (at) ZIF-8), and quaternized chitosan is innovatively used as a sol of the FK506 (at) ZIF-8 to prepare the ophthalmic gel for use. The problems that a novel potent immune preparation tacrolimus administration mode is short in drug retention time, fast in metabolism, poor in cornea permeability and insoluble in water, and consequently the bioavailability of the FK506 eye drops is low are solved. Compared with an FK506 direct administration mode, the administration mode of the novel nanoparticle drug-loaded ophthalmic gel is higher in drug utilization rate, has a treatment effect on corneal transplantation immunological rejection, and delays the occurrence and development of transplantation rejection.

Embodiments of the disclosure provide ophthalmic compositions and methods of use thereof. The embodiments disclose ophthalmic compositions including devices such as a punctal plug. Some embodiments are directed to a method of preparing and using such devices. One embodiment provides a method of dissolving a hydrophilic polymer and an active pharmaceutical ingredient (API) in alcohol to form a hydrophilic polymer / API solution, where the API includes tacrolimus, spray drying the hydrophilic polymer / API solution to form a hydrophilic polymer / API mixture, mixing the hydrophilic polymer / API mixture with a binder to form an API paste, and curing the API paste to form a punctal plug, where the punctal plug is configured to release an effective amount of the API for a treatment period of 30 days to one year.

This invention relates to a chemiluminescent immunoassay reagent for tacrolimus, its preparation, and detection method. The reagent comprises a first reagent, a second reagent, and a magnetic separation reagent. The first reagent is a buffer solution containing a fluorescein-labeled anti-tacrolimus monoclonal antibody at a pH of 6.0–9.0, with the concentration of the fluorescein-labeled anti-tacrolimus monoclonal antibody being 1.0–5.0 μg / mL. The second reagent is a buffer solution containing a tacrolimus-alkaline phosphatase conjugate at a pH of 6.0–9.0, with the concentration of the tacrolimus-alkaline phosphatase conjugate being 0.05–0.20 μg / mL. The magnetic separation reagent is a suspension of magnetic microparticles coated with the anti-fluorescein monoclonal antibody. This invention enables the quantitative detection of tacrolimus with lower cost and higher accuracy and precision.

The application discloses a kind of photodynamic balloon catheter systems, comprising: tube body, with opposite proximal end and distal end;Balloon, the balloon is fixed in the distal end portion of the tube body;Optical fiber assembly is inserted in the tube body, and with the light-emitting site extending to adjacent the balloon;The surface of the balloon is loaded with auxiliary material and photosensitizer in the form of coating;The photosensitizer can activate collagen and elastin under the wavelength of light 400-460nm to make them crosslink;The auxiliary material includes active drug and sustained-release material wrapped the active drug, the active drug is at least one of paclitaxel, rapamycin, zotarolimus, tacrolimus, everolimus, temsirolimus, zanolimus, biolimus, docetaxel, protein-bound paclitaxel and protein-bound dexamethasone;By the photodynamic balloon catheter system of the application can improve the utilization rate of active drug in intravascular administration.

The invention discloses a scar repair patch containing tacrolimus and a preparation method of the scar repair patch, and belongs to the technical field of medical dressings. The patch comprises a backing layer, a medicine storage and release layer and a protective film layer. The medicine storage and release layer is composed of a hydrogel matrix and tacrolimus, and the mass percent of tacrolimus is 0.01%-0.1%. The hydrogel matrix comprises polyvinyl alcohol, glycerol, a cross-linking agent and purified water. The preparation method comprises the following steps: dissolving tacrolimus in ethanol to form a medicine solution; preparing a polyvinyl alcohol hydrogel matrix; and mixing the medicine solution with the matrix, coating the mixture on the backing layer, and performing radiation crosslinking curing, slitting, packaging and sterilization. The hydrogel is adopted as a drug carrier, the technical problems that tacrolimus is non-uniformly dispersed and difficult to release in silica gel are solved, and a novel medical instrument which is stable in drug release, good in biocompatibility and suitable for inhibiting scar hyperplasia for a long time is provided.

The application discloses a kind of tacrolimus transdermal aerosol and preparation method thereof, belong to the technical field of pharmaceutical preparation preparation.It includes the following weight parts raw materials: 63~74 complex liposome mixed solution, 22~29 weight parts propellant and 1~3 weight parts penetration enhancer.The application is obtained by mixing and pressure filling tacrolimus complex liposome solution, propellant and penetration enhancer in pressure-resistant container to obtain tacrolimus transdermal aerosol, improves the encapsulation efficiency of tacrolimus, and the prepared tacrolimus transdermal aerosol is uniform without sedimentation, with good dissolution and dispersion characteristics.

