89 results about "Sulbactam" patented technology

A compound anti-beta-lactamase antibiotic is prepared from cefuroxime or its salt, sulbactam or its salt, and tazobactan or its salt. Its advantages are broad spectrum and high antibacterial effect.

The invention relates to an improved therapy for treating resistant bacterial infections caused by extended-spectrum β-lactamase (ESBLs)-producing strains in a warm-blooded animal, adjuvant step down therapy, and pharmaceutical compositions for such therapies. The invention also relates to a method for inhibiting bacterial resistance in ESBLs-producing strains so as to have better control over the therapy; achieve reduced hospital stay and adjuvant step down therapy so as to avoid recrudescence. In particular, the therapy includes antibacterial combination of cefepime with sulbactam via parenteral route, followed by oral third generation cephalosporin with a suitable β lactamase inhibitor.

The invention discloses a preparation process for compound recipe ceftiofur oil suspensoid injection. The preparation process comprises the following steps: (1) taking neutral soybean oil, filtrating, heating and sterilizing and cooling down the soybean oil, adding aluminum stearate into the soybean oil to prepare gel, diluting the gel into factice of 2+-0.2 percent through the filtrated and sterilized soybean oil, and filtrating the factice through a No.3 sintered glass funnel for standby; and (2) taking hydrochloric acid ceftiofur / sulbactam according to a recipe, mixing the hydrochloric acid ceftiofur / sulbactam with the factice, grinding the mixture, adding lecithin into the mixture till the mixture is ground evenly, and then obtaining the compound recipe ceftiofur oil suspensoid injection through shifting the ground hydrochloric acid ceftiofur / sulbactam into a graduated cylinder and so on. As the invention adopts the preparation method, compared with a single recipe ceftiofur preparation, the compound recipe ceftiofur oil suspensoid injection has the advantage that the compound recipe ceftiofur oil suspensoid injection has antibacterial activity against bacteria capable of resisting the single recipe ceftiofur, that is, the compound recipe ceftiofur oil suspensoid injection can effectively treat bacterial infection generating ESBLs.

The invention involves antibiotic compound recipe containing piperacillin, sulbactam or clavulanic acid, ion chelator which can inhibit the formation of particles chelator, the recipe can be further added in buffering ingredient as stability system, the characteristics of the recipe is that it can be prepared to stable pharmaceutical solutions, and with aminoglycoside antibiotics in the same container are re-prepared to drugs used for complex anti-microbial infection.

The invention relates to a detection kit and a detection method of raw milk and milk products, in particular to a detection kit and a detection method for beta-lactamase in raw milk and milk products. At present, no diary corporation in China can carry out production with the raw milk completely supplied by self-owned farms. All diary corporations need to purchase raw milk from dairy farmer to some extent. Thus, the detection of imparities and antibiotics becomes extremely important. The detection method adopts a standard strain of bacillus stearothermophilus absolutely sensitive to penicillin antibiotics, uses the specificity of sulbactam to inhibit the activity of the beta-lactamase, adds ampicillin as a reference and contrasts inhabitation zones of a sample with a beta-lactamase inhibitor and a sample without the inhibitor to detect the antibiotics. The detection kit comprises a sterilized culture dish with a vacuum package, a beta-lactamase standard product, a freeze-drying cillin bottle containing ampicillin and ampicillin and sulbactam, a blank filter paper sheet and a diluent. The detection kit and the detection method have the advantages of low cost, convenient and quick operation and high sensitivity.

