95 results about "Beta lactam antibiotics" patented technology

Class A beta-lactamase may be used for reducing side-effects in the intestine associated with antibiotic therapy with a combination of beta-lactam antibiotic and beta-lactamase inhibitor.

This invention provides beta-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a beta-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and / or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

The invention discloses the components and preparation method of beta-lactam injection. The beta-lactam injection comprises 5 to 20 percent of beta-lactam antibiotics, 0.05 to 5 percent of suspending agent, 0.005 to 0.3 percent of antioxygen, 0.1 to 0.2 percent of nonionic surfactant and the balance of vegetable oil or grease for injection. The injection can be used for preventing and curing animal bacterial infectious diseases and can be injected hypodermically or in muscle and be applied through breast for a few times. The preparation method provided by the invention comprises: firstly, making the antibiotics and the antioxygen into micro powder and making the suspending agent into fine powder; secondly, adding the vegetable oil or grease for injection, which is sterilized at high temperature, into the fine powder of the suspending agent, heating the mixture, uniformly mixing the mixture and keeping the mixture in a sterile environment to cool the mixture to room temperature for later use; and finally, transferring the prepared oil or grease added with the suspending agent to a colloid mill, adding medicament micro powder, the antioxygen and the non-ionic surfactant with stirring, and performing uniform mixing and sterilization to obtain the beta-lactam injection.

A pharmaceutical composition comprising: at least one aminoglycoside antibiotic and (a) at least one ion chelating agent used for inhibiting particulate formation, or (b) at least one buffer, or (c) at least one ion chelating agents and at least one buffer simultaneously. The composition for use in controlling microbial infection can be formulated into a solution, or combined with at least one beta-lactam antibiotic, or combined with at least one of beta-lactam antibiotic and at least one beta-lactamase inhibitor into a solution in a container.

The invention relates to targeted post translational modification of metallo-beta-lactamase by truncation and insertion of a dipeptide at the amino terminal end to reduce amino terminal heterogeneity in a recombinant DNA production system. A protein K-T-E-ΔBL is expressed, and modified by host proteases to E-ΔBL. Appropriate nucleotide molecules, vectors and hosts are also described. E-ΔBL is useful in a pharmaceutical composition for treating antibiotic induced adverse effects in the intestine of patients treated with beta-lactam antibiotics.

Stabilized preparations which contain a beta-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.

Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.

The present invention relates to a process for the preparation of Meropenem of formula (I) in sterile form and also provides an improved process for the preparation of compound of formula (V), which is an important intermediate in the synthesis of Meropenem.

A pharmaceutical composition comprising: at least one β-lactam antibiotic and at least one ion-chelating agent; wherein when said pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic.

A pharmaceutical composition, comprising: at least one β-lactam antibiotic and at least one buffer component; wherein when the pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic mixed with the β-lactam antibiotic and the buffer component.

The present invention relates to a convenient, flexible and cost-efficient technology for detection and resistance-profiling of bacteria, enabling effective, evidence-based treatment of infections. The invention provides methods and modular kits for the rapid and direct detection of beta-lactam resistant bacteria in a test sample, and optionally for susceptibility profiling of the bacteria, by directly determining hydrolysis product / s of beta-lactam antibiotic substrates in the tested sample. The invention also provides methods and modular kits for the rapid and direct detection of the presence of multidrug resistant bacteria in a test sample.

An improved stable pharmaceutical composition for controlled release of an active ingredient comprises a betalactam antibiotic such as cephalexin, cefaclor or their pharmaceutically acceptable hydrates, salts or esters as active ingredient, a calcium salt and a mixture of hydrophilic polymers selected from the group consisting of at least one sodium alginate and one xanthan gum and with or without hydroxypropyl methylcellulose, said composition optionally containing probenecid. The composition may also contain one or more of a water soluble and / or water dispersible diluent, wherein the quantities of the hydrophilic polymers and water soluble and / or water dispersible diluents are such that the therapeutically effective active ingredient is released at a rate suitable for once or twice daily administration of the pharmaceutical composition.

Administration of β-Lactam compounds, including β-lactam antibiotics and β-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.

Administration of β-Lactam compounds, including β-lactam antibiotics and β-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidence inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

The invention aims to provide a method for preparing a rapid detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay as well as a used detection method, aiming at solving the problem of sieve leakage in the process of detecting beta-lactam medicines in a traditional ELISA method. The invention discloses a method for preparing a detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay as well as an indirect competitive receptor assay method for detecting the content of beta-lactam drugs in milk by adopting the detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay. The methods have the beneficial effects that by utilizing the characteristic that the penicillin-binding protein 6 can be specifically bound to the beta-lactam drugs, the drugs can be specifically identified in a buffer liquid system or a sample matrix extracting solution and are not influenced by other antibiotics such as macrolides, quinolones and tetracyclines.

The invention relates to a method of rapidly degrading a beta-lactam antibiotic in water. The method concretely comprises the following steps: adding a certain quantity of peroxymonosulfate (PMS) as an oxidant in waste water which contains a beta-lactam antibiotic (such as cephalexin, i.e. CFX) at normal temperature and normal pressure, uniformly stirring, carrying out reaction for a period of time under a neutral condition while keeping a pH value of a system, and removing a pollutant with oxidative degradation. According to the method provided by the invention, the peroxymonosulfate as the oxidant has very high selectivity to the beta-lactam antibiotic, directly oxidizes and removes the pollutant without an additional persulfate activation step, is rapid in degradation with very little influence caused by other organic matters in a water body, and is more beneficial to removing the beta-lactam antibiotic in a polluted water body.