This invention discloses a reagent kit for detecting tacrolimus concentration in whole blood. The kit includes a box, a container rack, multiple reagent bottles, and a working solution preparation tube. The container rack is fixedly installed in the box and has multiple cavities. The reagent bottles and the working solution preparation tube are placed in the cavities. The working solution preparation tube consists of an upper chamber and a lower chamber. The lower chamber is an open cavity. The bottom end of the upper chamber is engaged with the top end of the lower chamber, forming a sealed cavity. A cap is provided at the top end of the upper chamber. A conical portion is provided inside the lower chamber, extending upwards from the bottom end of the lower chamber to contact the bottom end of the upper chamber. This invention simplifies the working solution preparation steps in traditional methods, eliminating the need for repeated weighing and pipetting, improving solution preparation efficiency, further saving time and costs, and increasing detection efficiency.

The invention relates to the technical field of biomedical diagnosis, in particular to application of DBP gene variation and / or CYP2A6 gene variation in individualized medication guidance of tacrolimus. The invention particularly relates to a tacrolimus individualized medication guidance system. The system comprises a sample information processing module, a diagnosis module and an information output module, the sample information module is used for receiving detected object information of a patient, and the detected object information at least comprises information of DBP gene variation and / or CYP2A6 gene variation; and the diagnosis module receives information input of the sample information processing module, obtains a blood concentration probability according to the information, and outputs the blood concentration probability to the information output module to output medication guidance suggestions.

This invention discloses a sustained-release membrane for postoperative treatment of diabetic peripheral neuropathy and its preparation method. The sustained-release membrane comprises, from the outside in, a PLGA nanofiber outer layer containing tacrolimus and magnesium hydroxide nanoparticles, a glucose-responsive hydrogel middle layer containing insulin and glucose oxidase / catalase, and a PCL-oriented nanofiber inner layer containing methylcobalamin. The layers are connected by a polydopamine interface layer, and the outermost surface of the outer layer is coated with a hyaluronic acid anti-adhesion coating. Insulin, as a local neurotrophic factor, directly activates the PI3K / Akt / mTOR and ERK / MAPK signaling pathways, promoting axonal regeneration and myelin repair. The sustained-release membrane integrates three major functions: immunomodulation / anti-inflammation, glucose-responsive insulin neurotrophic delivery, and sustained nerve regeneration promotion. It prevents postoperative nerve re-adhesion through a spatiotemporal sequential drug release strategy. All components are biodegradable and do not require secondary surgery for removal.

The invention provides a tacrolimus multi-layer coated pellet capsule and a preparation method of the tacrolimus multi-layer coated pellet capsule. The tacrolimus multi-layer coated pellet capsule is characterized by comprising an inner core pellet, a middle coating layer and an outer coating layer, the core pellet is prepared from tacrolimus, high molecular weight ethyl cellulose with the molecular weight of 100000 to 300000Da, a disintegrating agent and a filling agent; the middle coating layer comprises medium molecular weight ethyl cellulose with the molecular weight of 30000 to 50000 Da; the outer coating layer comprises low molecular weight ethyl cellulose with the molecular weight of 1000 to 10000 Da and a release accelerator. Through the innovative design of a three-layer coating structure, the multi-stage release characteristic of tacrolimus is realized. The core pellet adopts high-molecular-weight ethyl cellulose as a base material to provide a drug sustained release basis; the middle coating layer is made of medium-molecular-weight ethyl cellulose, so that a stable membrane-controlled release layer is formed, and the drug release rate is accurately controlled; and the outer coating layer adopts low-molecular-weight ethyl cellulose to be matched with a release accelerator, so that the quick release of the medicine is realized.

The invention discloses a molecularly imprinted electrochemical sensor for detecting tacrolimus. An electrochemical polymerization method is adopted, tacrolimus is used as a template molecule, o-phenylenediamine and chloroauric acid are used as functional monomers, electrochemical copolymerization is carried out on the surface of a gold electrode, and poly-o-phenylenediamine and gold nanoparticles are generated. And eluting the template molecules, and preparing the organic / inorganic hybrid containing the target molecular imprinting on the surface of the gold electrode. The gold electrode with the surface modified with the hybrid is immersed in a base solution containing potassium ferricyanide, and a three-electrode system of an electrochemical workstation is adopted for detecting redox signals through an electrochemical cyclic voltammetry method and a differential pulse voltammetry method. Samples containing different concentrations of tacrolimus are dropwise added to the surface of the modified electrode, and then the modified electrode is immersed in a base solution to measure the redox signal intensity of the modified electrode. The relationship between the concentration of the tacrolimus and the corresponding electrochemical signal intensity is established, and then the molecularly imprinted electrochemical sensor is developed and is used for efficiently detecting the tacrolimus.

The application belongs to the technical field of medicines, and discloses a tacrolimus lipid microsphere, a preparation method and application thereof. Compared with the existing eye tacrolimus preparation (such as Talymus), the tacrolimus lipid microsphere has the advantages of no irritation, long retention time, better treatment effect on dry eye, can improve tear film stability, and can treat corneal damage caused by dry eye.