The invention provides a method for detecting related substances in piperacillin sodium and sulbactum sodium for injection. The method adopts an octadecyl silane bonded silica-gel chromatographic column to carry out gradient elution so as to rapidly and precisely complete the detection on related substances in piperacillin sodium and sulbactum sodium. In the obtained chromatogram, the main related substance (2S)-2-amino-3-methyl-3-sulfinobutyric acid and piperacillin penicilloic acid are well separated, piperacillin and sulbactum are also well separated from other related substances, and the separation degree is more than 1.5. The degradation researches and methodology on piperacillin sodium and sulbactum sodium show that the provided method has a stability indicating function, and thus the detection method can be used to control the limits of impurities in piperacillin sodium and sulbactum sodium, and can also be used to control the quality of piperacillin sodium and sulbactum sodium for injection. The method has the advantages of convenient operation and low cost, and has a good economic profit and promotion prospect.

The invention discloses a sulbactam preparation method. In the method, 6-amino penicillanic acid (6-APA) serving as a raw material undergoes a dibromination reaction with bromine serving as a bromating agent in the presence of sulfuric acid or hydrobromic acid; the product of the dibromination reaction is oxidized by potassium permanganate; the product of the oxidization is subjected to debromination by using zinc powder or magnesium powder as a reducing agent; and thus, the sulbactam is prepared. In a manganese dioxide removing process in an oxidization phase, 50-percent sulfuric acid and 20 to 28-percent hydrogen peroxide are added alternately; in a pH value adjusting process in a reduction phase, the pH value is adjusted by adding sodium bicarbonate; and in a layer-based extraction process in the reduction phase, an organic layer is washed by 4 to 10 percent solution of potassium permanganate first till red color is stable and then washed by saturated aqueous solution of sodium chloride. Thus, byproducts are reduced, the yield of main products is increased, the product is very stable and avoids turning yellow, and a good basis is provided by down-stream products.

The invention discloses a synthesizing method of sulbactam acid. The method comprises the steps that: (1) under the existence of a strong acid, 6-aminopenicillanic acid, a diazotization reagent, and bromine or bromide are subjected to an insulation reaction in an organic solvent; excessive bromine is reduced; and a reaction product is extracted to a water layer; (2) an oxidant is dropped into the water-layer reaction product, and an insulation reaction is carried out; when the reaction is finished, a pH value is regulated; excessive potassium permanganate is reduced; an organic solvent is added, such that a reaction product is extracted to an organic solvent layer; (3) a catalyst is added into the organic-solvent layer product, such that hydrogenation bromine-removing is carried out; a reaction product is extracted to an organic-solvent layer; and distillation and crystallization are carried out. The organic solvent is ethyl acetate. According to the invention, ethyl acetate is adopted as the organic solvent in a four-step reaction, such that solvent consumption of the whole reaction is greatly reduced, and product total yield is effectively improved. With the method provided by the invention, by-product in the reaction can be comprehensively utilized, and advantages such as high yield, low cost, clean production, and the like are provided.

The present invention relates to a preparation method of sulbactam. Said method includes the following steps: using palladium-carbon as catalyst, using hydrogen gas as reducing agent, making dibromopenicillanic sulfone acid undergo the process of debromination and reduction at 0.2-0.6MPa, then making the reaction product undergo the processes of adsorption treatment by means of active carbon and purification so as to obtain the invented sulbactam whose yield is above 90%.

The invention relates to a rapid detection method for melamine and sulbactam in liquid milk, and belongs to the technical field of liquid milk analysis. In the rapid detection method, a sample is extracted through an acetic acid water solution, subjected to protein sedimentation through acetonitrile and diluted, Acquity UPLC BEH HILIC(100*2.1mm, i.d., particle diameter of 1.7 micrometers) separation is carried out, and electrospray ion source multi-reaction monitoring (MRM) mode tandem mass spectrum measurement is carried out. An extracting solvent, extracting time, purifying time, instrument measurement conditions and the like are optimized. Results prove that melamine and sulbactam have the good linear relation within the range of 0.02-20 ng / mL and 0.05-100 ng / mL respectively, and the correlation coefficient is larger than 0.99. In the high, middle and low addition levels, the recovery rate of practical samples is between 82.5% and 103.5%, the relative standard deviation (RSD n=6) is between 0.9% and 5.1%, and the method quantification limit of melamine and sulbactam is 10 micrograms per kilogram and 1.0 microgram per kilogram respectively. Pretreatment operation is simple and rapid, hydrophilic interaction chromatography-tandem mass spectrometry detection sensitivity is high, and qualitative and quantitative operation is accurate.

