65 results about "Azythromycin" patented technology

The invention relates to a norhalal-enoxacin conjugate as well as a preparation method and application thereof. The norhalal-enoxacin conjugate comprises a norhalal-enoxacin coupling compound, or a stereoisomer, a prodrug, a crystal form, a pharmaceutically acceptable salt, a pharmaceutically acceptable ester or a pharmaceutically acceptable solvate selected from the compound. Compared with enoxacin, kanamycin, streptomycin, lincomycin and azithromycin, the norharmann-enoxacin conjugate disclosed by the invention has a smaller MIC (Minimum Inhibitory Concentration) value, which shows that the norharmann-enoxacin conjugate has a better anti-staphylococcus aureus effect.

This disclosure describes the use of azithromycin, roxithromycin, and telithromycin, including derivatives thereof, as senolytic drugs. BrdU was used to induce senescence in model human fibroblast cell lines. Also disclosed are methods for screening compounds for senolytic activity. The SRB assay was used to measure cell viability through protein content. Azithromycin roxithromycin, and telithromycin, clinically-approved pharmaceuticals, were found to be senolytic drugs. However, the closely-related parent compound, erythromycin, showed no senolytic activity. Azithromycin strongly induced both aerobic glycolysis and autophagy in human fibroblasts, but showed bi-phasic effects including on mitochondrial oxygen consumption rates with inhibitory activity at 50 μM and stimulatory activity at 100 μM. The xCELLigence real-time assay system showed that azithromycin preferentially targets senescent cells, removing approximately 97% (nearly a 25-fold reduction in senescent cells).

The invention discloses a bacteriostatic composition which comprises a synergist and a bacteriostatic agent, the synergist is ethyl phenylacetate or a derivative thereof, and the bacteriostatic agent is selected from hydrogen peroxide, beta-lactam antibiotics, macrolide antibiotics and aminoglycoside antibiotics. The synergist disclosed by the invention is wide in synergistic effect spectrum range, and has a remarkable synergistic bacteriostatic effect when being combined with hydrogen peroxide, amoxicillin, ampicillin, benzylpenicillin potassium, erythromycin, azithromycin and amikacin; the antibacterial effect is weak when the compound is independently used, but the virulence of staphylococcus aureus can be remarkably reduced, the formation of hemolysin, staphylococcus flavin, enterotoxin and a biofilm can be inhibited, and meanwhile, the selective pressure on bacteria is favorably reduced due to the relatively low antibacterial activity, so that the occurrence of drug resistance is delayed; the method is suitable for various application scenes such as food processing industry.

This disclosure describes the use of azithromycin, roxithromycin, and telithromycin, including derivatives thereof, as senolytic drugs. BrdU was used to induce senescence in model human fibroblast cell lines. Also disclosed are methods for screening compounds for senolytic activity. The SRB assay was used to measure cell viability through protein content. Azithromycin roxithromycin, and telithromycin, clinically-approved pharmaceuticals, were found to be senolytic drugs. However, the closely-related parent compound, erythromycin, showed no senolytic activity. Azithromycin strongly induced both aerobic glycolysis and autophagy in human fibroblasts, but showed bi-phasic effects including on mitochondrial oxygen consumption rates with inhibitory activity at 50 μM and stimulatory activity at 100 μM. The xCELLigence real-time assay system showed that azithromycin preferentially targets senescent cells, removing approximately 97% (nearly a 25-fold reduction in senescent cells).

The present invention discloses a method for determining the content of polycarbophil in azithromycin eye drops, which adopts liquid chromatography to determine the content of polycarbophil in azithromycin eye drops in a size exclusion mode. The present invention provides a method for determining the content of polycarbophil in azithromycin eye drops, which specifically involves the selection of a chromatographic column, the optimization of a mobile phase and the verification of a chromatographic method, and can accurately determine the content of polycarbophil in azithromycin eye drops, with good separation effect, good repeatability, low interference and good quantitative linearity, thus filling the gap in the prior art.

