78 results about "Glycopeptide antibiotic" patented technology

In one aspect, the invention provides a stabilized lipid-based glycopeptide antibiotic composition and a process for producing the same. In another aspect, the invention provides methods for treating a bacterial pulmonary infection by administering to a subject in need thereof a therapeutically effective amount of the stabilized lipid-based glycopeptide antibiotic composition.

The invention relates to a method for preparing glycopeptides antibiotic teicoplanin, which comprises the following steps: after teicoplanin fermented solution is subjected to filtration, adsorption by macroporous resin and decoloring by active carbon, the decoloring solution is concentrated and desolventizing by nanofilteration or hyperfiltration to obtain the teicoplanin water solution with high concentration, and then the teicoplanin is deposited from the solution by adjusting pH, adding salt or adjusting pH and adding salt simultaneously, and the mixture is filtered to obtain teicoplanin. The effective ingredients of the teicoplanin obtained through deposition are obviously improved, and other impurities are reduced. Meanwhile, the appearance color of the product is improved obviously.

Disclosed are pharmaceutical compositions containing a cyclodextrin and a therapeutically effective amount of a glycopeptide antibiotic or a salt thereof. Also disclosed are methods of treating a bacterial disease in a mammal by administering such pharmaceutical compositions.

In one aspect, the invention provides a stabilized lipid-based glycopeptide antibiotic composition and a process for producing the same. In another aspect, the invention provides methods for treating a bacterial pulmonary infection by administering to a subject in need thereof a therapeutically effective amount of the stabilized lipid-based glycopeptide antibiotic composition.

Novel glycopeptide antibiotic derivatives, processes for their preparation, their use as a medicine, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections are provided. The present invention relates to the use of glycopeptide antibiotics and their semisynthetic derivatives to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses belonging to Retroviridae, Herpes viridae, Flaviviridae and the Coronaviridae, like HIV (human immunodeficiency virus), HCV (hepatitis C virus), BVDV (bovine viral diarrhoea virus), SARS (severe acute respiratory syndrome) causing virus, FCV (feline coronavirus), HSV (herpes simplex virus), VZV (varicella zoster virus) and CMV (cytomegalovirus).

This invention is directed to a novel method of treating an individual suffering from a bacterial infection, such as bacterial infections of various tissues or organs of an individual. In general, the method of treatment involves administering to an individual a pharmaceutical formulation that comprises a liposome-encapsulated antimicrobial agent, wherein polyethylene glycol (PEG) molecules are covalently attached to the surface of the liposomes.

Solutions comprising a glycopeptide antibiotic, for example Vancomycin, and an amino acid or amino acid derivative such as N-acetyl-Glycine or N-acetyl-D-Alanine are provided. These solutions are stable or stabilized for long-term periods at conditions of normal use and storage, and can be formulated as pharmaceutical solutions for use in subjects. Methods of manufacturing and using these solutions are also provided, as are methods of stabilizing a glycopeptide antibiotic, for example Vancomycin, using amino acids or amino acid derivatives such as N-acetyl-Glycine or N-acetyl-D-Alanine.

The invention discloses a glycopeptide antibiotic derivative shown as a general formula (I) and pharmaceutically accepted salt thereof, and a preparation method thereof. R1 represents C3-9 saturated fatty alkyl, decylamine methyl or an aromatic group, which is unsubstituted or substituted phenyl ring, biphenyl ring or naphthalene ring; and a substituent of the phenyl ring, biphenyl ring or naphthalene ring is one or more selected from the group of halogen, hydroxy, amino, C1-9 alkyloxy, nitro and isopropyl. R2 represents H or CH2-R3. R3 represents C3-9 saturated aliphatic hydrocarbon group. In addition, the invention also provides a pharmaceutical composition containing the glycopeptide antibiotic derivative and pharmaceutically acceptable salt thereof as active components, and application thereof. The compound and pharmaceutical composition provided by the invention have good antibiosis activity and great significance for development of novel antibacterial medicament.

