18 results about "Linezolid" patented technology

The invention relates to a method for detecting six second-line antituberculous drugs by high performance liquid chromatography. The method comprises the following steps: providing an internal standard stock solution and a standard stock solution of six second-line antituberculosis drugs; preparing an internal standard working solution and a standard curve working solution by utilizing the diluent; preparing a solution of a product to be detected by using the Tianlongitudinal sample extraction liquid TZ-002; a liquid chromatograph is used for detection, and the conditions are as follows: a mobile phase A is a Tianlongitudinal sample releasing agent TZ-D004; a mobile phase B is acetonitrile; a mobile phase C is water; and gradient elution. According to the method, the plasma concentration of the second-line antituberculous drug taken by a tuberculosis patient is measured by applying the reversed-phase high-performance liquid chromatography, the cost is relatively low, the analysis time is short, the sensitivity is high, and the accuracy is high. The kit can be used for simultaneously detecting the blood concentration of six second-line antituberculosis drugs such as isopropylthioamide, levofloxacin, linezolid, moxifloxacin, deramanib and bedaquiline in human serum, and is expected to provide a more reliable basis for clinicians to adjust the dosage of the antituberculosis drugs.

This invention relates to a 1,3,4-thiadiazole peptide deformylase inhibitor and its preparation and application. The structural formula is shown in formula (1): wherein, R 1 It is n-butyl or cyclopentylmethyl; R 2 The compounds are hydrogen-containing, straight-chain alkanes, cyclic alkanes, aromatic rings, substituted biphenyls, or heterocyclic rings. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention can effectively inhibit bacterial protein synthesis, thereby achieving sterilization. These compounds exhibit excellent inhibitory activity against Gram-positive drug-resistant bacteria, especially the clinically challenging methicillin-resistant Staphylococcus aureus (MRSA). In particular, some preferred compounds show inhibitory activity 4-8 times that of the control standards vancomycin and linezolid. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention also exhibit inhibitory activity against Gram-negative drug-resistant bacteria, especially against drug-resistant Acinetobacter baumannii, known as "superbugs," with an inhibitory activity reaching 0.5 μg / mL, far superior to vancomycin and linezolid.

The present disclosure relates to linezolid derivatives, in particular of Formula (I), the definition of p, A, A1 and R1 are as defined in the specification; the process of preparing the same and uses thereof in treatment of brain cancers, in particular glioblastoma.

The present invention relates to a co-administered formulation for alleviating anti-tuberculosis drug-induced toxicity comprising dead cells, and a pharmaceutical composition for preventing or treating tuberculosis comprising same. By co-administering Lactobacillus sakei CVL-001 or Lactobacillus reuteri NCHBL-005 as the dead cells with the anti-tuberculosis drug, the present invention exhibits excellent effects in alleviating drug toxicity (hepatotoxicity and nephrotoxicity) caused by the anti-tuberculosis drug, thereby increasing drug adherence of the anti-tuberculosis drug to obtain the effect of inhibiting the emergence of multidrug-resistant tuberculosis and recurrence of tuberculosis. In addition, the present invention can be used as an adjuvant for co-administration with drugs that have high efficacy despite significant side effects, such as bedaquiline or linezolid, with the expected effect of reducing the treatment period of tuberculosis, thereby being effectively used in the treatment process of tuberculosis.

A composition of fluticasone / linezolid-loaded nanodiamond / polyacrylonitrile nanofibers, consisting of: • Fluticasone propionate in a quantity of 25 mg to 100 mg; • Linezolid in a quantity of 25 mg to 100 mg; • Nanodiamonds dispersed in a concentration of approximately 1 mg / ml dimethylformamide (DMF); and • a polyacrylonitrile (PAN) polymer matrix prepared as a 10% w / v solution in DMF, wherein the drugs, nanodiamonds and PAN are uniformly combined to form an electrospinnable nanocomposite solution, and electrospinning is carried out under conditions suitable for producing nanofibers with controlled drug release, porosity and structural integrity for wound healing applications.