The invention provides an anti-Acinetobacter baumannii drug combination and an application thereof. The drug combination contains meropenem and sulbactam with the weight ratio of meropenem to sulbactam being 1:2-4. The invention is designed by a checkerboard method. The synergetic antibacterial effect of the combined use of meropenem and sulbactam to carbapenems sensitive and drug resistant Acinetobacter baumannii is found by broth microdilution detection. As shown in the test result, no matter meropenem drug resistant strain or meropenem sensitive strains, most of them show a synergetic and partly synergetic effect to the combined use of meropenem and sulbactam and the strains which show a synergetic effect account for 25%.

The invention discloses a method for preparing sulbactam and belongs to the technical field of pharmaceuticals. The method is characterized in that a 'one-pot' method is adopted, starting from 6-aminopenicillanic acid (6-APA), under the action of sodium nitrite and hydrobromic acid, a reaction solution which contains product 6 alpha-penicillanic acid is obtained through bromination reaction, and then, solid sulbactam is obtained through further oxidation and reduction reaction. The solid sulbactam is directly prepared during the reaction preparation process without separation, thus the method is simple to operate and easy for industrial production; the method adopts single-bromination reaction to substitute double-bromination reaction; moreover, bromine which has greater pollution is not used as a raw material, but hydrobromic acid is taken as a raw material, and the method is simple to operate and is low in cost; and the sulbactam solid which is prepared through the method is high in yield and good in quality.

The invention relates to a method for separation and enrichment of penicillin antibiotics in water. The method comprises the following steps of adjusting a pH value of a water sample to 2-4 by an acid; filtering the water sample to obtain a pretreated water sample; activating an HLB solid-phase extraction column by acetone, methanol and a formic acid aqueous solution containing ammonium acetate successively; adding ultrapure water to keep a resin in the HLB solid phase extraction column in an activated state; passing the water sample through the column; drying the HLB solid-phase extraction column under the protection of nitrogen after enrichment is finished; eluting with an eluent; collecting the eluent; blow-drying under a nitrogen flow; adding acetonitrile to dissolve residual materials for detection; and detecting the concentrations of penicillin antibiotics quantitatively. The method is advantageous in that the pretreatment of the water sample is environment-friendly; and the method can be operated easily, has high enrichment coefficient, low detection limit and good repeatability, and can analyze the content of two trace penicillin antibiotics in a water environment rapidly and accurately.

Pharmaceutical compositions and methods for treating or preventing bacterial infections are disclosed. The pharmaceutical compositions typically comprise pharmaceutically effective amount of: (a) sulbactam or a pharmaceutically acceptable salt thereof, and (b) at least one beta-lactamase inhibitor or a pharmaceutically acceptable salt thereof, with the provision that the beta-lactamase inhibitor is not sulbactam.

The invention belongs to the field of chemical synthesis, and specifically to a synthesis method for sulbactam. According to the method, 6-APA is adopted as a raw material, and bromine is adopted as a brominating agent to carry out a diazotization-bromination reaction; the resulting material is oxidized into sulfone through potassium permanganate; finally the sulfone is subjected to hydrogenation reduction in the presence of a catalyst to prepare the sulbactam, wherein the total yield of the product is 75%. The main characteristics of the method of the invention are that: in the step (1), hydrobromic acid is adopted as the medium so as to increase the reaction conversion rate; in the step (2), a phase transfer catalyst is introduced, and a brominated quaternary ammonium salt is adopted to catalyze the two-phase reaction, such that characteristics of high yield, recovery of the catalyst, and the like are provided; in the step (3), Raney nickel is adopted as the catalyst to catalyze the hydrogenation reduction reaction so as to improve the purity and the total yield of the product. Compared to the traditional process, the method of the present invention has the following advantages that: the process conditions are reasonable, the operation is safe and reliable, the production cost is low, and great practical values and economic benefits are provided.