The invention discloses a method for synthesizing an azithromycin intermediate by an aqueous phase method. The azithromycin intermediate 9-deoxy-9a-aza-9a-cis-erythromycin A is obtained by taking erythromycin oxime as an initial raw material and carrying out rearrangement and reduction reaction, and is characterized in that paratoluensulfonyl chloride is taken as a rearrangement reagent, the rearrangement reaction and the reduction reaction are carried out in a water phase by a one-pot method, and the azithromycin intermediate 9-deoxy-9a-aza-9a-cis-erythromycin A is obtained. Polymer PEG-CS is introduced as a solubilizer, an acid-binding agent, a defoaming agent and a hydrolysis promoting agent to participate in rearrangement and reduction reactions, other auxiliary agents and auxiliary materials do not need to be additionally added, the problem that excessive auxiliary agents and auxiliary materials need to be used in existing rearrangement and reduction reactions is solved from the source, and the recovery cost of the solvent and the use and post-treatment cost of the auxiliary materials are remarkably reduced.

The invention discloses a method for preparing azithromycin by using a microchannel reactor. The method uses erythromycin as a starting material and prepares azithromycin through oximation, rearrangement, reduction and methylation reactions. During the oximation reaction, the contact time of the feed liquid in the microchannel reactor is very short, which greatly reduces the safety risk of the oximation reaction. The reduction reaction is carried out in the microchannel reactor, and neither explosive sodium (potassium) borohydride nor a high-pressure reactor is used, which reduces the safety risk. A tray layer of palladium carbon is laid on the reaction bed to achieve the hydrogenation target, while greatly improving the utilization efficiency of palladium carbon. In the rearrangement reaction, a milder leaving group, sodium 2-naphthalenesulfonate, is used to replace the existing leaving group. Water is used as a solvent and the reaction is carried out at room temperature. The method is green, safe, and has a high yield, and is suitable for industrial production.

This invention belongs to the field of pharmaceutical crystallization technology, specifically relating to a crystallization process for small-particle-size azithromycin fumarate with low solvent residue. In existing processes, azithromycin fumarate crystallizes in alcohol solvents, often resulting in residual ethanol. This invention provides a crystallization process for azithromycin fumarate by adding a portion of fumaric acid to azithromycin, then adding azithromycin fumarate seed crystals, inducing crystallization through ultrasonication, continuing to add fumaric acid, and then concentrating under reduced pressure for isothermal crystal growth. The azithromycin fumarate crystals prepared by this method have a particle size distribution range of 15-30 μm, and the ethanol residue is reduced to below 0.5%, allowing for direct use in pharmaceutical preparations without further purification. This results in a high-quality, economically viable active pharmaceutical ingredient.

To provide an ophthalmic agent and an ophthalmic antibacterial agent that contain azithromycin and are administered in specific doses and dosage regimens for specific indications.SOLUTION: The present invention relates to an ophthalmic agent that contains azithromycin and ophthalmologically acceptable additives to prevent or treat one or more of a patient's blepharitis, hordeolum, and lacrimal pouchitis or to prevent the progression of the disease, the ophthalmic agent being applied to the patient twice daily for 2 days and then once daily for 12 days in an appropriate quantity once. The invention also relates to an ophthalmic antibacterial agent.SELECTED DRAWING: None

The invention discloses a novel Fe-C-N-coated Au material and a preparation method and application thereof.According to the Fe-C-N-coated Au material, iron monatomic nano-enzyme Fe-C-N serves as a core, gold nanoparticles are loaded on the surface, the Fe-C-N nanoparticles and a HAuCl4 aqueous solution are stirred at low temperature, then an ice-cold NaBH4 solution is slowly added into a mixed solution, and the Fe-C-N-coated Au material is obtained after reaction and treatment. The novel Fe-C-N-coated Au material disclosed by the invention can be used for rapidly and sensitively detecting the azithromycin or macrolide drug-resistant gene ermB.