The invention discloses a linezolid tablet containing a coating layer and a preparation method of the linezolid tablet, and relates to the technical field of pharmaceutical preparations, the linezolid tablet comprises a linezolid tablet core and a coating film layer wrapping the surface of the linezolid tablet core; the coating film layer is prepared from the following raw materials in percentage by mass: 5%-10% of acetic acid-cellulose butyrate, 2%-3% of glutamine, 0.5%-1% of carbodiimide, 3%-5% of cane sugar, 0.1%-0.5% of polyethylene glycol and the balance of an organic solvent. The linezolid tablet prepared by adopting the preparation method disclosed by the invention not only can slow down the release speed of a medicine, prolong the retention time of the medicine in a body and enable the medicine effect to be slowly and lastingly played, but also has a certain moisture-proof function due to the coating layer, and prolongs the shelf life of the medicine.

The invention relates to the technical field of medicine synthesis, and particularly discloses a synthesis method of high-purity N-carbobenzoxy-3-fluoro-4-morpholinyl aniline. According to the method, the dehalogenation inhibitor is added to participate in the reduction reaction, so that the purpose of reducing the content of defluorination impurities in the 3-fluoro-4-morpholinyl aniline can be achieved, the purity of the N-carbobenzoxy-3-fluoro-4-morpholinyl aniline is further effectively improved, and a new design thought is provided for preparation of high-purity linezolid. According to the technical scheme, the problems that in the prior art, due to the fact that the content of defluorination impurities in 3-fluoro-4-morpholinyl aniline is high, the content of the defluorination impurities in N-carbobenzoxy-3-fluoro-4-morpholinyl aniline is high, the purity of the defluorination impurities in the N-carbobenzoxy-3-fluoro-4-morpholinyl aniline is low, the drug effect of linezolid is reduced, and follow-up large-scale production is not facilitated are effectively solved.

The present application relates to the preparation method of 3-phenyl-5-aryl-1,2,4-oxadiazole by electro-oxidation, and the preparation reaction is as follows: wherein R is selected from hydrogen, 4-fluoro, 4-chloro, 2-bromo, 4-tert-butyl, 3-methyl or 3,4-dimethyl; Ar is selected from phenyl, 2-thiophenyl, 2-fluorophenyl, 4-chlorophenyl, 2-bromophenyl, 4-fluorophenyl or 4-methylphenyl. The preparation method of electro-oxidation is that (Z)-N'-hydroxy-N-(arylmethyl) benzamidine, organic solvent, base and electrolyte are used as electrolyte in a non-membrane electrolytic cell, and then constant voltage electrolysis is carried out at a certain temperature for a certain time, so that 3-phenyl-5-aryl-1,2,4-oxadiazole (I) is obtained by electro-oxidation reaction. The preparation method of electro-oxidation can be used for preparing line thiophene and ataluren.

The invention provides application of sitagliptin and related compounds thereof to preparation of a medicament for resisting microbial infection. The inventor of the invention finds that sitagliptin has a remarkable inhibition effect on microbial infection, especially infection caused by staphylococcus aureus, MRSA, enterococcus faecalis, MRSE and escherichia coli. Under the same dosage, the antibacterial effect of sitagliptin on staphylococcus aureus and MRSA exceeds that of a positive control drug linezolid. The biofilm inhibition effect of sitagliptin on MRSA is higher than that of linezolid under the same dosage. In addition, the sitagliptin sodium also has the effects of resisting staphylococcus aureus and MRSA (Methicillin Resistant Staphylococcus Aureus). Oral administration of the sitagliptin sodium can significantly reduce the level of MRSA in the heart, liver, spleen, lung, kidney and abdominal cavity of MRSA systemically infected mice. In addition, administration of sitagliptin at wounds promotes healing of MRSA infectious wounds. And a new thought is provided for the preparation of antibacterial drugs.

The application discloses pyridine-containing oxazolidinone compounds, a synthesis method and application thereof. A structural general formula of the pyridine-containing oxazolidinone compounds is shown in general formula I. In the application, a B ring phenyl ring of linezolid is replaced by a pyridine heterocycle, the introduction of the pyridine ring changes the distribution of the electron cloud, increases the basicity of the molecule, and further transforms a C ring. In order to further improve the antibacterial activity, fluorine is connected to the pyridine ring of part of the products, and the antibacterial activity is obviously improved. In-vitro antibacterial activity tests show that the pyridine-containing oxazolidinone compounds provided by the application all have definite antibacterial activity, and are expected to become substitutes of linezolid for clinical use.

