477 results about "Azithromycin" patented technology

A novel, non-hygroscopic form of azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization of azithromycin from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this novel form of azithromycin are also disclosed.

The present invention relates to the technical fields of organic chemistry and pharmaceutical chemistry, concretely discloses a synthetic method for a known compound tylosin. The synthetic method comprises the following steps: taking Azithromycin A as a raw material, the protected Azithromycin A can be obtained by Cbz-Cl and then oxidized through a modified Pfitznor-Moffat method, the protected ketone by Cbz can be obtained, ketone is reacted through Wittig-Horner, keto is conversed into alkenyl to obtain the protected alkene, the protected alkene is oxidized to obtain an epoxy compound protected by Cbz, the epoxy compound protected by Cbz is deprotected to obtain a deprotected epoxy compound under the catalysis of Pd / C, the deprotected epoxy compound is reacted with n-propylamine and is performed a ring-opening to obtain a tylosin crude product, the tylosin crude product and acid are carried out a salt forming and purifying, then tylosin can be obtained by resolving. The synthetic route is changed by the method of the invention, the super low-temperature is not employed in the route, and the tylosin enables the effective industrialization production.

The invention provides a tulathromycin intermediate, a preparation method of the tulathromycin intermediate, and a preparation method of the tulathromycin. The preparation method of the tulathromycin has the advantages of mild condition, convenience for operation, and low cost. The preparation method of the tulathromycin comprises the following steps of: using azithromycin A as a raw material; protecting 2'-hydroxy and 6'-amino in the azithromycin A through di-tert-butyl dicarbonate so as to obtain double-protective azithromycin A; carrying out Swern oxidation to 4''-hydroxy to the double-protective azithromycin A; salifying along with trifluoroacetic acid; and synchronously removing boc t-butyloxycarbonyl to obtain the azithromycin A bitrifluoroacetic acid salt of 4''-carbonyl; and then reacting with trimethylsulfonium bromide to obtain 4''-epoxy compound; and finally carrying out nucleophilic addition on the 4''-epoxy compound by n-propylamine so as to obtain the phosphate of tulathromycin; and further neutralizing via alkaline to obtain the target compound tulathromycin; and synchronously obtaining the tulathromycin intermediate of azithromycin A bitrifluoroacetic acid salt of 4''-carbonyl.

The invention discloses a novel method for preparing tulathromycin and relates to a semi-synthetic macrolide antibiotic. The method comprises the following steps: simultaneously protecting 2'-hydroxyl and 6a-amino of desmethyl azithromycin with acetyl, then carrying out oxidation and epoxidation on 4''-hydroxy, then removing the protecting groups under alkaline alcohol solution conditions, and carrying out nucleophilic addition on 4''-epoxy group with n-propylamine to obtain the target compound tulathromycin. Compared with the prior art, the method for preparing tulathromycin has the advantages of simple process, mild conditions, high yield and the like, and is beneficial to industrial production.

The invention discloses a method for preparing azithromycin. The method comprises the following steps of: in acid aqueous solution and under an action of potassium borohydride, performing the reduction reaction of erythromycinA6, 9-imine ether represented by a formula II, then performing methylation reaction, and putting the reaction products in a mixed solvent of water and halogenated hydrocarbons for hydrolysis reaction so as to obtain the azithromycin represented by a formula I. In the method, the reducer is properly consumed, the yield is high, and the cost of the preparation of the azithromycin is obviously reduced. The invention also relates to a method for preparing the erythromycinA6, 9-imine ether and erythromycinA9-oxime.

The invention discloses a medicament formula for relieving pain caused by infusion medicament and preventing phlebitis. The medicament formula can be used for relieving pain caused by intravenous supplementing potassium, infusion mannitol, azithromycin, fructose diphosphate sodium and chemotherapeutic medicaments, and can be used for effectively preventing and treating extravasation phlebitis caused by long-term use of a remaining needle, infusion of vein high-nutrition medicaments, infusion of chemotherapeutic medicaments, infusion extravasation and the like. According to the medicament formula, 20-35ng of anisodamine, 6-13ml of lidocaine, 15-26mg of dexamethasone and 4-6ml of glycerin are arranged in a sterile kidney basin, sterile gauze is coated above a puncture part after being uniformly wetted, and an external preservative film is wound on the gauze. The medicinal formula has the advantages of continually and efficiently relieving local pain caused by infusion medicaments, and effectively preventing and treating local inflammation, swelling pain and stripped cable change caused by infusion.

The invention features methods and compositions for treating ocular infections. The method comprises topically administering to an eye of an animal in need of such treatment an ocular infection-treating amount of azithromycin.

