19 results about "Voriconazole" patented technology

This invention belongs to the field of intelligent healthcare, specifically relating to a personalized dosing method for sirolimus combined with voriconazole in the treatment of PID in children. The method includes: obtaining the age of the PID child; determining the sirolimus dosage when combined with voriconazole based on the PID child's age; if the PID child's age is in the range of [1, 6) years, the dosage is [0.100, 0.330] mg / QD; if the age is in the range of [6, 13) years, the dosage is [0.280, 0.540] mg / QD. This application is the first to develop a PPK model for PID children using sirolimus combined with voriconazole (VRC), and based on the PPK, explores the optimal dosage for PID children using sirolimus combined with VRC, providing concise dosage guidance for children of different age groups; and through posterior Bayesian methods, it can provide individualized sirolimus medication guidance.

The invention provides an application of a fusarium verticillium transcription factor FVEG06682 in regulating the sensitivity of fusarium to azole drugs, and belongs to the technical field of drug resistance. The invention provides an application of a fusarium verticillium transcription factor FVEG06682 in regulating the sensitivity of fusarium to azole drugs or regulating the toxicity of fusarium to plants, and the FVEG06682 improves the sensitivity of fusarium to azole drugs and reduces the toxicity of fusarium to plants through negative regulation. Therefore, the transcription factor is identified and proved to be a key molecule for regulating and controlling the intrinsic resistance of the azole drugs in the fusarium verticillium for the first time, and the sensitivity of pathogenic bacteria to various clinical and agricultural azole drugs (such as ketoconazole, voriconazole, triazolone and tebuconazole) can be remarkably improved by knocking out the FVEG06682 gene; a brand-new and efficient molecular target is provided for overcoming the inherent drug resistance problem of fusarium.

The invention discloses a nano-robot based on tear driving, a preparation method of the nano-robot and application of the nano-robot in eye drops. The preparation method comprises the following steps: step 1, loading ophthalmic disease treatment drugs such as amphotericin B, voriconazole and natamycin into nano-particles such as polylactic acid-glycolic acid copolymer, chitosan and sodium alginate; 2, coupling urease on the surfaces of the nano-particles to obtain a nano-robot with autonomous movement ability; step 3, performing morphology characterization on the obtained nanometer robot driven by the tear liquid; and step 4, dispersing the prepared tear-driven nano-robot in a buffer solution to prepare the eye drops. The tear-driven nano-robot can utilize urea in tears as fuel to generate cluster motion on the cornea surface, so that the retention time is remarkably prolonged, the drug retention amount is increased, and the treatment effect is improved. The nano-robot eye drops based on tear driving have biocompatibility and treatment safety, and have wide application prospects in the field of ophthalmic local administration.

This invention relates to the field of biomedical technology, specifically to an antifungal nanoparticle, a combination drug, and its application. The antifungal nanoparticle is prepared by covalently linking the aptamer AU1 to drug-loaded silk fibroin nanoparticles via amide bonds. The mass ratio of the drug-loaded silk fibroin nanoparticles to the aptamer AU1 is 20:0.5~2.0. The antifungal nanoparticles of this invention are prepared by a desolvation method using voriconazole-loaded silk fibroin nanoparticles, and the targeting aptamer AU1 is attached to their surface using a carbodiimide chemical cross-linking method. This allows for specific recognition of Candida albicans, increasing drug accumulation at the infection site. Further combination with methylene blue-mediated photodynamic therapy can disrupt biofilm structures, enhance nanoparticle penetration, achieve synergistic bactericidal activity, and reduce systemic toxicity, providing a novel, highly effective, and low-toxicity treatment strategy for fungal biofilm infections.

The invention relates to a voriconazole dry suspension. The voriconazole dry suspension comprises the following components: 2-4 parts of voriconazole; 36 to 41 parts of isomaltitol; 1-4 parts of a microcrystalline cellulose-sodium carboxymethyl cellulose compound; 0.1 to 0.5 part of colloidal silicon dioxide; 0.2 to 1.0 part of sodium lactate; 0.05 to 0.2 part of disodium hydrogen phosphate; 0.05 to 0.5 part of essence; 0.1-0.3 part of a preservative; the dry suspension disclosed by the invention has the characteristics of high settling volume ratio, excellent stability and remarkably improved dissolution rate.

This invention discloses the application of primer sets for identifying polymorphic site combinations in the preparation of a kit for predicting voriconazole metabolism, and the kit itself. The polymorphic site combinations include rs4244285, rs4986893, rs3740066, rs4149056, and rs4646437. This invention enables effective prediction of voriconazole blood concentrations, overcoming the lag and empirical limitations of traditional therapeutic drug monitoring.

Disclosed in the present invention are antifungal compounds, a preparation method therefor, and the use thereof. The compounds have the following general formula I, wherein L represents a linking moiety, referring to a small molecule fragment, and Ar represents a heterocyclic ring or a substituted heterocyclic ring. The series of compounds of the present invention can better bind to an enzyme target by means of various interaction forces, thereby exhibiting good activity; and the compounds exhibit excellent activity in both in vitro experiments and animal experiments, the activity of most of the compounds against Candida albicans being better than that of fluconazole. In addition, the series of compounds have anti-inflammatory effects while eliminating fungal infections; and compared with voriconazole, the series of compounds of the present invention can remarkably down-regulate the expression of an inflammatory factor interleukin 6.