This application relates to a tacrolimus detection kit. Specifically, the glucose-6-phosphate dehydrogenase mutant of this application contains one or a combination of mutations selected from the following, compared to the wild-type glucose-6-phosphate dehydrogenase: D306C, D375C, and G426C. The detection kit prepared using the glucose-6-phosphate dehydrogenase mutant of this application exhibits high specificity, high sensitivity, ease of operation, short detection time, and accurate quantification, making it suitable for high-throughput detection.

The present application relates to the technical field of biomedical diagnosis, and particularly to application of DBP gene variation and / or CYP2A6 gene variation in individualized medication guidance of tacrolimus, and more particularly to an individualized medication guidance system of tacrolimus, which comprises a sample information processing module, a diagnosis module and an information output module; the sample information processing module is used for receiving patient subject information, wherein the subject information at least comprises information of DBP gene variation and / or CYP2A6 gene variation; the diagnosis module receives information input of the sample information processing module, obtains blood drug concentration probability according to the information, and outputs medication guidance suggestion by the information output module.

The utility model discloses a novel oven transfer tray belongs to transfer tray technical field, include: stainless steel protective shell, the rear end left side hinged of stainless steel protective shell has the door of rotation, the rear end right side fixedly connected with handle of door of rotation, dust adsorption mechanism, the front end mounting of stainless steel protective shell has dust adsorption mechanism, the inner chamber bottom of stainless steel protective shell is installed with fixed plate, the upper end mounting of fixed plate has tray mechanism, through the stainless steel filter screen, conveniently make tacrolimus crude product in the process of oven drying play the function of dust prevention, through dust adsorption mechanism, conveniently in the transfer process of this device, the tacrolimus crude product powder generated in stainless steel protective shell is adsorbed and is recycled and is used, avoids the internal dust and scatters, thereby causes the staff contact, through tray mechanism, conveniently the tacrolimus crude product of drying on the tray is vibrated, and the tray is separated with tacrolimus crude product conveniently.

A blood test method includes: a preparation step of preparing whole blood collected from a subject; a pretreatment step for preparing a sample for analysis by pretreating the whole blood; a separation step in which the sample for analysis is separated by components using a liquid chromatograph; and an analysis step for analyzing the separated component using a mass spectrometry device, the subject being administered with a first immunosuppressant comprising at least one substance selected from the group consisting of tacrolimus, cyclosporin A, everolimus, and sirolimus, and with a second immunosuppressant comprising at least one substance selected from the group consisting of cyclosporin A, everolimus, and sirolimus. The second immunosuppressive agent contains at least one substance selected from the group consisting of mycophenolic acids and metabolites thereof, the separated component contains the first immunosuppressive agent and the second immunosuppressive agent, and when the first immunosuppressive agent is analyzed as a target component in the analysis using the mass spectrometry device, the first immunosuppressive agent is separated from the target component, and when the second immunosuppressive agent is separated from the target component, the second immunosuppressive agent is separated from the target component. When the first immunosuppressive agent is analyzed as a target component, analysis is performed in a positive ion pattern, and when the second immunosuppressive agent is analyzed as a target component, analysis is performed in a negative ion pattern.

The present disclosure relates to methods for the treatment of diseases or disorders (e.g., cancer) with mTOR inhibitors. Specifically, the disclosure relates to methods of treating a subject having a cancer by administering a particular dosage of an mTOR inhibitor. In some embodiments this disclosure includes methods for delaying, preventing, or treating acquired resistance to RAS inhibitors using a dosage of an mTOR inhibitor. In some embodiments, this disclosure relates to methods of treating or preventing adverse events associated with administration of an mTOR inhibitor using tacrolimus.

The application relates to the technical field of computers and discloses a tacrolimus dosage prediction method based on a clustering model combination, which comprises a data preprocessing module, a clustering and grouping module, a concentration prediction module, a dosage recommendation module and a display module. A patient grouping modeling end is arranged, seven clinical indexes are integrated by using a clustering algorithm, subgroups with large metabolic characteristic differences are divided, the limitation that patients are regarded as homogeneous groups in a traditional model is broken through, subgroup-specific modeling is realized, the group specificity of dosage prediction is improved, a subgrouping and prediction joint architecture is constructed, a model is independently deployed for each subgroup after subgrouping and dimension reduction, the sample quantity required by a single model is effectively reduced, the failure risk of machine learning under a small sample is reduced, reliable modeling can be realized in hundreds of clinical data, a dynamic prediction modeling end is arranged, memory functions are generated by fusing multi-time point historical data, and the prediction deviation rate caused by initial value disturbance is reduced.

This invention relates to a method for producing high-purity tacrolimus, which involves removing impurities with similar chemical structures but lacking unsaturated alkyl groups (particularly astemine (FK520) and propyl analogues of tacrolimus) from process products containing unsaturated alkyl lactone compounds (particularly tacrolimus (FK506)). More specifically, the invention provides an economical purification method that recovers high-purity tacrolimus in high yield by dissolving the tacrolimus process product in an aqueous solution of silver ions and then using a small amount of adsorption resin to remove similar impurities that do not bind to silver ions.