The processing technology comprises the following steps: stirring and mixing beta-cyclodextrin and purified water in a stirring tank according to a ratio of 1: 1.25 to prepare a saturated aqueous solution, mixing azithromycin and absolute ethyl alcohol according to a ratio of 1: 1.5 to completely dissolve the azithromycin, and granulating the azithromycin and the absolute ethyl alcohol to prepare the azithromycin dry suspension. The preparation method comprises the following steps: adding dissolved azithromycin into a beta-cyclodextrin saturated water solution, uniformly mixing through a wet mixing granulator to prepare a suitable soft material, carrying out boiling drying, granulating, totally mixing, carrying out inner packaging and outer packaging by using a composite film, and finally warehousing. According to the characteristic that the effective components are bitter in taste, the beta-cyclodextrin has a unique annular structure, the interior of a molecular cavity of the beta-cyclodextrin is hydrophobic, the exterior of the beta-cyclodextrin is hydrophilic, various guest molecules can be included in the cavity through intermolecular acting force to form an inclusion compound, the bitter effective components are included in a framework of the beta-cyclodextrin, and the taste is improved.

Provided herein are pharmaceutically acceptable compositions containing macrolide antibiotics, in particular azithromycin. In particular, compositions containing azithromycin with low toxicity, especially for administration to felines, are provided herein.

The utility model relates to the technical field of pharmacy, in particular to an azithromycin solution sterilizer for injection, which can uniformly heat an azithromycin solution, and is good in sterilization effect, convenient to use and high in practicability. Comprising a bottom plate, a support and a box body, the box body is fixedly installed at the upper end of the bottom plate through the support, and a cavity is formed in the box body; the feeding pipe is rotationally installed on the upper portion of the box body, a valve is arranged on the feeding pipe, the driving mechanism is used for driving the feeding pipe to rotate, the input end of the heat exchange mechanism communicates with the lower end of the feeding pipe, and the heat exchange mechanism is located in a cavity of the box body; the two sets of fixing plates are installed at the left end and the right end of a cavity of the box body respectively, a plurality of sets of heating lamps are arranged on the two sets of fixing plates, the output end of the heat exchange mechanism communicates with the discharging mechanism, and the discharging mechanism is installed on the box body and the bottom plate and has a discharging function.

The present disclosure describes the use of azithromycin, roxithromycin and telithromycin (including their derivatives) as anti-aging drugs. BrdU was used to induce senescence in a model human fibroblast cell line. A method for screening compounds with anti-aging activity is also disclosed. The SRB assay is used to determine cell viability by protein content. The clinically approved drugs azithromycin, roxithromycin and telithromycin have been found to be anti-aging drugs. However, the closely related parent compound erythromycin does not show anti-aging activity. Azithromycin strongly induces both aerobic glycolysis and autophagy in human fibroblasts, but shows a bidirectional effect, including 50 μM inhibitory activity and 100 μM stimulatory activity on mitochondrial oxygen consumption rate. The xCELLigence real-time assay system showed that azithromycin preferentially targeted senescent cells, removing approximately 97% of senescent cells (a nearly 25-fold reduction in senescent cells).

The present invention discloses a novel hydrogel-based BMSCs-loaded azithromycin formulation, its preparation method, and application. The novel hydrogel-based BMSCs-loaded azithromycin formulation comprises albumin-azithromycin-nanoparticles sequentially encapsulated by rat bone marrow mesenchymal stem cells and chitosan hydrogel; the mass ratio of the albumin-azithromycin-nanoparticles, rat bone marrow mesenchymal stem cells, and chitosan hydrogel is 1:1-2:1-2; the albumin-azithromycin-nanoparticles are nanoparticles formed by encapsulating azithromycin in albumin, and the mass ratio of the azithromycin to the albumin is 1:4-5. The present invention successfully prepared a novel formulation, BMSCs-TAT-AZM-NPs@Gel; this system not only exhibits anti-inflammatory, antioxidant, and promotes damaged tissue repair; at the same time, the novel formulation also reduces the toxic and side effects of AZM, improves the safety of the drug, and provides a new approach for the treatment of spinal cord injury.

A medicated eyelid cleansing composition comprising a medicated scrub composition and an eyelid cleansing composition. The medicated scrub composition has one or more antibacterial and anti-inflammatory agents, including azithromycin and diclofenac sodium or dexamethasone phosphate. The medicated scrub composition can further include a combination of metronidazole and ivermectin. The composition is optimized for physiological compatibility and can be combined with a suitable substrate for use as a medicated eyelid cleanser.