The invention discloses a midget anti drug-tolerance staphylococcus aureus polypeptide comprised of passage structure domain to form ion channel colicine and staphylococcus aureu pheromone, as well as opposite coded nucleotide sequence and recombination plasmid contained said sequence. Wherein, the plupeptide can not induce bacteria to generate trsditional drug-tolerance by the mechnism that it forms directly ion channel on cell film of target cell to kill bacteria. This invention has more single antimicrobial spectrum without effect to Gram-negative bacteria of escherichia coli, shows at least 500 times effect to pheneazonecillin, and can be used as synergist to beta-lactam antibiotics.

A bioluminogenic assay system including: providing a bioluminogenic substrate incorporating a beta-lactam antibiotic, a bioluminescence initiating compound, and a chemical linkage joining the beta-lactam antibiotic to the bioluminescence initiating compound; exposing the bioluminogenic substrate to a beta-lactamase enzyme that catalyzes the release of the bioluminescence initiating compound from the bioluminogenic substrate; co-exposing the bioluminogenic substrate to a bioluminescence indicator reaction that employs the bioluminescence initiating compound as a substrate; and detecting a light from the bioluminescence indicator reaction as a measure of the activity of the beta-lactamase enzyme.

The method to prepare high active extended spectrum beta-lactamase through directed evolution in vitro of the invention belongs to medical bioengineering technical field. In particular, the invention adopts two directed evolution strategies of error-prone PCR and DNA shuffling to transform a lab strain plant which contains TEM-1 gene. The substrate spectrum enzymes of the mutated strain plant and the wild strain plant, and the activity of the substrate spectrum enzymes are compared, showing that the original substrate spectrum is enlarged because of mutation and the degradability of the third representative generation of beta-lactam antibiotics ceftazidime (CAZ) and the cefotaxime (CTX) is improved from zero to a specific activity of 43IU / mg to 78IU / mg.

This invention provides beta-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a beta-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and / or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

The present invention relates to antibiotic synergism of pharmaceutical compositions comprising a defensin and a beta-lactam antibiotic.

The invention discloses new application of berberine. Berberine can be used as metal beta-lactamase inhibitor to be used for preventing compounds sensitive to metal beta-lactamase inhibitor from being hydrolyzed by enzymes, particularly hydrolysis of metal beta-lactamase for beta-lactam antibiotics, and antibiotics are protected.

The invention relates to a method for detecting beta-lactamase in a dairy produce. The method is characterized in that a fluorescence substrate probe which can be specifically catalyzed by beta-lactamase is designed, and the main structure of the fluorescence substrate probe is chemically synthesized through using the mother ring of fluorescein and beta-lactam antibiotic. The beta-lactamase can catalyze the fluorescence substrate probe to emit strong fluorescence, and the content of beta-lactamase is calculated according to the fluorescence intensity obtained through a reaction. 0.1ng / mL of Beta-lactamase can be detected through the method, the sensitivity of the method is two orders of magnitude higher than that of traditional ELISA methods, the detection time is shortened to 45min, and the method also has the advantages of strong specificity, high sensitivity, simplicity, rapid detection, and great reduction of the detection cost.

Compositions and methods for the treatment of antibiotic resistant Staphylococcus aureus infections are provided comprising β-lactam antibiotics, as well as a hyaluronic acid binding peptide. The antibiotics include cephalosporins as well as the ηoη-β lactam antibiotic vancomycin. The methods provide administering the composition to the subject in an amount effective to reduce or eliminate the infection.

The present invention discloses a method for producing novel lactam antibiotics by using specific engineered bacteria transformant BL21(DE3) / PET28-ASPGA. According to the method, a penicillin acylase amino acid sequence represented by SEQIDNO:1 is adopted as basis, a mutation site is introduced, reverse design is performed to obtain a nucleotide sequence, optimization is performed, complete gene synthesis and recombinant vector construction are sequentially performed to construct a recombinant strain, and the constructed recombinant strain is treated through steps of fermentation, cell disruption, separation, purification, decoloration and immobilization to finally obtain the novel lactam antibiotic immobilized enzyme finished product capable of being directly used for industrial production. According to the present invention, the immobilized enzyme prepared by using the method has characteristics of high enzyme activity, good stability and excellent repeated use effect, and can be provided for catalyzing synthesis of a variety of lactam antibiotics such as amoxicillin, cephalexin and cefaclor.

The present invention provides a β-lactam antibiotic such as cefepime and a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

The invention relates to a beta-lactam antibiotic solution, comprising beta-lactam antibiotic and a solvent, wherein the solvent is a mixing solvent formed by 2-pyrrolidone and propylene glycol; and 5-50g of beta-lactam medicine is dissolved in every 100mL of the mixing solvent. The preparation process of the solution is simple, and can adopt a nonaseptic raw material for preparation and a filtering method for degerming. The medicine is evenly dispersed in the solvent in a micromolecule mode which can be absorbed rapidly after entering the organism, can quickly enter the tissue and has high bioavailability, can be used for target animals without being frozen in the environment below 0 DEG C, does not need to oscillate and heat before being used, and can be taken orally, administrated outside intestinal tracts and locally administrated.

The present invention relates to a pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of Formula (I), compounds of Formula (I), the use of a therapeutically effective amount of one or more compounds of Formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.

A compound powder injection or freeze-dried powder injection is prepared from the sodium (or potassium) salt of probenecid and the beta-lactam kind of antibiotics including penicillin G, ampicillin, ancef, cefuroxime, cefotaxime and cefoxitin. It can elongate the half life of antibiotic, increase the AUC and plasma level and prevent the generation of drug-resistant bacteria.