78 results about "Tacrolimus" patented technology

The present invention relates to the use of cannabidiol (CBD) in the treatment of patients with childhood-onset epilepsy who are concurrently taking immunosuppressant drugs. In particular the immunosuppressant drug is a calcineurin inhibitor. More particularly the immunosuppressant drug is tacrolimus. Where the CBD is used in combination with an immunosuppressant drug, caution should be taken. For example, the dose of either the CBD and / or the immunosuppressant drug may be required to be reduced. Moreover, the patient may need to be monitored for side effects of said drug-drug interaction. Preferably the CBD used is in the form of a highly purified extract of cannabis such that the CBD is present at greater than 98% of the total extract (w / w) and the other components of the extract are characterised. In particular the cannabinoid tetrahydrocannabinol (THC) has been substantially removed, to a level of not more than 0.15% (w / w) and the propyl analogue of CBD, cannabidivarin, (CBDV) is present in amounts of up to 1%. Alternatively, the CBD may be a synthetically produced CBD.

The invention relates to the field of drug concentration detection, in particular to a rapid tacrolimus drug concentration detection device based on a micro-fluidic chip. The detection device comprises a blood sampling area, a separation area, a liquid medicine storage area, a waste liquid storage area and a spectrograph, the separation area is used for separating a tacrolimus medicine in a blood sample solution, and a liquid medicine sample and a waste liquid sample are obtained; the spectrograph is used for collecting liquid medicine spectral data of the liquid medicine sample in the liquid medicine storage area and waste liquid spectral data of the waste liquid sample in the waste liquid storage area, and detecting the concentration of the tacrolimus medicine in the blood sample solution according to the liquid medicine spectral data and the waste liquid spectral data. According to the invention, the accuracy of detecting the concentration of the tacrolimus drug in the blood can be improved.

The invention discloses a tacrolimus detection kit and application thereof. The tacrolimus detection kit comprises a reagent R1, a reagent R2, a reagent R3, a standard substance, a reagent tube A, a reagent tube B, a reagent tube C and a freeze-drying bottle, wherein the reagent tube A, the reagent tube B, the reagent tube C and the freeze-drying bottle are respectively used for the reagent R1, the reagent R2, the reagent R3 and the standard substance; the reagent R1 is a magnetic bead antibody working solution; the reagent R2 is an enzyme-labeled antigen working solution; the reagent R3 is a blood sample treatment solution, which is a TBS buffer solution containing EDTA-2Na (Ethylene Diamine Tetraacetic Acid), a zinc sulfate solution, Triton X-100 and ProClin300; the standard substance is a freeze-dried whole blood standard substance containing tacrolimus. According to the tacrolimus detection kit and the application thereof, the general blood sample treating fluid is adopted, so that the reliability and the stability of a detection result of tacrolimus in a blood sample are improved.

The invention provides application of FXR protein as a target spot in preparation of a medicine for relieving and / or treating renal toxicity of tacrolimus, and belongs to the technical field of biological medicine. The invention proves that the activity or expression level of the FXR protein is regulated in a targeted manner, so that the Tacrolimus-induced renal tubule epithelial cell vacuolation and renal tubule injury can be effectively prevented or relieved, and the abnormal rise of early renal injury markers such as urine NAG enzyme and the like is reduced, thereby directly improving the renal toxicity problem of Tacrolimus. The invention provides a new drug action target and a treatment strategy for clinic, and by developing an FXR agonist or a gene intervention means, the long-term renal injury risk of tacrolimus can be reduced while the anti-rejection curative effect is maintained, the transplanted kidney function and the survival time of a patient are prolonged, and the clinical application prospect is wide. And an effective means is provided for solving the unsatisfied clinical demand of the renal toxicity of the tacrolimus after the transplantation operation.

The present invention discloses an active exosome scaffold coating based on traditional Chinese medicine enhanced secretion, its preparation method and application, belonging to the technical field of biomedicine and interventional devices. The scaffold coating of the present invention includes: exosomes, including cardiomyocyte active exosomes and human mesenchymal stem cell active exosomes enhanced by traditional Chinese medicine; wherein, the traditional Chinese medicine includes: placenta extract, pilose antler extract, sheep myocardial peptide, sea cucumber peptide, black wolfberry peptide, osthole, curculigo rhizome extract, and morinda officinalis extract; the intervention concentration of each component added to the cells is 2-50 μg / mL; a photocurable gel matrix, including methacrylated gelatin, a photoinitiator, and polyether 127; tacrolimus; the final concentration of exosomes is 1×10 9 ~12×10 9 particles / mL, and the final concentration of tacrolimus is 5-25 μg / mL. This coating can be coated on the surface of a poly-L-lactic acid degradable stent to prepare a degradable stent, which has obvious ability to promote blood vessel repair.

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.