The present invention belongs to the technical field of semen preservation solution, in particular to a goat semen preservation solution and a preservation method thereof. The preservation solution comprises the following components per 100 mL: component A: 1.2-1.3 g of fructose, 1.7-1.8 g of citric acid monohydrate, 3.5-3.6 g of tris(hydroxymethyl)aminomethane; component B: 19-21 mL of fresh egg yolk, 3.5-4.5 mL of vitamin E, 0.4-0.6 g of bovine serum albumin, 0.4-0.6 g of vitamin C, 3.5-4.5 mL of glycerol, 100 00-15000IU of penicillin sodium, 10000-15000IU of streptomycin sulfate, 0.5-0.7mg of Y-27632·2HCl, 5-6mg of ectoine, 0.2-0.3mg of bifendate, 0.3-0.4mg of tiopronin, 0.5-0.6mg of amifostine, 2-2.5mg of azithromycin, 0.1-5mg of dexamethasone; the rest is double distilled water. The present invention can effectively solve the problem of yolk aggregation of goat semen in yolk-containing preservation solution, prolong the storage time of goat semen under low temperature conditions, and achieve the best quality of sperm.

This application relates to the field of biotechnology, and particularly to primer pairs, primer-probe compositions, PCR premixes, kits, and methods for detecting multiple respiratory pathogens. Nucleic acid sequences are shown in primer pairs as indicated by SEQ ID NO: 1-2, 4-5, 7-8, 10-11, 13-14, 16-17, 19-20, 22-23, 25-26, 28-29, 31-32, 34-35, 37-38, and 40-41. For target respiratory pathogens, this application designs specific amplification primer pairs, paired with suitable probes, enabling the simultaneous detection of eight targets. Furthermore, the detection process avoids interference from heme, trimethoprim, sulfamethoxazole, amphotericin B, itraconazole, fluconazole, azithromycin, adrenaline, and lidocaine hydrochloride in the test sample. It exhibits good anti-interference properties and shows no cross-reactivity with *Rhodococcus equi*, *Candida tropicalis*, and *Candida krusei*.

The application belongs to the technical field of antibacterial infection materials, and particularly relates to preparation and application of a biomimetic mineralization nanoparticle. x S y / AZM, which is obtained by fixing glucose oxidase (GOx) in FexSy nanoparticles hybridized with azithromycin (AZM) through a biomimetic mineralization strategy, and the nanoparticle GOx@Fe x S y / AZM serves as a therapeutic drug to catalyze a large amount of active oxygen free radicals (ROS) to improve inflammatory response in order to rapidly kill infectious microorganisms in the early stage of bacterial infection of a wound surface; and in the subsequent healing period, H2S released by the material and AZM will jointly promote the polarization of macrophages to M2 macrophages of a repair type to effectively mediate the tissue repair after a high inflammatory response, so that the ordered treatment of a high blood sugar infection wound surface is achieved.

The application discloses a molecular imprinting polymer electrocatalytic polar plate and a preparation method and application thereof, and the preparation method comprises the following steps: cleaning an electrode plate; stirring a benzene[1,2-B:4,5-B']dithiophene-4,8-dione, 3-boronic acid thiophene, azithromycin, 3,3'-bithiophene and tetrabutylammonium perchlorate acetonitrile solution to obtain a polymerization solution; taking a graphite plate as a working electrode and a counter electrode, and taking a non-aqueous Ag + The electrode is a reference electrode, the electro-polymerization is completed in the polymerization solution, and a MIP (PBth-BQ) molecular imprinting catalytic electrode is obtained; the MIP (PBth-BQ) molecular imprinting catalytic electrode is taken as a working electrode, the graphite sheet is taken as a counter electrode, saturated mercury is taken as a reference electrode, constant-temperature water bath stirring is carried out, the template is removed, and cleaning is carried out. The electrocatalytic polar plate has holes on the surface, the azithromycin is wrapped first and then removed, the adsorption effect is better, the selectivity is high, the adsorption and electrocatalysis are synergistically combined, and the removal effect is good.