Drug delivery systems for delivering agents capable of reducing the quantity of residual antibiotics reaching the colon following oral or parenteral antibiotic therapy, and for delivering metallo-dependent enzymes, and methods of using the drug delivery systems, are disclosed. The drug delivery systems include pectin beads that encapsulate the active agent (which can be a metallo-dependent enzyme), where the pectin is crosslinked with zinc or any divalent cation of interest and the pectin beads are coated with Eudragit®-type polymers. The drug delivery systems are orally administrable, but can deliver the active agents to the colon. In some embodiments, they can administer the agents to various positions in the gastro-intestinal tract, including the colon. One metallo-dependent enzyme is the β-lactamase L1 from Stenotrophomonas maltophilia, and agents that inactivate macrolide, quinolone, fluoroquinolone or glycopeptide antibiotics can also be used. The delivery of the active agent can be modulated to occur at various pre-selected sites of delivery within the intestinal tract by gelling / crosslinking a mixture of the active agent, such as a metallo-dependent enzyme, and pectin, with divalent metallic cations such as Ca+2 or Zn+2. A stable metallo-dependent enzyme formulation can be delivered to the lower intestine or colon. The use of zinc cations to crosslink the pectin is particularly preferred when specific metallo-dependent enzymes, which are Zn2+ dependent, could interact with other cationic species if they were used to gel the pectin beads and thus adversely affect the activity of such metallo-dependent enzymes.

The invention discloses a method for simultaneously detecting various glycopeptides antibiotics in animal derived food. The method mainly comprises the following steps: carrying out solution extraction on a sample; carrying out series purification and enrichment by using HLB solid-phase extraction columns and strong cation (MCX) solid-phase extraction columns; separating the sample by using reversed phase columns, and then detecting the sample by using an ultra-efficient liquid chromatography tandem mass spectrometry in a multi-reaction monitoring mode; and carrying out qualitative and quantitative analysis. Five glycopeptides antibiotics including telavancin, teicoplanin, oritavancin, dalbavancin and vancomycin in the sample animal derived food such as milk, eggs and chicken can be detected simultaneously. The detecting method is sensitive, accurate and rapid; and the five glycopeptides antibiotics can be qualitatively and quantitatively analyzed by six minutes displayed on an instrument. Moreover, the detecting method also has certain reference value for detection of other glycopeptides antibiotics.

An antibiotic polymer combination / antibiotics polymer combination that ensures the continuous release of antibiotics over a period of several days under physiological conditions, and that can be used in human and veterinary medicine. Surprisingly, one or more antibiotic salts, which are sparingly soluble in water, from the groups comprising aminoglycoside antibiotics, lincosamide antibiotics, tetracycline antibiotics, glycopeptide antibiotics, quinolone antibiotics and chlorhexidine, are suspended in homogeneous polymer mixtures, which comprise one or more hydrophobic, nonionic polymers from the groups comprising poly(vinyl, chloride), post-chlorinated poly(vinyl chloride), poly(vinylidene chloride), poly(vinyl fluoride), poly(vinylidene fluoride) and copolymers comprising vinyl chloride and one or more nonionic monomers, and which comprise one or more hydrophilic polymers from the groups comprising polyethers, and this suspension forms composites that exhibit the release of an active ingredient over a period of days in an aqueous medium.

Drug delivery systems that can deliver therapeutic and / or diagnostic agents to the colon are disclosed. The systems include pectin beads crosslinked with zinc or any divalent cation of interest, which beads are then coated with Eudragit TM -type polymers. The drug delivery systems are orally administrable, but can deliver the active agents to the colon, or, in some embodiments, to various other positions in the gastro-intestinal tract. The agents can be used to diagnose, treat, prevent, or investigate a variety of conditions, including infectious diseases, inflammatory diseases, cancers and the like. Certain agents, such as metallo-dependent enzymes, for example, ss-lactamase Ll from Stenotrophomonas maltophilia, as well as agents that inactivate macrolide, quinolone, fluoroquinolone or glycopeptide antibiotics, can reduce the quantity of residual antibiotics reaching the colon following antibiotic therapy.

Disclosed is a method and apparatus for determining a concentration of a glycopeptide antibiotic containing a phenol moiety such as Vancomycin in a complex sample matrix by extracting the glycopeptide antibiotic from a metered portion of the complex sample matrix by exposing said metered portion to an extraction material having an affinity with the glycopeptide antibiotic; and exposing the extraction material to a metered portion of an eluent for releasing the glycopeptide antibiotic from the extraction material; and by determining a concentration of the glycopeptide antibiotic by adding a Gibbs reagent (2,6 dichloroquinone-4chloroimide) to the metered portion of the complex sample matrix or the eluent; activating the Gibbs reagent and, after the reaction between the activated Gibbs reagent and the antibiotic has stabilized; detecting the reaction product of the activated Gibbs reagent and the antibiotic in said eluent; and determining the concentration of the antibiotic in the complex sample matrix from the detected reaction product. A method of designing a personalized drug administration regime using the thus obtained concentration is also disclosed.