A cobalt-chromium alloy stent comprising several main body units, wherein each main body unit is composed of several supporting rings connected by flexible ribs and the adjacent main body units are connected by several connecting ribs. A drug eluting stent comprising the cobalt-chromium alloy stent and a drug coating containing arsenic trioxide and tacrolimus. The drug release curves of the two composite drugs of arsenic trioxide and tacrolimus used in the present invention are adjusted, so that the inflammatory response of vascular endothelial cells and the proliferation behavior of vascular smooth muscle cells are effectively inhibited, and the vascular restenosis rate is reduced.

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 application of tacrolimus in preparation of a medicine for treating type 2 diabetes and complications thereof, and belongs to the field of biological medicine. Animal experiments prove that Tacrolimus (TM) can effectively improve type 2 diabetes mellitus and obesity-related abnormal glycolipid metabolism. In addition, the TM can also relieve liver injury caused by diabetes and obesity and improve liver fatty degeneration and abnormal lipid metabolism. What's more important is that toxicity of TM to pancreatic beta cells is not observed in long-term multi-model experiments (including diabetes, obesity and elderly mice). The invention provides an important basis for developing novel diabetes treatment drugs, lays a foundation for expanding new indications of tacrolimus, and has potential clinical transformation value.

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.

The invention discloses application of naringenin in preparation of a medicine for preventing and treating cardiotoxicity induced by tacrolimus. The naringenin disclosed by the invention is a natural active matter, is non-toxic to cells, and has a potential heart protection effect of reversing, preventing and treating tacrolimus-induced cardiotoxicity; naringenin reduces expression of Cav1.2 on a membrane so as to influence a calcium signal channel and reverse calcium overload and cell apoptosis caused by tacrolimus; cav1.2 can be used as a target spot for preventing and treating cardiotoxicity induced by FK506, and the invention also prompts that overload calcium can be treated by using a corresponding calcium chelating agent, so that a theoretical basis is provided for the naringenin as a potential auxiliary medicine for tacrolimus application; the further deep research is expected to be beneficial to deep understanding of the action mechanism of the naringenin and provide more support for clinical application of the naringenin.

A degradable biomedical magnesium alloy drug-eluting vascular stent and a preparation method. With the total weight of a magnesium alloy being 100% for calculation, the magnesium alloy comprises the following components in percentage by weight: 3.0-6.0% of Gd, 2.5-5.5% of Y, 1.0-3.0% of Li, 0.3-1.0% of Zn, 0.2-1.0% of Zr, and the balance being Mg. The stent has good radial support strength and strain dispersion capability by means of finite element design. After a protective coating is used, the corrosion resistance of the magnesium alloy stent is greatly improved. An arsenic trioxide / rapamycin and tacrolimus composite drug sustained-release system is used to fully adapt to the damage repair process of blood vessels. An implantation result of large animals shows that the vascular stent system has a good anti-restenosis treatment effect.

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.

A long acting injectable formulation based on combination of biodegradable poly(D,L-lactide-co-glycolide) microparticles comprising different PLGA polymers and Tacrolimus. The microparticles may include Tacrolimus, a first polymer and a second polymer, and the first and second polymer may differ from each other. Each of the first and second polymers may be a poly(D,L-lactide-co-glycolide) polymer. Each of the first and second polymers may have an identical lactide to glycolide ratio. Each of the first and second polymers may have a different molecular weight

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.

The application belongs to the technical field of biological medicine, and particularly relates to a double-drug microneedle of tacrolimus combined with siRNA and a preparation method and application thereof. The double-drug microneedle comprises a backing part and a needle tip part arranged on one side of the backing part, and the needle tip part is obtained by mixing and solidifying tacrolimus, siRNA targeting TNF-alpha, methacrylated gelatin, carrageenan and sodium alginate or by mixing and solidifying tacrolimus, siRNA targeting IL-6 and polyvinyl alcohol. The double-drug microneedle provided in the application simultaneously loads tacrolimus and TNF-alpha siRNA or IL-6 siRNA, realizes the administration of two therapeutic drugs at the same time by one microneedle, and experiments prove that the double-drug microneedle has a better therapeutic effect than the single tacrolimus microneedle.

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 present disclosure relates to buccal mucoadhesive patch formulation of tacrolimus loaded in the solid lipid nanoparticles and using the polymeric carrier matrix and pharmaceutically acceptable additives to deliver tacrolimus through the trans buccal route to the systemic circulation. The overall exposure to tacrolimus with the tacrolimus buccal mucoadhesive patch formulation of present invention is considerably higher compared to the conventional oral administration for equivalent dose. It provides an immediate and controlled release of tacrolimus by avoiding the first pass metabolism and providing a steady concentration of tacrolimus in the systemic circulation.

The present invention relates to a composition for topical application comprising:a first discontinuous phase comprising a first oil and tacrolimus;a second discontinuous phase comprising a second oil; anda continuous aqueous phase;wherein the first oil is different from the second oil.

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.