17 results about "Clarithromycin" patented technology

The invention discloses a medicine for inhibiting helicobacter pylori infection, the medicine is oridonin, and the structural formula of the medicine is as shown in formula 1. In-vitro experiments show that the oridonin has a remarkable antibacterial effect on helicobacter pylori strains SS1, ATCC700392 and ICDC11101, and can remarkably reduce the urease activity of the helicobacter pylori, inhibit the formation of a biological membrane, destroy the growth of thalli and reduce the adhesion effect of the helicobacter pylori on gastric epithelial cells, and in addition, the oridonin and antibiotics are combined for use, so that the effect of preventing and treating the gastric epithelial cells can be achieved. The compound has a synergistic antibacterial effect with metronidazole and clarithromycin, has the effect of reducing the dosage of antibiotics in clinical application, and has potential application value for improving the current drug resistance situation of the antibiotics.

The invention discloses a formula and application of a compound infertility agent containing clarithromycin and quinestrol and based on CYP enzyme activity inhibition. The clarithromycin composition comprises clarithromycin, quinestrol and baits. The CYP enzyme inhibitor and the endocrine sterilant are combined for use, so that the synergist can effectively inhibit the activity of CYP enzyme in tissues such as livers of rats, the metabolic clearance rate of the sterilant is remarkably reduced, and the oral bioavailability and the system exposure level of the sterilant are improved. Therefore, when the same infertility effect is achieved, the use dosage of the infertility agent can be greatly reduced, so that the cost is saved, and the environmental load is reduced; or under the same dosage, a more thorough and more lasting population sterility effect can be obtained, and the practicability and competitiveness of a pest mouse sterility control technology are greatly improved.

The application provides a macrolide derivative and a preparation method and application thereof, relates to the technical field of medicinal chemistry, and the macrolide derivative is a compound with a general structure shown in the following formula I: in the formula, A is selected from any one of alkynyl, alkenyl or piperazine; R is selected from any one of H or F; X is selected from any one of CH or N, Y is selected from any one of methyl, ethyl or cyclopropyl, and n is an integer in the range of 2-6. The macrolide derivative is connected by different lengths of ether hydrocarbons at the 3-position, thereby avoiding the problem that the instability of a synthesized compound is caused by using an ester group as a side chain to connect a quinolone group. The application successfully prepares a macrolide derivative with double targets, and the antibacterial activity of the macrolide derivative is obviously better than the antibacterial activity of erythromycin, telithromycin, clarithromycin and ciprofloxacin which only have single targets.

We report improved adjuvant compounds that have an aryl 2-aminoimidazole structure for macrolide potentiation against a virulent strain of gram-negative bacteria, AB5075. Compounds were discovered to retain significant adjuvant activity at 10 μM, lowering the minimum inhibitory concentration (MIC) of clarithromycin (CLR) from 8-fold to 128-fold or greater. 2-Aminoimidazole compounds linked to aryl groups via either an amide or urea linker showed significantly improved activity over control compounds.

The invention discloses a composition with a synergistic anti-helicobacter pylori effect with antibiotics and a preparation method of the composition, and belongs to the technical field of traditional Chinese medicines. The composition is prepared from clove, kaki calyx, ginseng and ginger according to a specific proportion through water or ethanol extraction. Experiments show that the composition has remarkable bacteriostasis and sterilization effects on helicobacter pylori standard strains and clinical drug-resistant strains, and can generate a synergistic effect (FICI < = 0.5) with antibiotics such as clarithromycin and the like. The invention provides a traditional Chinese medicine anti-HP scheme which is safe, effective and not prone to drug resistance, and has a good development prospect.

A new class of dimeric 2-aminoimidazole (2-AI) compounds that potentiate macrolide antibiotics against A. baumannii. A parent dimer lowers the MIC of clarithromycin (CLR) from 32 μg / mL to 1 μg / mL at a concentration of 7.5 μM (3.4 μg / mL), while a structure activity relationship (SAR) study on the dimeric 2-AI scaffold resulted in the identification of several compounds with increased activity. Substitution of fluorine on a central phenyl ring resulted in the most potent activity, with the lead compound, containing a fluorine ortho to each of the 2-AIs, that lowered the CLR MIC to 2 μg / mL against AB5075 at 1.5 μM (0.72 μg / mL), exceeding the activity of both the parent dimer and the lead aryl-2-AI. Furthermore, these dimeric 2-AI analogs exhibit favorably low mammalian cell toxicity.