The present invention relates to crystalline forms of azithromycin derivatives, and the pharmaceutical formulations and therapeutic uses thereof, specifically salts, for example, crystalline forms, of the macrolide, (2S,3R,4S,6R)-4-(dimethylamino)-2-[[(2R,3S,4R,5R,8R,10R,11R,125,135,14R)-2-ethyl-3,4,10,13-tetrahydroxy-3,5,6,8,10,12,14-heptamethyl-15-oxo-1-oxa-6-azacyclopentadec-11-yl]oxy]-6-methyl-tetrahydropyran-3-yl]benzoate), in particular, the tartrate, oxalate and naphthalene di-sulphonate salts.

The invention provides azithromycin water-free swallowing granules and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The azithromycin water-free swallowing granules are prepared by mixing medicine-containing taste-masking pellets and taste-modifying granules. The medicine-containing taste-masking pellet sequentially comprises a medicine-containing pellet core, an isolating layer and a taste-masking layer from inside to outside, and the medicine-containing pellet core is prepared through a centrifugal pelleting process. The technical problem to be solved is that the azithromycin water-free swallowing granule can realize water-free rapid swallowing, keeps good taste in the whole process, remarkably improves medication convenience and patient compliance, and is particularly suitable for children and other groups with difficulty in swallowing.

The invention relates to an azithromycin hapten, an azithromycin artificial antigen and application thereof. The azithromycin A is used as an initial raw material, an active arm is introduced from a secondary amine terminal, all hydroxyl and tertiary amine structures of an azithromycin drug are completely reserved, the prepared hapten has a relatively good space structure, the electron cloud density of the hapten is basically consistent with that of an original drug, and the immunogenicity of the antigen is improved; the prepared azithromycin artificial antigen and the monoclonal antibody are high in specificity when being used for ELISA (enzyme-linked immunosorbent assay) detection, and the IC50 value is 0.03 g / L; a further established colloidal gold immunochromatography test strip can rapidly and conveniently realize qualitative detection of azithromycin, the sensitivity of the azithromycin in a standard solution is 0.5 g / kg, and the detection sensitivity of the azithromycin in a sample can reach 0.5 g / kg.

The invention relates to the technical field of traditional Chinese medicines, and particularly discloses a navel therapy composition and a navel therapy preparation for preventing and treating abdominal pain caused by intravenous drip of azithromycin in children and a preparation method of the navel therapy composition and the navel therapy preparation. The technical key points are as follows: the fructus evodiae and the dysentery are combined according to a specific weight ratio, and are matched with pharmaceutic adjuvants such as a transdermal enhancer and an excipient to prepare special navel therapy dosage forms such as pills, cakes, patches and the like. According to the composition, by utilizing the characteristics that the Shenque acupoint (navel) epidermal cuticle is thin, the barrier function is weak, blood vessels are rich, and medicines are easy to disperse and absorb, adverse reactions such as gastrointestinal spasmodic pain, nausea and vomiting and the like caused by intravenous drip of azithromycin in children are effectively relieved through an administration mode of external application. Through clinical verification, the umbilical therapy preparation can remarkably reduce the incidence rate and severity score of stomachache, vomiting and diarrhea, and remarkably improve the treatment compliance of child patients.

The application discloses a synergistic bactericidal composition, comprising the following components: a toona sinensis extract: 16-2048 mu g / mL; a macrolide antibiotic: 0.0625-4096 mu g / mL; the bacteria are staphylococcus aureus or methicillin-resistant staphylococcus aureus, and the macrolide antibiotic is erythromycin or azithromycin. The application further discloses a use of the synergistic bactericidal composition in preparation of a medicine for treating skin and soft tissue infections. The composition provided by the application can convert the traditional macrolide antibiotics such as erythromycin and azithromycin which only have a bacteriostatic effect into a preparation which has clear bactericidal activity on staphylococcus aureus and drug-resistant strains thereof. After the toona sinensis extract is combined with the antibiotic, a synergistic effect is exhibited, and the concentration of the toona sinensis extract and the antibiotic required when the toona sinensis extract and the antibiotic are used alone can be greatly reduced.