The present invention discloses an antibiotic composition. It includes the following components: cefmenoxime or cefmenoxime salt or hydrate of cefmenoxime salt or cefmenoxime ester or precursor medicine of cefmenoxime as active component, and beta-lactamase inhibitor as inhibitor; the described beta-lactamase inhibitor is clavulanic acid or sulbactam or tazobactam or clavulanic acid medicinal salt or its hydrate or precursor medicine of clavulanic acid or sulbactam medicinal salt or its hydrate or tazobactam medicinal salt or its hydrate or tazobactam ester or precursor medicine of tazobactam. The mixing ratio of both cefmenoxime and inhibitor (by weight portion) is 1:0.1-99.

The invention discloses a detection method for sulbactam in milk. The method comprises: (1) detecting the antibiotics in the antibiotic positive control group, the β-lactamase positive control group and the sample group respectively, wherein, the antibiotic positive control group is obtained by incorporating antibiotic-free, β-lactamase Amase and sulbactam milk mixed with antibiotics obtained; the β-lactamase positive control group is obtained by mixing milk without antibiotics, β-lactamase and sulbactam, antibiotics and β-lactam Amidase is obtained by mixing; the sample group is obtained by mixing the milk to be tested, antibiotics and β-lactamase; (2) based on the detection results, the sulbactam in the milk to be tested is qualitatively determination. The method of the invention can accurately detect the sulbactam in milk and is easy to operate.

The invention discloses a broad spectrum and efficient composite antibacterial agent and a preparation method thereof. The preparation method comprises the following steps of: taking cefoperazone or physiologically-acceptable salt thereof, cefradine or physiologically-acceptable salt thereof, sulbactam or physiologically-acceptable salt thereof as active ingredients; adding acceptable carriers orminor ingredients; and adopting a certain preparation technology to prepare into various clinically applicable preparations. Compared with other antibacterial agents, according to the antibacterial agent disclosed by the invention, the antibacterial activity against G+ bacteria is 2-8 times of that of the traditional cephalosporin antibacterial agent, and the antibacterial activity against G-bacteria is 2-4 times of that of the traditional cephalosporin antibacterial agent and is 2.5-10 times of other traditional antibacterial agents. The antibacterial agent can overcome the defect of drug resistance of bacteria caused by unreasonable application of the clinical antibacterial drug, and has obvious advantages showed by wide antibacterial spectrum when being used for treating pathogen infection and infection with unclear sensitivity condition, in particular severe infections or mixed infections caused by fungi. The preparation cost of the broad spectrum and efficient composite antibacterial agent is economical, the preparation method is simple and easy to operate, and the preparation technology is environmentally-friendly.

The present invention belongs to the field of medicine technology, relates to compound antibiotic medicine capable of inhibiting bacteria produced beta-lactamase, and is especially compound antibiotic azlocillin / sulbactam medicine. The compound antibiotic azlocillin / sulbactam medicine is compounded with azlocillin and sulbactam or its derivative in the weight ratio of 1-16 as the active components. Azlocillin and sulbactam in the compound medicine has obvious synergistic effect, and the compound medicine can inhibit the activity of beta-lactamase and protect azlocillin against the destruction of bacteria produced beta-lactamase, is favorable to the antibiotic effect of azlocillin in strengthen antibiotic activity, widened antibiotic spectrum, less resistance and raised clinical treating effect.