This invention discloses a gelling material for treating gastric diseases and its preparation method, belonging to the field of pharmaceutical preparation technology. The gelling material is composed of 8-10g of Codonopsis pilosula extract, 6-10g of Bletilla striata extract, 6-8g of Dioscorea opposita extract, 2-4g of Citrus reticulata peel extract, 2-3g of gelatin, 2-4g of xylitol, 0.1-0.2g of citric acid, and 60.8-73.9g of purified water. As a carrier matrix, the gelling material of this invention exhibits good compatibility with commonly used antacids (such as calcium carbonate), PPIs (such as omeprazole), antibiotics (such as amoxicillin and clarithromycin), and traditional Chinese medicine extracts. During preparation, the above-mentioned active pharmaceutical ingredients (APIs) can be uniformly dispersed in the gel matrix, achieving integrated synergistic treatment of "mucosal protection + acid suppression / bactericidal action" without compromising their chemical stability or causing burst release problems, providing an ideal platform for developing compound gastric disease preparations.

The invention provides a method for preparing clarithromycin through a single solvent system, and belongs to the technical field of erythromycin derivatives. The preparation method comprises the following steps: by taking erythromycin oxime as a raw material, carrying out etherification reaction and silanization reaction, adding 1, 3-dimethyl-2-imidazolone into the obtained product, carrying out ice-water bath, reducing the temperature to 0-5 DEG C, adding potassium hydroxide and methyl p-toluenesulfonate, carrying out first-stage heat-preservation reaction, heating to 14-20 DEG C, carrying out second-stage heat-preservation reaction, and after the reaction is ended, cooling to room temperature to obtain the erythromycin oxime. Adding methyl tert-butyl ether to extract the reaction product, standing for liquid separation, and recovering the obtained methyl tert-butyl ether layer under reduced pressure to obtain a methylated product; and reacting the methylated product to obtain a clarithromycin crude product, and recrystallizing to obtain a finished product clarithromycin. According to the method, the amount of alkali required by the reaction and the reaction temperature are remarkably reduced, generation of alkali damage impurities and dimethyl impurities in the reaction process is effectively controlled, the liquid phase content of the methylation intermediate is increased, and then the yield of clarithromycin is increased.

This invention relates to combinations for treating nontuberculous mycobacterial diseases. Specifically, it relates to combinations of bedaquiline, macrolides (e.g., clarithromycin), and optionally ethambutol for use in the treatment of diseases associated with nontuberculous mycobacteria (NTM).

The invention discloses a method for detecting the concentration of eight second-line antituberculous drugs based on HPLC-MS / MS. The eight second-line antituberculous drugs are divided into two groups for detection, one group takes levofloxacin as an internal standard substance, and an internal standard stock solution is prepared; the method comprises the following steps: detecting by taking standard substances of levofloxacin, ciprofloxacin and gatifloxacin as target substances; and in the other group, albendamide, deramanib, pritomanib, clarithromycin and azithromycin are used as target objects for detection. According to the method, the detection time is short, only 5 min is needed, and the detection time is saved; meanwhile, according to the method disclosed by the invention, the consumption of an organic solvent is reduced, so that the pollution to the environment is reduced, and the method has the characteristics of high accuracy and good precision, and provides the fastest and effective basis for clinical treatment.

The present invention relates to a composition for eradicating Helicobacter pylori and its use. The composition of the present invention maintains an intragastric pH at a certain level or higher for a certain period of time or longer, thereby maximizing the action of amoxicillin and clarithromycin to show an excellent effect on the eradication of Helicobacter pylori.