The present invention is directed to a pharmaceutical composition comprising a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. A suitable antibiotic is selected from the group consisting of doxycycline, gentamicin, tobramicin, ciprofloxacin, clindamycin, clarithromycin, azithromycin and metronidazole. Preferred antibiotics are doxycycline and ciprofloxacin. More preferably, the antibiotic is doxycycline. In its second aspect, the present invention is directed to a method for treating periodontal disease in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of misoprostol and an effective amount of an antibiotic. Typically, the mammalian patient is a human.

A controlled-release dosage form of azithromycin having an improved side effect profile; a process for preparing the dosage form; and a method of treating a microbial infection, comprising administering azithromycin in such a controlled-release dosage form to a mammal, including a human patient, in need of such treatment.

The invention provides a method for preparing a tulathromycin compound. The method comprises the steps that: demethylated azithromycin is adopted as a raw material; and reactions such as substitution, oxidation, addition, reduction, condensation, and the like are carried out, such that a target compound is obtained. According to the invention, a cheaper raw material is adopted, and a traditional process employing low-temperature reaction is changed. The method has the advantages such as short process route, easy-to-control reaction, high yield, and the like. The method is suitable for large-scale industrialized productions.

Azithromycin is first reacted with equivalent organic or inorganic salt to produce water soluble salt, with it then further produced into eye drop, including eye tablet comprising the water soluble salt of Azithromycin and some medical supplementary material as well as special liquid comprising water, medical supplementary material and bacteriostat. When used, the eye tablet is thrown into the special liquid and the mixture liquid is shacked to obtain clear and transparent eye drop for dropping eye. Compared with available oral preparation, the eye drop is well soluble, low in dosage, direct absorbed in eye to reach the effective bacteriostasis density fast and other advantages.

The invention provides a sterilizing method of a spherical phaeocystis culture solution, and relates to a microalgae culture solution. The method comprises the following steps: centrifuging algae solution which grows to an exponential phase, and removing supernatant; carrying out gravity suspension on algae cells with an f / 2 culture medium, centrifuging, and removing supernatant, repeating twice, and carrying out gravity suspension on the algae cells with the f / 2 culture medium; adding SDS (sodium dodecyl sulfate) and antibiotics, wherein the antibiotics are clindamycin, azithromycin, gentamicin, kanamycin, streptomycin, cefotaxime, ampicillin and rifamycin; culturing under illumination, centrifuging the algae solution and removing supernatant during culturing, carrying out gravity suspension on the algae cells with the f / 2 culture medium, centrifuging and removing supernatant, removing residual SDS and the antibiotics, transferring into the f / 2 culture medium, and culturing under illumination; and selecting survival transferred algae solution which is treated with SDS and the antibiotics, and detecting whether bacteria exist or not after the transferred algae solution grows to the exponential phase. The method is convenient to operate, complex operations, such as bacterium separation and test on sensitivity to antibiotics and the like, are avoided, and long-term treatment of high-concentration antibiotics has good sterilization effect.

The invention relates to the field of chemical synthesis and particularly relates to a preparation method of tulathromycin. The method comprises protecting a 2-hydroxyl group of demethyl azithromycin through 4-nitrobenzyl chloroformate, carrying out oxidation and epoxidation on a 4"-hydroxyl group, and carrying out deprotection and 4"-epoxy nucleophilic addition through n-propylamine to obtain tulathromycin. Comprised with the prior art, the preparation method has simple processes, mild conditions and a high yield, is free of palladium-carbon hydrodeprotection and is conducive to industrial production.

The invention relates to the field of pharmaceutical preparation, in particular relates to an azithromycin ophthalmic instant molding gel. The azithromycin ophthalmic instant molding gel is characterized in that the azithromycin ophthalmic instant molding gel comprises azithromycin, a temperature sensing substrate, carbomer, a permeation pressure conditioning agent and water for injection, wherein the temperature sensing substrate comprises poloxamer 407 and poloxamer 188. The invention further discloses a preparation method thereof. The invention uses the poloxamer 407 and the poloxamer188 as the temperature sensing substrate with good biocompatibility. The preparation is flowable fluid preparation under the condition of invitro storage; the preparation forms gel when the external environment of dropping in ocular region is changed, so as not to flow in ocular region; therefore, the pharmic action time is remarkably prolonged, time administer drug is reduced and the adaptability of the patient is improved.

The invention relates to application of azithromycin to preparation of anti-coronavirus-infection medicine, and application of a medicine composition containing azithromycin to preparation of anti-coronavirus-infection medicine or combined application of azithromycin and other antiviral medicine.