This invention provides an electrospun gastric perforation patch based on Ag / Zn bimetallic MOF and its preparation method. The gastric perforation patch comprises a tissue integration layer, an antibacterial drug-loaded core layer, and an anti-adhesion layer integrally formed by electrospinning. The antibacterial drug-loaded core layer is composed of Ag / Zn bimetallic MOF loaded with antifungal drugs and a biodegradable polymer material. In the Ag / Zn bimetallic MOF, the molar ratio of zinc to silver is (8:1) to (12:1), and the antifungal drug is voriconazole or amphotericin B. This invention combines the broad-spectrum antimicrobial properties of Ag / Zn bimetallic MOF with a three-layer functional gradient design, enabling the patch to adhere firmly to tissue without sutures. It can actively prevent infection, inhibit adhesion, promote tissue regeneration, and gradually degrade and absorb postoperatively, significantly reducing the risk of foreign body reaction, infection, and recurrence, demonstrating excellent biocompatibility and broad clinical application prospects.

The invention relates to the technical field of medical artificial intelligence, and discloses an artificial intelligence-based voriconazole hepatotoxicity occurrence risk prediction method, which comprises the following steps of: firstly, obtaining a medical record data set containing basic information of a patient, medicine information, inspection information and a research end point index, and performing cleaning and conversion treatment to obtain a medical record data set; a random forest, a naive Bayes algorithm and a limit gradient lifting algorithm are respectively adopted to construct a model, the performance of the model is evaluated through 5-fold cross validation in combination with multiple indexes, and an optimal liver injury endpoint index and a corresponding prediction model are determined; identifying a core risk factor by using the feature importance and an SHAP method; and finally, inputting medical record data of a patient to take medicine to obtain a risk assessment result, and automatically generating a medicine adjustment suggestion in combination with a risk threshold. According to the method, voriconazole hepatotoxicity risk accurate prediction and medication guidance are realized, and medication safety is improved.

The invention relates to the field of medicines, in particular to a compound and application thereof. The compound is shown as a formula I, and also comprises pharmaceutically acceptable salts, prodrugs, tautomers, stereoisomers, isotope derivatives or solvates of the compound. The compound disclosed by the invention has good antifungal activity, particularly has exact and excellent inhibition and antibacterial activity on candida, cryptococcus and rhizopus arrhizus, and also has excellent antibacterial activity on voriconazole drug-resistant bacteria. The compound can be used for preventing and / or treating various diseases caused by fungal infection.

The application adopts a gene knockout method of homologous recombination to knockout a gene sequence of an ABC transport protein coding gene Af-ABC in Aspergillus fumigatus, and has very important scientific significance and application value for studying growth, virulence and sensitivity to voriconazole of Aspergillus fumigatus, and researching new targeted drugs for the gene and the coded protein, and screening aspergillosis treatment drugs.

The present application relates to the field of pharmaceutical preparations, and discloses a voriconazole freeze-dried powder injection and a preparation method thereof.The freeze-dried powder injection comprises voriconazole, sulfobutyl betacyclodextrin, sorbitol, sodium chloride and methanesulfonic acid, and the solubility and stability of the drug are significantly improved by optimizing the proportion of the excipients and the pH value (4.0-5.0). Experiments show that in the accelerated test (40℃±2℃, 75%RH) and the long-term stability test (25℃±2℃, 60%RH), the content decrease rate is ≤3%, the total impurities are ≤0.1%, the moisture is ≤0.5%, and the effective period can reach 24 months. In addition, after reconstitution, the compatibility with various clinical diluents (such as 0.9% sodium chloride and 5% glucose) is good, without precipitation or degradation. The present application solves the problems of high toxicity of excipients, poor stability and easy precipitation of diluents in the prior art, and has significant clinical application value.

The present invention discloses a voriconazole and multivitamin compound freeze-dried powder injection, and relates to the technical field of pharmaceutical preparations, the voriconazole and multivitamin compound freeze-dried powder injection comprises: an active component comprising voriconazole or a pharmaceutically acceptable salt thereof, and a multivitamin system composed of at least one water-soluble vitamin and at least one fat-soluble vitamin; the stable system comprises a microenvironment regulating agent containing fat-soluble vitamins and an antioxidant synergist for the whole system; and freeze-drying the skeleton agent. According to the voriconazole freeze-dried powder injection disclosed by the invention, fat-soluble vitamins are clathrated by adopting a microenvironment regulating agent to form a water dispersible compound, and a specific antioxidant synergist and a freeze-dried skeleton agent system are combined, so that voriconazole, water-soluble vitamins and fat-soluble vitamins with different chemical properties can stably and uniformly coexist in the same freeze-dried powder injection.