The utility model discloses a medical sewage treatment system based on antibiotic regulation and control and multistage photocatalysis, which relates to the technical field of medical sewage treatment and is characterized in that organic matters are efficiently degraded and a nitrification process is started through the synergistic effect of clarithromycin and nitrosomonas; the device greatly improves the ammonia nitrogen removal efficiency of sewage, adopts a Z-type heterojunction photocatalyst in the mineralization pool to efficiently degrade micro pollutants such as antibiotics, has a better drug residue removal effect compared with the traditional technology, is matched with a PID controller to realize full-process automatic control, optimizes operating parameters, is strong in comprehensiveness, and is suitable for large-scale popularization and application. The treatment effect is more efficient and thorough.

The present application belongs to the technical field of natural product development and bioactivity application, and particularly relates to a preparation method of Phyllanthus niruri extract and application thereof in anti-Helicobacter pylori drugs. The Phyllanthus niruri medicinal material is crushed, soaked in purified water, extracted by water bath reflux, concentrated by rotary evaporation, and freeze-dried to obtain the Phyllanthus niruri water extract. The Phyllanthus niruri water extract has obvious anti-Helicobacter pylori activity. The MIC of the Phyllanthus niruri water extract dissolved in brain heart infusion for different strains is as low as 160-320 μg / mL, and the MBC is as low as 320-640 μg / mL. The Phyllanthus niruri water extract is mixed with different antibiotics in different proportions to test the minimum combined inhibitory concentration. It is found that the combined inhibitory index value of the Phyllanthus niruri water extract and clarithromycin for strain ATCC700392 is 0.75, which is an additive effect. Therefore, the Phyllanthus niruri water extract and clarithromycin can be combined to be used in anti-Helicobacter pylori drugs.

The application provides a clarithromycin taste-masking solid dispersion and a preparation method thereof, and belongs to the technical field of medicine preparation. TM One or more of HPC; the mass ratio of the clarithromycin and the auxiliary material is 1-2:1-8. The application adopts hot melt extrusion (HME) to prepare a CLA amorphous solid dispersion (SD). By comparing the differences in the Hansen solubility parameters, the polymers used for HME are preliminarily selected to predict the miscibility of the drug and the polymers. E100 is selected as the polymer because it combines the taste-masking effect and the solubility.

The invention discloses a synthetic method of a clarithromycin preparation promoted by ionic liquid and the clarithromycin preparation. The synthetic method comprises an etherification reaction, a silanization reaction and a methylation reaction. The etherification reaction comprises the following steps: adding erythromycin A-9-oxime into a reaction container, and adding ionic liquid [Bmim] BF4 as a reaction solvent. The silanization reaction comprises the following steps: adding 1, 1, 1, 3, 3, 3-hexamethyl disilazane and imidazole into a reaction container containing an etherification reaction result feed liquid of the [Bmim] BF4 reaction solvent. The methylation reaction comprises the step of adding methyl bromide and potassium hydroxide into a reaction container containing silanization reaction result feed liquid of the [Bmim] BF4 reaction solvent. The three-step reaction of etherification, silanization and methylation is carried out in the same reactor, and products in all steps do not need to be separated, so that a continuous process is realized. The ionic liquid as a reaction solvent is non-volatile and non-flammable, and is an important path for realizing green synthesis and clean production.

The invention relates to a clarithromycin derivative containing a quinolone structure as well as a preparation method and application of the clarithromycin derivative. The compound provided by the invention has antibacterial activity equivalent to that of telithromycin in constitutive streptococcus pneumoniae drug-resistant bacteria and streptococcus pyogenes drug-resistant bacteria. And the antibacterial activity on haemophilus influenzae is better than that of Thailimycin. Furthermore, the anti-streptococcus pyogenes 12-206 activity of part of the compounds disclosed by the invention is obviously superior to that of the existing compounds. In addition, the compound provided by the invention not only can act on ribosome, but also can act on topoisomerase, and is a double-target compound at the cellular level. Therefore, the compound disclosed by the invention is not easy to induce bacteria to generate mutation, and the service life of the compound as an antibacterial agent can be prolonged.