39 results about "Clarithromycin" patented technology

The invention relates to the technical field of pathogenic bacterium detection, in particular to a method and a kit for detecting helicobacter pylori gene mutation in excrement. According to the technical scheme, the kit for detecting helicobacter pylori gene mutation in excrement is developed by combining multiple advanced technical means such as ARMS-PCR design, blocking primers, locked nucleic acid modification (peptide nucleic acid modification), MGB probes, nested PCR design and degenerate base design. The kit can detect nine gene mutation sites related to the drug resistance of helicobacter pylori at one time, and has a wide coverage range. The kit in the scheme can be used for detecting the drug resistance of quinolone antibiotics and / or clarithromycin antibiotics of helicobacter pylori, and the technical problem that a high-specificity and high-sensitivity excrement helicobacter pylori gene mutation detection method is lacked in the prior art is solved. The method is simple and convenient to operate and can be completed within 1-2 hours, the detection cost is reduced, and the method has ideal application and popularization prospects.

The invention provides a preparation method of a nitrosamine impurity, and belongs to the technical field of heterocyclic compounds. The clarithromycin related nitrosamine impurity is 3 '-N-demethyl-3'-N-nitroso-6-O-methyl erythromycin, and is prepared by carrying out demethylation and nitrosation on clarithromycin. The clarithromycin intermediate erythromycin oxime related nitrosamine impurity is 3 '-N-demethyl-3'-N-nitroso erythromycin A (E)-9-oxime, and the clarithromycin intermediate erythromycin oxime related nitrosamine impurity is prepared from erythromycin A (E)-9-oxime through demethylation, etherification, nitrosation and hydrolysis.

The invention belongs to the field of medical technology, and specifically relates to a pharmaceutical composition comprising clarithromycin and sudapyridine. The technical problem solved is that the drug selection for inhibiting mycobacterium abscessus is limited, the treatment cycle is long, the disease is prone to recurrence, and the drug resistance to commonly used antibiotics in clinical practice is high. The pharmaceutical composition inhibits mycobacterium abscessus by combining clarithromycin and sudapyridine, wherein sudapyridine has good activity in inhibiting mycobacterium abscessus, clarithromycin has good safety and good anti-mycobacterium abscessus activity, the pharmaceutical composition can increase the blood concentration of sudapyridine in tissue within 16 hours by combining clarithromycin and sudapyridine, and a drug combination scheme having better mycobacterium abscessus inhibition activity and improving the cure rate of mycobacterium abscesses is formed by combining clarithromycin and sudapyridine. The specific technical scheme is that the ratio of clarithromycin and sudapyridine is preferably 15-20:9-15.

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.

The invention relates to a compound medicine composition and application thereof in resisting helicobacter pylori infection, in particular to the compound medicine composition, a medicine preparation, a preparation method and application, and the composition comprises at least two selected from the following components: (I) Vonoprazan or pharmaceutically acceptable salt thereof, (II) Vonoprazan or pharmaceutically acceptable salt thereof, (III) Vonoprazan or pharmaceutically acceptable salt thereof, (III) Vonoprazan or pharmaceutically acceptable salt thereof, (III) Vonoprazan or pharmaceutically acceptable salt thereof and (III) Vonoprazan or pharmaceutically acceptable salt thereof; (II) amoxicillin or a pharmaceutically acceptable salt thereof; (III) clarithromycin; according to the composition prepared by compounding different anti-infection active ingredients, the problems of patient compliance and medication convenience can be effectively solved, for example, the tablet dosage is reduced, wrong taking, missing taking, excessive taking and the like of a patient are avoided, the stability and safety of the preparation can be accidentally improved, and the content of harmful impurities is particularly reduced.

The invention relates to a novel method for synthesizing clarithromycin, which specifically comprises the following steps: simultaneously protecting 9-position carbonyl, 11-position hydroxyl and 12-position hydroxyl of erythromycin by using o-aminophenylboronic acid and derivatives thereof, protecting 2 '-position hydroxyl and 4'-position hydroxyl of erythromycin by using trimethylsilyl, methylating, and hydrolyzing to obtain clarithromycin. The method has the effects of short process route, cheap and easily available raw materials, high yield and low cost.

The invention provides a preparation method of a clarithromycin crude product, and relates to the technical field of medicine preparation. According to the method, oxime etherified silanide is taken as a starting material, various methylation reagents are adopted, toluene is taken as a solvent system, tributyl methyl ammonium chloride is taken as a solid-liquid phase transfer catalyst, potassium hydroxide is taken as an acid-binding agent, a methylation reaction is carried out, deprotection is carried out through tetrabutylammonium fluoride, and oxime hydroxyl is reduced through potassium borohydride, so that a clarithromycin crude product is obtained.