The invention discloses a synthetic method for tazobactam. The method comprises the following steps: adding propiolic acid, 2 beta-azidomethyl penicillanic acid-1 beta-oxide, sodium ascorbate and a catalyst containing cuprous ions or copper ions to a solvent in sequence; stirring and reacting these materials for 0.5-72 h at 20-180 DEG C; and after the reaction is finished, extracting a reactant and carrying out column chromatography on the reactant so as to obtain the tazobactam. Through the method, the synthetic method for the tazobactam, disclosed by the invention, has the advantages as follows: the tazobactam is a novel sulbactam type beta-lactamase inhibitor and can be used for treating a plurality of bacterial infections; and compared with a method with acetylene as raw material, the method has the advantages as follows: through using the propiolic acid as the raw material, the safety in the reaction process is enhanced and an electricity absorbing carboxyls on a molecule is beneficial for carrying out cycloaddition reaction and preferably compatible with a reaction substrate; the reaction condition is mild; the reaction can be conducted at normal temperature; the operation process is convenient and simple; the yield of obtained products is high; and industrial production can be carried out on a large scale.

The invention relates to an antibiotic compound containing piperacillin, sulbactam or clavulanic acid, and an ionic chelating agent capable of inhibiting particle generation. The compound can be further added with a buffer component as a steady system. The compound is characterized by being prepared into a steady solution preparation and prepared into a medicine for resisting microbial infection together with aminogylcoside antibiotics in the same container.

The present invention discloses one kind of compound beta-lactamase resisting antibiotic preparation, and is especially compound preparation comprising Cefonicid and its salt and Sulbactam and its salt or Tazolbactum and its salt in the weight ratio of 0.5-10. The weight ratio between Cefonicid and its salt and Sulbactam and its salt is 0.5-6, preferably 1, and weight ratio between Cefonicid and its salt and Tazolbactum and its salt is 1-6, preferably 2. Compared with Cefonicid, the present invention has ever wide antibiotic spectrum and ever strong antibiotic effect.

The invention relates to the field of medicine synthesis and provides a synthesis method of sulbactam acid, aiming at the problem of low yield of a traditional synthesis manner. The synthesis method comprises the following steps: S1, carrying out diazotization and bromination reaction: adding bromine, a dilute sulfuric acid solution and a sodium nitrite solid into 6-aminopenicillanic acid, whereinthe concentration of the dilute sulfuric acid solution is 20 to 25 percent; reacting to obtain a first intermediate; S2, carrying out oxidization reaction: dropwise adding potassium permanganate andthe dilute sulfuric acid solution into the first intermediate, wherein the concentration of the dilute sulfuric acid solution is 20 to 25 percent; S3, carrying out hydrogenation reaction: dropwise adding zinc powder and the dilute sulfuric acid solution into a second intermediate and reacting to obtain the sulbactam acid. The dilute sulfuric acid solution with the concentration of 20 to 25 percentis used for reacting, which facilitates the improvement of the activity of the diazotization and bromination reaction and the oxidization reaction, and reactants are enabled to react more completely,so that the improvement of the yield of the diazotization and bromination reaction and the oxidization reaction is facilitated, and the total yield of the reaction is further improved.

The present invention is directed to combinations of a β-lactamase inhibitor with sulbactam and, optionally, imipenem / cilastatin. The combinations are useful for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant pathogens. More particularly, the invention relates to a combination of β-lactamase inhibitor compound 1: or a pharmaceutically acceptable salt thereof, with sulbactam, or a pharmaceutically acceptable salt thereof, and, optionally, imipenem / cilastatin, or a pharmaceutically acceptable salt thereof.

The invention discloses a synthesis method of an amoxicillin artificial antigen, and belongs to the technical field of biochemical industry. The synthesis method comprises the following steps: coupling an amoxicillin parent nuclear structural analogue sulbactam and an amoxicillin hapten to obtain a novel amoxicillin hapten, then coupling the hapten and bovine serum albumin (BSA) by an isobutyl chloroformate method, and dialyzing to obtain an amoxicillin complete antigen. Through gel electrophoresis analysis on the complete antigen and a BSA protein band, a result shows that the amoxicillin is successfully coupled to the BSA, and an antibody obtained through animal immunization confirms the successful synthesis of the artificial antigen. By the synthesis method, the molecular weight of the amoxicillin is increased, the immunogenicity of the amoxicillin is further enhanced, the immunizing effect is enhanced, and an important basis is provided for preparation of a high-sensitivity amoxicillin antibody.