The invention belongs to the field of detection, and particularly discloses a method for simultaneously detecting concentrations of six drugs in blood, and the method comprises the following steps: detecting a sample to be detected by using liquid chromatography-mass spectrometry, and determining the content of the drugs in the sample to be detected according to a detection result and a standard curve, the medicine is prepared from meropenem, vancomycin, voriconazole, linezolid, tacrolimus and cyclosporine A. The invention further discloses a preparation method of the medicine. According to the invention, LC-MS / MS is adopted to simultaneously detect the blood concentration of six drugs in blood, and the method has the advantages of high separation degree, high sensitivity, high accuracy, fast detection speed and the like, provides a reliable basis for clinical precise medication, and improves the safety and effectiveness of immunosuppressor combined antibacterial drug treatment.

The MFSmt gene reveals the role of voriconazole in treating Aspergillus fumigatus under the condition of pathogenicity: the deletion of MFSmt gene leads to the increase of amphotericin B resistance and the increase of voriconazole sensitivity in Aspergillus fumigatus. This finding suggests that if the drug that makes the MFSmt gene deletion or reduces the amount of expressed protein is used in clinical treatment, it can be combined with voriconazole to have a more effective bactericidal effect, and at the same time, the use of amphotericin B should be avoided to prevent drug resistance. This has important clinical value for determining the treatment plan for effective treatment of clinical Aspergillus fumigatus infection and controlling drug-resistant strains.

The invention discloses a method for simultaneously determining the concentrations of Venoclarias, Selanisol, voriconazole and fluconazole in human plasma, and belongs to the technical field of drug analysis and treatment drug monitoring. The invention aims to solve the problem that the prior art is lack of a method for synchronously monitoring the blood concentration of four drugs of'vinca + Sanisole 'double-targeted chemotherapy and'voriconazole + fluconazole' antifungal scheme. The method is characterized by comprising the following steps: taking a plasma sample, precipitating protein through an internal standard solution and an organic solvent, and taking supernatant as a test solution; carrying out gradient elution by adopting a C18 chromatographic column and taking an aqueous solution containing formic acid and an organic solvent as mobile phases; detecting elution components by adopting an electrospray ionization source positive ion mode and a multi-reaction monitoring mode; and finally calculating the concentrations of the four drugs according to a detection result by an internal standard method. The method is mainly used for rapid and synchronous treatment drug monitoring when a clinical patient jointly uses the four drugs, and a basis is provided for accurate dose adjustment.

The invention provides a voriconazole inhalation dry powder inhalation. The voriconazole inhalation dry powder inhalation comprises the following components in parts by weight: 60-80 parts of voriconazole; 20.3-30 parts by weight of a phospholipid emulsifier; 1.4 to 2.5 parts by weight of a divalent cation chloride; 0-11 parts by weight of a crystal inhibitor; and no flow aid is contained. Compared with the prior art, by selecting the specific emulsifier and adopting the divalent cation chloride as the emulsion stabilizer, honeycomb structures and wrinkles are generated on the surfaces of the drug particles, so that the specific surface area is increased, the aerodynamic performance of the particles is better, the particles are easier to deliver to the lung, and the purpose of increasing the effective delivery dosage is achieved; and sugar glidants such as lactose do not need to be added, so that the possibility of layering of active ingredients and inactive ingredients in a pharmaceutical preparation process is avoided, and the stability of a preparation process can be effectively improved.

The application discloses a detection kit for simultaneously determining the concentrations of 12 kinds of antibiotic drugs in trace serum and application, the 12 kinds of antibiotics including vancomycin, meropenem, imipenem, cilastatin, trimethoprim, linezolid, voriconazole, piperacillin, cefoperazone, sulfamethoxazole, cefepime and ceftazidime; the detection kit comprises pretreatment reagents and a liquid chromatography mobile phase; the pretreatment reagents comprise a protein precipitant and purified water; the protein precipitant comprises 50v / v% of methanol and 50v / v% of acetonitrile; the liquid chromatography mobile phase comprises phase A and phase B, the phase A comprises 0.02% of formic acid and 99.98% of water, and the phase B comprises 100% of acetonitrile. The method of the application only needs 10 muL of human serum sample, and can complete the detection within 4 min, can quantitatively determine 12 kinds of antibiotics with significant structural differences, and is simple, rapid, sensitive, accurate and specific.

The invention relates to the technical field of drug detection, in particular to a method for detecting five potential genotoxic impurities in a voriconazole bulk drug, and the method comprises the following steps: detecting the genotoxic impurities in the voriconazole bulk drug by adopting a high performance liquid chromatography-tandem mass spectrometry to obtain the content of the genotoxic impurities; wherein the high performance liquid chromatography takes a formic acid aqueous solution as a mobile phase A and a formic acid methanol solution as a mobile phase B. By adopting the high performance liquid chromatography-tandem mass spectrometry method, exclusive separation of voriconazole and five genotoxic impurities can be realized, and the content of each genotoxic impurity can be sensitively detected. According to the method, the sample treatment mode is simple, multiple genotoxic impurities can be detected at the same time, and the detection method is high in specificity, good in sensitivity and good in repeatability and durability.