The invention belongs to the technical field of clinical drug treatment monitoring, and discloses a risk prediction model for predicting the limit exceeding of the steady-state blood concentration of linezolid, and the model is a column diagram model constructed based on multi-factor Logistic regression analysis. The risk probability calculation module is used for calculating the risk probability that the blood concentration is greater than or equal to 8 mg / L according to clinical indexes of a patient; the input variables of the model comprise age, albumin level and serum creatinine level; the albumin level and the serum creatinine level are the albumin level and the serum creatinine level detected last time before blood concentration monitoring of the patient. The method is constructed based on real world data and verified by an independent queue, the model shows good distinguishing ability and calibration degree, and the prediction accuracy is good. The model only contains three clinically conventional easily available indexes of age, albumin and serum creatinine, and is presented in the form of a column diagram without complex calculation, so that clinical doctors can quickly complete risk assessment at the bedside.

1. The name of the design product: packing box (linezolid dry suspension). 2. The use of the design product: packing for linezolid dry suspension. 3. The design points of the design product: the combination of shape, pattern and color. 4. The picture or photo that best shows the design points: perspective view. 5. The design claimed contains color. 6. The view omitted: the bottom view of the product involved in the design patent application is not easy to see or not visible when used, so the top view is omitted.

The invention discloses a pharmaceutical composition containing a substance X, a substance Y and an optional substance z and application of the pharmaceutical composition in preparation of drugs for treating diseases caused by mycobacterium tuberculosis. The substance X is a compound I or a pharmaceutically acceptable salt thereof, and the substance Y and the substance Z are selected from pyrazinamide, linezolid, moxifloxacin, preremanib or deramanib. # imgabs0 #

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 invention relates to the field of medicinal chemistry, in particular to a biaryl oxazolidinone compound and application thereof. The invention relates to a biaryl oxazolidinone compound, which is a compound as shown in a general formula I, and a stereoisomer, a pharmaceutically acceptable salt, a solvate or a prodrug thereof. The compound provided by the invention has better antibacterial activity than linezolid, and has remarkable antibacterial activity on drug-resistant bacteria. Meanwhile, compared with linezolid, the compound has lower MAO inhibition and better safety.

The invention relates to the technical field of antibacterial capsules, in particular to a whole-body antibacterial capsule and a production process. An enteric coating layer; a slow release intermediate layer; the core antibacterial composition is prepared from ceftriaxone sodium microspheres, linezolid nanocrystals and Ga-EDTA (Ethylene Diamine Tetraacetic Acid) silicon dioxide nanoparticles. According to the invention, Ga-EDTA-silicon dioxide competitively inhibits iron metabolism, so that the killing ability of traditional antibiotics on bacteria in a biological membrane is remarkably enhanced, and the problem that a single drug does not reach a target spot in mixed infection is effectively solved. Secondly, due to the composite structure of the slow-release middle layer and the enteric coating layer, the intestinal targeting and continuous release of the medicine are realized, and the defects that the medicine in the traditional dosage form is inactivated in gastric acid and the blood concentration does not reach the standard are overcome. Moreover, the mesoporous structure of silicon dioxide prevents Ga < 3 + > from being captured by biofilm polysaccharide through a physical confinement effect, and the penetrability is enhanced by utilizing a stealth effect modified by PEG, so that the problem of insufficient permeation of a traditional anti-biofilm drug is directly solved.

Provided is a biaryloxazolidinone compound, wherein the compound is a compound of general formula I and a stereoisomer, pharmaceutically acceptable salt, solvate or prodrug thereof. The present invention relates to the field of pharmaceutical chemistry, and in particular to a bbiaryloxazolidinone compound and a use thereof. The compound has better antibacterial activity than linezolid and has significant antibacterial activity against drug-resistant bacteria. In addition, the compound exhibits lower MAO inhibition and better safety compared to linezolid.

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.