The invention provides a breast perfusion preparation for treating mammitis of milk cow in lactation period, which belongs to the field of medical preparation for veterinary use; every 3g of the perfusion preparation contains 150-250 mg of amoxicillin, 50-125 mg of sulbactam, 5-15 mg of prednisolone and the rest of substrate; the substrate contains 0.1-12% of suspending aid, 0.1-2% of wetting agent, 0.01-1% of antioxidant, 0.05-1% of preservative and the rest of dispersion medium; the invention can be obtained via the following steps: firstly, dissolving or dispersing suspending aid, antioxidant, wetting agent and preservative into proper amount of dispersion medium, then slowly adding the rest of the dispersion medium into a colloid mill to obtain the substrate, adding medicine into the substrate, grinding via the alternating method of circularly grinding and non-circularly grinding. The preparation of the invention is simple in preparation technique, easy to realize industrialization, low in production cost, low in expenditure for treatment, low in toxicity, wide to use and high in efficiency; the invention can be clinically used for treating mammitis in lactation period caused by Gram positive bacterium and Gram negative bacterium.

The invention discloses a synthesizing method of sulbactam acid. The method comprises the steps that: (1) under the existence of a strong acid, 6-aminopenicillanic acid, a diazotization reagent, and bromine or bromide are subjected to an insulation reaction in an organic solvent; excessive bromine is reduced; and a reaction product is extracted to a water layer; (2) an oxidant is dropped into the water-layer reaction product, and an insulation reaction is carried out; when the reaction is finished, a pH value is regulated; excessive potassium permanganate is reduced; an organic solvent is added, such that a reaction product is extracted to an organic solvent layer; (3) a catalyst is added into the organic-solvent layer product, such that hydrogenation bromine-removing is carried out; a reaction product is extracted to an organic-solvent layer; and distillation and crystallization are carried out. The organic solvent is ethyl acetate. According to the invention, ethyl acetate is adopted as the organic solvent in a four-step reaction, such that solvent consumption of the whole reaction is greatly reduced, and product total yield is effectively improved. With the method provided by the invention, by-product in the reaction can be comprehensively utilized, and advantages such as high yield, low cost, clean production, and the like are provided.

The invention discloses an anti-beta-lactamase antibiotic compound preparation, which is specifically a compound preparation composed of cefuroxime and its salt, sulbactam and its salt, or tazobactam and its salt. The weight ratio range of cefuroxime and its salt and sulbactam and its salt or tazobactam and its salt in the compound preparation is 1:1 to 10:1; cefuroxime and its salt and sulbactam and its The preferred weight ratio range of its salt is 2:1 to 6:1, the optimum weight ratio is 4:1, the preferred weight ratio range of cefuroxime and its salt and tazobactam and its salt is 1:1 to 6 : 1, the optimum weight ratio is 2: 1. Compared with cefuroxime, the invention has wider antibacterial spectrum and stronger antibacterial effect.

The antibiotic medicine composition is mixture of cefpiramide and beta-lactamase inhibitor in the weight ratio of 1 / 3 to 10. The cefpiramide may be replaced with alkali metal salt of cefpiramide or the mixture of cefpiramide, sodium carbonate and arginine. The beta-lactamase inhibitor may be clavulanic acid or its derivative, sulbactam or its derivative, or tazobactum or its derivative. The antibiotic medicine composition has high antibiotic effect, especially on sensitive bacteria and zymogenic bacteria, and wide antibiotic spectrum.