A penetrating antibiotic gel for treating pain, inflammation and other pathological conditions affecting musculoskeletal tissues and other soft tissues of the body. The composition includes an antibiotic compound and a mobilizing agent in an amount sufficient to enable the antimicrobial compound to penetrate into the sub-dermal soft tissues. The antimicrobial compound may be a macrolide antibiotic compound such as azithromycin, erythromycin or roxithromycin, for example, and the mobilizing agent may be an organogel compound, such as pluronic lecithin liposomal organogel (PLO). The composition may further include a penetration enhancing adjuvant, such as d-limonene, for example. The composition may be applied topically so as to penetrate into the sub-dermal soft tissues, or may injected so as to be absorbed into the soft tissues locally.

The invention discloses a preparation method of azithromycin intermediate, in particular to a preparation method of azithromycin intermediate 9- deoxidation-alpha- heterocyclic nitrogen-9a-erythromycin A, belonging to the field of pharmaceutical chemical synthesis. The preparation method comprises the steps of: in acid aqueous solution, under the action of potassium borohydride or sodium borohydride, carrying out reduction reaction on erythromycin A 6, 9-imine ether, adding organic saccharic acid for hydrolysis reaction, and obtaining the 9-deoxidation-alpha-heterocyclic nitrogen-9a-erythromycin A. By adopting the method, the hydrolysis of boric acid ester is thorough, the products of acid degradation are less, the yield is high, the production cost of azithromycin is remarkably reduced, and the industrialized production can be very smoothly carried out.

The invention provides an azithromycin production technology. The azithromycin production technology comprises (1), erythromycin oxime synthesis, (2), erythromycin A-6,9-iminoether synthesis, (3), 9-deoxo-9a-aza-9a-homoerythromycin synthesis, (4), azithromycin synthesis and (5), refining. The azithromycin production technology realizes strict control of an acetone-water ratio in erythromycin A-6,9-iminoether synthesis, guarantees dispersibility of erythromycin oxime in a system, is convenient for reaction control, improves a yield and can be industrialized easily. In 9-deoxo-9a-aza-9a-homoerythromycin synthesis, pH is controlled in a range of 1.0-1.5 in reduction product acidolysis so that reduction product hydrolysis is thorough, a yield is improved and post-treatment troubles are reduced. In a methylation reaction for azithromycin synthesis, a crystallization water dropwise addition rate and a dropwise addition total amount are strictly controlled so that crystallization is complete, granularity is uniform and an azithromycin yield is improved.

The invention relates to a method for preparing azithromycin superfine powder by ultrasound homogenization dissolvent diffusion method which comprises the steps of, (1) loading water solution of 0.2-2% (w / v) of hydrophilic polyelectrolyte stabilizer into 0-25 deg. C water-bath, (2) under the ultrasonic condition, dropping ethanol solution of Azithromycin into water solution of hydrophilic polyelectrolyte stabilizer, (3) subjecting the opacity solution system to ageing 2-24 hours, high speed centrifugalizing until the complete separation of solid body, (4) centrifugally washing the obtained solid body with distilled water 2-8 times, drying in 40-60 deg. C vacuum drying oven.

This invention relates to methods of treating dry eye disease. The methods comprise identifying a patient suffering from dry eye disease, and topically administering to the eyes of the patient an effective amount of azithromycin and an effective amount of a retinoid. The method is useful in relieving the signs and symptoms of dry eye disease. This invention also relates to a pharmaceutical composition comprising azithromycin and a retinoid such as retinyl palmitate.

The invention discloses an enteric-coated azithromycin preparation and its preparing process, which comprises effective dosage of azithromycin or medicinal excipient, wheein the medicinal excipient include surface active agent, bulking agent, crumbling agent, lubricating agent, moistening agent or binding agent, intestine solution dressing material and plasticizer.

The invention discloses azithromycin eye drops and the preparation. The eye drops is a stable ophthalmic preparation made by azithromycin or axithromycin salt as the active ingredient which is assisted by a stabilizer, a pH regulator, an antiseptic, an isotonic agent and a pasting agent; wherein the optimized stabilizer is propanetriol, the pH regulator is sodium phosphate buffer, the antiseptic is Ethyl p-hydroxybenzoate, the isotonic agent is sodium chloride and the pasting agent is sodium hyaluronate. Compared with oral delivery, the invention has the advantages of less dose, small side effect on a whole body, direct absorption at the ocular region, quick achieving effective antibacterial concentration and quick developing treating function; and compared with ophthalmic gel or ophthalmic ointment, the invention has the advantages of convenient application and good tolerance for a patient; thus the reasonable preparation process and stable performance of the invention guarantees the clarity and stability of eye drops.