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 relates to the field of pharmaceutical analysis, in particular to a determination method of clarithromycin methylate related substances. The determination method comprises the following steps: detecting the related substances of clarithromycin methide by adopting a high performance liquid chromatography, wherein chromatographic conditions are as follows: a mobile phase is a phosphate solution and acetonitrile in a volume ratio of (20: 80)-(40: 60), and a stationary phase is octadecylsilane chemically bonded silica. The method disclosed by the invention is simple, convenient, rapid and accurate to operate, and can be well used for detecting the related substances of the clarithromycin methylate.

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.

The present invention relates to a compound pharmaceutical composition and its application in preventing Helicobacter pylori infection, and more specifically, to the compound pharmaceutical composition, pharmaceutical preparation, preparation method and use. The composition comprises at least two selected from the following components: (I) vonoprazan or a pharmaceutically acceptable salt thereof; (II) amoxicillin or a pharmaceutically acceptable salt thereof; (III) clarithromycin; and (IV) a bismuth agent. The composition prepared by compounding different anti-infective active ingredients can not only effectively solve the problems of patient compliance and medication convenience, such as reducing the dosage of tablets and avoiding patients from taking the wrong tablets, missing a dose, or taking more than one dose, but also unexpectedly improve the stability and safety of the preparation, and is particularly conducive to reducing the content of harmful impurities.

The invention discloses a radix scutellariae extract for resisting Helicobacter pylori, a preparation method thereof and a composite drug. The invention first obtains a radix scutellariae water extract by a water extraction method, and then extracts the radix scutellariae extract by using ethyl acetate as a solvent. In vitro experiments show that the method enriches the main active substances of radix scutellariae for resisting Helicobacter pylori, has a significant antibacterial effect on the standard strain SS1 of Helicobacter pylori, and has a minimum inhibitory concentration (MIC) of 32 μg / ml, which significantly inhibits the biofilm formation of the standard strain SS1 of Helicobacter pylori. In addition, it is also found that the radix scutellariae extract of the invention is used in combination with antibiotics commonly used in clinical treatment of HP infection, and has a synergistic effect with metronidazole and levofloxacin, and an additive effect with clarithromycin and amoxicillin, which has the effect of reducing the amount of antibiotics used in clinical application, and has potential application value for improving the current status of antibiotic resistance. Compared with the water extract, the MIC of the radix scutellariae extract extracted by the invention against Helicobacter pylori is greatly reduced, and the in vitro antibacterial activity is significantly enhanced.

The invention provides a clarithromycin derivative, a pharmaceutical composition and application of the clarithromycin derivative, and relates to the technical field of pharmaceutical chemistry, the clarithromycin derivative has a general formula structure as shown in the following formula I. In the formula I, W is selected from any one group of oxygen atom and NOCH2C = C-Ar, and the structural formula is shown in the description. Ar is selected from any one of pyridyl, quinolyl, isoquinolyl, substituted pyridyl, substituted quinolyl and substituted isoquinolyl; v is selected from any one of oxygen atoms and 11-site side chains of telithromycin; x is selected from any one of-C is equivalent to C-,-OCH2CH2C is equivalent to C-and piperazinyl; q is selected from any one of methylene and fluorine-substituted carbon atoms; z is selected from any one of methylene, fluorine-substituted carbon atoms, nitrogen atoms and methoxyl carbon atoms; r1 and R2 are respectively and independently selected from any one of hydrogen atoms, C1-C3 alkyl groups, halogen-substituted C1-3 alkyl groups, C3-4 cycloalkyl groups, halogen-substituted C3-4 cycloalkyl groups and halogen-substituted phenyl groups; and the value range of n is an integer between 3 and 6. # imgabs0 #

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.

Pharmaceutical microemulsion composition of clarithromycin with improved stability, bioavailability and antimicrobial activity against Helicobacter pylori, comprising: (a) 1 gram of clarithromycin as active pharmaceutical ingredient; (b) 8 grams of an oil phase consisting of a 1:1 mixture of glyceryl tricaprylate and peppermint oil; (c) 40 grams of a surfactant mixture (Smix), the surfactant being Tween 80 and the co-surfactant being Transcutol P, present in a ratio optimized to maintain an isotropic and thermodynamically stable microemulsion; (d) 52 grams of an aqueous phase comprising purified water; wherein the microemulsion composition is characterized by a mean droplet size of less than 30 nanometers, a viscosity in the range of 3.91 to 18.97 centipoise (cps), and a pH in the range of 4.56 to 7.06; and wherein the composition provides improved solubility, bioavailability, and physicochemical stability of clarithromycin under gastric pH conditions, thereby improving therapeutic efficacy against Helicobacter pylori.