Novel glycopeptide antibiotic derivatives, processes for their preparation, their use as a medicine, their use to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections are provided. The present invention relates to the use of glycopeptide antibiotics and their semisynthetic derivatives to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections of subjects, more in particular infections with viruses belonging to Retroviridae, Herpes viridae, Flaviviridae and the Coronaviridae, like HIV (human immunodeficiency virus), HCV (hepatitis C virus), BVDV (bovine viral diarrhoea virus), SARS (severe acute respiratory syndrome) causing virus, FCV (feline coronavirus), HSV (herpes simplex virus), VZV (varicella zoster virus) and CMV (cytomegalovirus).

The invention provides compounds of formula Wherein R1, R2, R3, R4, R5, R6a, R6b, R6c, R6d, R6e and R7 are defined in the specification. These compounds are useful as antibiotic agents.

The invention discloses a kit for simultaneously detecting triazole antifungal drugs and glycopeptide antibiotics, the kit comprises an extracting solution, a diluent, a mobile phase, a calibrator anda quality control material, the calibrator and the quality control material comprise fluconazole, voriconazole, posaconazole, itraconazole, vancomycin and teicoplanin; wherein the extracting solutioncomprises an isotope internal standard substance and a methanol aqueous solution, and the isotope internal standard substance comprises fluconazole-d4, voriconazole-d3, posaconazole-d4 and itraconazole-d5; wherein the diluent is distilled water or ultrapure water. The invention has the advantages that the invention firstly provides a kit capable of detecting a micromolecular antifungal drug and simultaneously detecting macromolecule glycopeptide antibiotics; the kit is simple in sample pretreatment and short in pretreatment time, improves the detection efficiency, can detect multiple types ofmedicines, can meet the detection requirements of clinically high-throughput samples, has a very good application prospect, and is convenient to popularize.

The invention relates to a preparation method for a multi-mode-combined vancomycin stationary phase of chromatography. The preparation method comprises the following steps: modifying the surface of asilicon sphere with an amino group; then with glutaraldehyde as a spacer, bonding the macrocyclic glycopeptide antibiotic vancomycin onto the surface of the silicon sphere through an aldimine condensation reaction; and carrying out bonding and terminating by using small-molecular amino acids or sugar so as to prepare the multi-mode-combined chiral stationary phase of chromatography. A vancomycin structure has a plurality of function groups and is applicable to separation operation in different chromatographic separation modes; moreover, glutaraldehyde is used as the spacer for bonding the macrocyclic glycopeptide antibiotic onto the surface of the silicon sphere, so steric-hinerance effect is effectively reduced and bonding efficiency is improved; and termination via small molecules can shield the negative effect of residual silicon hydroxyl groups in chromatographic separation, provide more action sites of different types and improve separation efficiency and separation selectivity.

Glycopeptide antibiotics, such as oritavancin, demonstrate significant activity against B. anthracis. Methods for the treatment, prophylaxis and prevention of B. anthracis infection and disease in animals, including humans, are described.

The invention relates to a pharmaceutical composition, particularly to a pharmaceutical composition with antitumor activity. The pharmaceutical composition with antitumor activity comprises 5,6-dimethylxanthenone-4-acetic acid (DMXAA) or an pharmaceutically acceptable salt or ester thereof and one drug component selected from glycopeptide antibiotics, actinomycins, mitomycins, glucoside antibiotics, Colchicum alkaloid, elemenes, aromatic enzyme inhibitors, LH-RH receptor antagonists, animal antitumor drugs and somatostatin analogues. The synergic composition has better antitumor activity. More specifically, the invention provides an application of the composition in treating tumors.