The present invention relates to a method for treating non-infectious, inflammatory chronic posterior blepharitis in a subject. The present invention also relates to a method for treating chronic posterior blepharitis in a subject for over two weeks. The method comprises identifying a subject in need thereof, and topically administering to the eye of the subject a pharmaceutical formulation consisting essentially of an effective amount azithromycin. The present invention further relates to a method for treating dry eye secondary to blepharitis in a subject. The method comprises the steps of: identifying a subject suffering from dry eye secondary to posterior blepharitis, and topically administering to the eye of the subject a pharmaceutical formulation comprising an effective amount of azithromycin. The present invention further relates to method for reducing contact lens intolerance of a subject due to blepharitis or dry eye secondary to blepharitis.

The invention provides an azithromycin-containing aqueous pharmaceutical composition, which comprises at least one member selected from the group consisting of azithromycin, its anhydride, its hydrate, and pharmaceutically acceptable salts thereof, and at least one member selected from the group consisting of monoethanolamine, diethanolamine, triethanolamine, amino acid, ethylenediaminetetraacetic acid, and pharmaceutically acceptable salts thereof, and which does not comprise boric acid or pharmaceutically acceptable salts thereof, and a method for the preparation of the composition, wherein an azithromycin-containing liquid is maintained at pH of 4.0 or higher throughout the method for the preparation. The composition has good heat and storage stability.

The invention discloses an Azithromycin derivant and preparing method and medicinal application relating to macrolides medicine, which also relates to medicinal compositions with one or a plurality of Azithromycin derivants and the application of compound and medicinal compositions in treating communicable disease from sensitized bacteria and other causal agents.

The present invention is one kind of composition for eye medicine preparation. The composition contains antibiotic azithromycin lactobionate as active component; at least one kind of surfactant and / or co-surfactant, such as hydrogenated castor oil and Transcutol-p, in such amount as to form micro emulsion; and medicinal supplementary material, such as boric acid, borax and sodium bisulfite. The composition is prepared into eye drop or eye gel, and when it is prepared into gel, carbomer is used as the gel matrix. Compared with similar products, the composition of the present invention has high stability, less irritation to eye, capacity of be used to child and other advantages.

The present invention discloses a kind of oral azithromycin resin suspension and its preparation process, and aims at making the suspension possess good taste. The oral azithromycin resin suspension consists of in each 100 ml azithromycin 0.25-4.0 g, ion exchange resin 0.5-8.0 g and water for the rest. Its preparation process includes the following steps: mixing azithromycin, inorganic acid and / or organic acid and pure water; adding ion exchange resin to obtain mixed liquid; preparing suspension medium with suspending agent, surfactant and pure water; adding metal ion complexing agent, preservative, corrective and colorizing agent; adding the mixed liquid. The present invention is superior to available technology in that the oral azithromycin resin suspension has the bitter of azithromycin masked by the ion exchange resin and thus good taste.

The present invention relates to a method for treating non-infectious, inflammatory chronic posterior blepharitis in a subject. The present invention also relates to a method for treating chronic posterior blepharitis in a subject for over two weeks. The method comprises identifying a subject in need thereof, and topically administering to the eye of the subject a pharmaceutical formulation consisting essentially of an effective amount azithromycin. The present invention further relates to a method for treating dry eye secondary to blepharitis in a subject. The method comprises the steps of: identifying a subject suffering from dry eye secondary to posterior blepharitis, and topically administering to the eye of the subject a pharmaceutical formulation comprising an effective amount of azithromycin. The present invention further relates to method for reducing contact lens intolerance of a subject due to blepharitis or dry eye secondary to blepharitis.

The invention provides a synthetic method of high-purity tulathromycin. The method includes subjecting demethylated azithromycin adopted as a raw material to substitution, oxidation, addition, reduction, condensation, and the like, so as to obtain a target compound. According to the synthetic method, the cheaper raw material is adopted, and a traditional process employing low-temperature reaction is changed. The method has the advantages of short process route, easy-to-control reaction, high yield, and the like. The method is suitable for large-scale industrialized production.

The invention relates to a preparation method for a tulathromycin intermediate. The preparation method comprises the following steps: oxidizing 4'-hydroxyl of demethylazithromycin of which the hydroxyl is protected by acetyl under a mild condition to obtain ketone by using a dimethyl sulfoxide and acetic anhydride system, and continuing to epoxidize the obtained ketone to obtain an epoxide by using a phase transfer catalyst, wherein the intermediate epoxide of tulathromycin can be introduced into propylamine through an open loop, and is subjected to deprotection to obtain the tulathromycin. According to the reaction method, a phase transfer catalyst system is adopted for the first time in an exoxidizing process, reaction conditions are mild, and the method is high in yield and more suitable for industrial production.