The present invention relates to a macrolide compound, and a preparation method therefor and the use thereof. Specifically disclosed is a compound as shown in formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits a significant antibacterial activity, comprising the antibacterial activity against bacteria resistant to macrolide drugs such as azithromycin. The compound described herein has a low hepatotoxicity and superior safety compared to other macrolide compounds. The compound can be used for infectious diseases, etc.

The present invention relates to an aminopyridone macrolide compound and the use thereof. Specifically disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antibacterial, antimycoplasmal or antichlamydial activity, and can be used for preventing and / or treating related diseases caused by bacteria, mycoplasmas or chlamydias. Further, the compound of the present application can achieve an antibacterial activity comparable to or better than that of azithromycin or solithromycin at a lower dosage. Still further, the compound of the present application exhibits a superior antibacterial effect on Gram-positive bacteria. Even further, the compound of the present application exhibits a better inhibitory activity against mycoplasmas and a lower hepatotoxicity.

The invention provides application of synergy of ethyl ferulate and antibiotics in preparation of a synergistic antibacterial drug for escherichia coli O157: H7, and belongs to the technical field of antibacterial drugs. The invention firstly provides an application of ethyl ferulate in preparation of a medicine for resisting a biofilm inhibitor, and provides an application of ethyl ferulate and antibiotics in preparation of a synergistic antibacterial medicine for escherichia coli O157: H7 based on the application of ethyl ferulate and antibiotics in preparation of a synergistic antibacterial medicine for escherichia coli O157: H7. The invention proves that the ethyl ferulate has a remarkable inhibition effect on the formation of an escherichia coli O157: H7 biofilm for the first time. The invention also proves that when the ethyl ferulate is combined with the existing antibiotics (fosfomycin sodium, cefquinome, gentamicin, tetracycline and azithromycin), a synergistic effect can be generated. Therefore, the ethyl ferulate is thought to have dual effects of resisting the biofilm and synergistically resisting bacteria on the escherichia coli.

An aseptically prepared pharmaceutically acceptable azithromycin premix formulation has a pH value of 5.5 to 7.5, preferably 6.0 to 7.0, more preferably 6.3 to 7.0, even more preferably 6.3 to 6.7, for example about 6.5. Preferred embodiments of the aseptically prepared pharmaceutically acceptable azithromycin premix formulation contain azithromycin, a buffering agent, water and optionally a tonicity adjusting agent and are stable for one month, three months, six months, nine months, twelve months, fifteen months, eighteen months or even twenty-four months, during storage at refrigerated temperatures, such as about 5 °C, even without any additional components beyond the azithromycin, the buffering agent, and the optional tonicity adjusting agent in the premix formulation. The pharmaceutically acceptable azithromycin premix formulation may be aseptically filled into a container, preferably a glass or flexible container, to form a sterile pharmaceutical azithromycin premix product which does not undergo terminal sterilization. The azithromycin premix product can be a single use premix which is a sterile, stable and ready-to-use aqueous solution for parenteral administration, for example intravenous (IV) administration such as IV infusion, and requires no dilution prior to parenteral administration.

The invention discloses an azithromycin fumarate sustained-release tablet and a preparation method thereof, and particularly relates to the technical field of pharmaceutical preparations, and the sustained-release tablet comprises the following components based on 100% of the total mass of the sustained-release tablet: 30-50% of azithromycin fumarate, 5-20% of a wax retardant material, 20-40% of a high polymer material sustained-release matrix, 10-20% of a filler, 5-10% of a sweetener, 0.5-5% of a lubricating flow aid, and the balance of an adhesive. According to the invention, the dissolution and release degree of the medicine can be reduced, the peak concentration of the medicine is reduced, the peak valley fluctuation of the blood concentration is reduced, the adverse reaction of the medicine is slowed down, the effective blood concentration duration is prolonged, the clinical treatment effect of the medicine is improved, and the compliance, convenience and compliance of patient medication are also improved; the generation of drug resistance is reduced to the greatest extent.