The invention discloses a molecularly imprinted microsphere for detecting teicoplanin and a preparation method and application thereof. The preparation method includes: selecting a molecule similar toa glycosyl portion in a teicoplanin molecular structure as a template molecule, 4-vinylphenylboronic acid and methyl methacrylate as functional monomer and divinyl benzene as a crosslinking agent toprepare the molecularly imprinted microsphere. When pH value is 9.0, the synthesized molecularly imprinted microsphere can be combined with target glycopeptide antibiotic; when the pH value is loweredto below 4.0, the combined glycopeptide antibiotic can be released, so that a glycosyl molecularly imprinted solid-phase extraction column prepared on this principle can intercept the glycopeptide antibiotic in the solid-phase extraction column in a slightly alkaline condition, then the glycopeptide antibiotic is eluted in an acidic condition. On the basis of the glycosyl molecularly imprinted solid-phase extraction column, teicoplanin in serum and urine samples can be detectedly effectively, and the molecularly imprinted microsphere has high recovery rate, low detection limit and good application prospect.

The invention discloses a group of glycopeptides compounds with anti-resistance bacterial activity. The glycopeptides compounds in accordance with a general formula (I) are as shown in the following specification. The invention further provides a preparation method and an application for the above glycopeptides compounds. Through testing, compared with a second-generation glycopeptides pharmaceutical oritavancin, the glycopeptides antibiotic compounds have the higher inhibitory activity to endurance strains, especially MRSA or VRE. Through further testing, the most of the glycopeptides compounds have the higher safety than the oritavancin, and can be used for preparing pharmaceuticals for treating or preventing various diseases, such as skin and soft tissue infection, cephalomeningitis, sepsis, pneumonia, arthritis, peritonitis, bronchitis, and empyema, caused by bacterial infection.

The invention discloses a vancomycin derivative as well as a preparation method and a pharmaceutical use thereof. The invention belongs to the technical field of medicines and relates to a glycopeptide antibiotics derivative substituted by heterocyclic nitrogen with a general formula (1) as shown in the specification, a pharmaceutically acceptable salt of glycopeptide antibiotics derivative, an isomer of the glycopeptide antibiotics derivative, a preparation method of the compounds and uses of the compounds in preparation of medicines for treating or preventing bacterial infectious diseases. An extraneous bacteriostasis experiment shows that the antimicrobial activity of the compounds is 60 times the antimicrobial activity of vancomycin or norvancomycin, particularly the bacteriostatic activity of the compounds to various gram-positive bacteria is obviously higher than that of vancomycin or norvancomycin. Thus, by adopting the preparation method, medicines containing the derivative as an active ingredient can be prepared, particularly medicines resisting to bacterial infection. The structure formula is as shown in the specification.

Glycopeptide antibiotics, such as oritavancin, demonstrate significant activity against both a vegetative form of C. difficile and C. difficile spores. Methods for the treatment, prophylaxis and prevention of C. difficile infection and disease in animals, including humans, are described.

The invention provides compounds of formula Wherein R1, R2, R3, R4, R5, R6a, R6b, R6c, R6d, R6e and R7 are defined in the specification. These compounds are useful as antibiotic agents.

The invention discloses a temperature-sensitive gel pharmaceutical preparation and a preparation method thereof. The raw material formula of the temperature-sensitive gel pharmaceutical preparation contains a drug, a temperature-sensitive gel composition, and an excipient C; the excipient C is one or more of metal salts, carbohydrates, and hydrophilic polymers for injection; The metal salt is a pharmaceutically acceptable metal salt that dissociates divalent metal cations in an aqueous solution; the drug is a substance A that exists in an anion form in an aqueous solution, and the substance A is a protein drug, a polypeptide One or more of class drugs and glycopeptide antibiotics. The preparation method comprises the following steps: according to the formula of raw materials, the drug is dissolved in the temperature-sensitive gel composition in the form of solution. The temperature-sensitive gel pharmaceutical preparation is especially suitable for water-soluble drugs, reduces the burst release effect, releases the drugs slowly, and achieves the purpose of sustained release.

The present invention relates to the field of antibiotics, and more specifically to the isolation of nucleic acid molecules that code for the biosynthetic pathway of the glycopeptide antibiotic A40926. Disclosed are the functions of the gene products involved in A40926 production. The present invention provides biosynthetic genes that code for A40926 production, the encoded polypeptides, the recombinant vectors comprising the nucleic acid sequences that encode said polypeptides, the host cells transformed with said vectors and methods for producing glycopeptide antibiotics using said transformed host cells, including methods for producing A40926, a precursor thereof, a derivative thereof or a modified glycopeptide different from A 40926 or a precursor thereof.