The invention discloses an anti-helicobacter pylori combined medicine, and aims to provide the anti-helicobacter pylori combined medicine which has a remarkable inhibition effect on a helicobacter pylori standard strain SS1, can effectively destroy the biological membrane structure of the helicobacter pylori standard strain SS1 and has a synergistic antibacterial effect. According to the technical scheme, the traditional Chinese medicine composition consists of fructus amomi essential oil extract and clinically common antibiotics for treating helicobacter pylori infection, experiments show that the technology provided by the invention has a synergistic effect with metronidazole, levofloxacin, clarithromycin and amoxicillin; the effect of reducing the dosage of antibiotics in clinical application is achieved, and the potential application value is achieved for improving the current drug resistance situation of the antibiotics; belongs to the technical field of medicine.

The invention provides a composition capable of detecting helicobacter pylori clarithromycin drug resistance gene mutation, a kit and application, and belongs to the technical field of gene detection. The invention designs an As-RPA primer pair and crRNA capable of realizing multiple simultaneous detection of three single-base mutation A2142C, A2142G and A2143G and one double-base mutation A2142G / A2143G, and an As-RPA-CRISPER / Cas12a system established on the basis of the sequence, the system can detect four mutation types of helicobacter pylori within 1 hour under the condition of constant temperature, and the primer pair and crRNA have the advantages of high specificity, high sensitivity, high sensitivity, high sensitivity and the like. The kit has remarkable advantages in the aspects of sensitivity, specificity, detection speed, multiple detection capability, visual result interpretation, applicability and the like, provides an efficient and convenient solution for detecting the drug resistance of helicobacter pylori clarithromycin, and has important clinical application value and popularization prospect.

The application discloses a combined medicine against helicobacter pylori, and aims to provide a combined medicine against helicobacter pylori, which has a significant inhibiting effect on a standard strain SS1 of helicobacter pylori, can effectively destroy a biofilm structure of the standard strain SS1 of helicobacter pylori, and has a synergistic bacteriostatic effect. The technical scheme is that an extract of fructus amomi essential oil is combined with antibiotics commonly used in clinical treatment of helicobacter pylori infection. Experiments show that the technology provided by the application has a synergistic effect with metronidazole, levofloxacin, clarithromycin and amoxicillin. The technology has an effect of reducing the dosage of the antibiotics used in clinical application, has potential application value for improving the drug resistance status of the antibiotics, and belongs to the technical field of medicines.

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 present invention relates to a method for rapidly detecting lincomycin, clindamycin, erythromycin, clarithromycin and roxithromycin in water, belonging to the technical field of analytical detection. By means of specific fully automated on-line solid-phase extraction conditions in combination with specific high performance liquid chromatography-tandem mass spectrometry conditions, the present invention realizes sample enrichment, purification, separation and determination, and fully automatically analyzes lincomycin, clindamycin, erythromycin, clarithromycin and roxithromycin in water. The present invention realizes fully automated operation, and the total determination time only needs 11 min. The detection limit reaches the ng / L level. By washing the solid-phase extraction column with an ammonium bicarbonate aqueous solution, the problem of matrix effect commonly encountered in the analysis of complex matrix samples is overcome, meeting the requirements for ultra-trace detection of lincomycin, clindamycin, erythromycin, clarithromycin and roxithromycin in water.

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 present invention relates to a composition for eradicating Helicobacter pylori and a use thereof. The composition of the present invention maintains an intragastric pH at a certain level or more for a certain period of time or longer, thereby maximizing an action of amoxicillin and clarithromycin to show an excellent effect on eradicating 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 invention discloses lactobacillus johnsonii with bacteriostatic activity and high digestive tract tolerance and application of the lactobacillus johnsonii, the lactobacillus johnsonii is a new strain HL-RH01, can inhibit growth of helicobacter pylori and can inhibit adhesion of the helicobacter pylori to human gastric mucosa epithelial cells, and meanwhile, the lactobacillus johnsonii has good digestive tract tolerance. Active freeze-dried bacterial powder prepared from the strain can effectively remove helicobacter pylori colonized in a model animal body, and the removal effect is obviously better than that of antibiotic (clarithromycin). The lactobacillus johnsonii with a remarkable bacteriostatic effect is used for treatment or adjuvant treatment of helicobacter pylori infection, so that the clinical problems of low patient compliance and non-ideal eradication effect caused by use of a large dose of antibiotics can be relieved to a certain extent; a wider selection space is provided for the probiotics as a new way for treating helicobacter pylori infection.