31 results about "Flucloxacillin sodium" patented technology

The invention discloses a flucloxacillin sodium compound and a method for preparing the same. The method comprises that: firstly, N'N-dibenzylethylene diamine salt and flucloxacillin acid are mixed and reacted to form a salt; and secondly, high-purity flucloxacillin sodium is obtained through the displacement of a cation exchange resin. The invention adopts a purification method which is simple and easy to operate, thereby greatly improving the purity of the flucloxacillin sodium compound to a certain degree, removing a large amount of high molecular polymers, stabilizing the product quality of related preparations and ensuring the safety of clinic medication use.

The invention relates to a preparation method for flucloxacillin sodium. The method comprises the following steps of: (1) weighing 6-aminopenicillanic acid, 3-(2-chloro-6-fluorophenyl)-5-methyl isoxazole-4-phosgene and sodium iso-octoate; (2) adding water into 6-aminopenicillanic acid, cooling in an ice bath, and adding acetone to obtain a solution A; (3) preparing 3-(2-chloro-6-fluorophenyl)-5-methyl isoxazole-4-carbonyl chloride and an organic solvent into a solution B; (4) adding the solution B into the solution A, and performing an acylation reaction; (5) after reacting, acidifying, and adding an organic solvent for extracting; (6) slowly adding a part of organic solution of sodium iso-octoate into the an extracting solution obtained in the step (5), performing a salt-forming reaction, and growing a crystal after the crystal is precipitated out; and (7) after growing the crystal, continually adding the residual sodium iso-octoate solution, preserving heat, stirring, leaching, soaking, washing and drying in vacuum. The method has the advantages of short process route, high process operability and capability of effectively increasing product quality and yield.

The invention provides a suspension powder-injection preparation of an amoxicillin sodium, and flucloxacillin sodium medicinal composition and new application thereof, and particularly discloses a suspension powder-injection preparation of an amoxicillin sodium and flucloxacillin sodium medicinal composition and a method for preparing the same. The suspension powder-injection preparation comprises the following components in part by weight: 1 part of amoxicillin sodium, 1 part of flucloxacillin sodium, 2 to 18 parts of emulsifier, 0.5 to 12 parts of auxiliary emulsifier and 3 to 20 parts of freeze-dry supporting agent. Furthermore, the invention relates to the application of the suspension powder-injection preparation in the preparation of medicaments for treating pelvic inflammatory diseases.

The invention discloses a preparation method for flucloxacillin sodium. The method comprises: (1) adding an initial raw material 1 into dichloromethane, dropwise adding triethylamine, and then dropwise adding pivaloyl chloride for reaction, so as to obtain a mixed anhydride; (2) adding 6-APA into dichloromethane, then adding triethylamine, reacting until the material solution is clear, so as to obtain a 6-APA triethylamine salt solution; dropwise adding the mixed anhydride into the 6-APA triethylamine salt solution for reaction, then distilling at a reduced pressure to remove dichloromethane, so as to obtain an oily substance, then adding acetone into the oily substance, stirring, and filtering off triethylamine hydrochloride, so as to obtain an acetone solution of flucloxacillin triethylamine salt; and (4) adding water and an ethyl acetate solution of sodium 2-ethylhexanoate into the acetone solution of flucloxacillin triethylamine salt, controlling the temperature to be 0-40 DEG C after adding is finished, and crystallizing, so as to obtain flucloxacillin sodium monohydrate. The preparation method has the advantages of mild reaction conditions, high yield, good purity, simple operation, friendliness to environment, and the like.

The invention provides an amoxicillin sodium flucloxacillin sodium medicine compound liposome injection which comprises amoxicillin sodium, flucloxacillin sodium, liposome carrier, lyoprotectant and optionally existing preservative, wherein the liposome carrier is soy lecithin and cholesterol. The liposome injection has good preparation stability, the liposome during freeze drying process does not crack caused by dehydration, fusion, ice crystal formation and the like; and likewise, the liposome keeps good encapsulation efficiency after hydration redissolution.

The invention discloses a method for preparing a flucloxacillin sodium compound, which comprises the following steps of: 1, dissolving flucloxacillin sodium serving as a raw material in water, adding a water-immiscible solvent, and extracting to obtain an aqueous phase which is subjected to primary purification and contains the flucloxacillin sodium; 2, adding alkaline metal or alkaline earth metal alkoxide into the aqueous phase for processing, optionally heating during processing, and filtering to obtain filtrate, namely aqueous solution which is subjected to secondary purification and contains the flucloxacillin sodium; and 3, separating and purifying the solution by using a preparative neutral alumina chromatographic column, collecting a flucloxacillin part in eluent, concentrating under reduced pressure, and drying in vacuum to obtain flucloxacillin sodium subjected to tertiary purification. By the method, the quality of a preparation product is improved, and the toxic and side effects of the flucloxacillin sodium in the process of preparing an antibacterial medicine are reduced; and the method is suitable for large-scale industrial production.

The invention discloses a chemical synthesizing method of 3-(2'-chlorine-6'-fluorophenyl)-5-methyl-4-isooxazole formyl chloride as key intermediate of antibiotic sodium flucloxacillin, which is characterized by the following: adopting di-(trichloromethyl) carbonate and 3-(2'-chlorine-6'-fluorophenyl)-5-methyl-4-isooxazole formic acid as raw material; dissolving the mass into organic solvent acted by organic amide under 0-120 deg.c for 1-20h; recycling organic solvent to obtain the product with high receiving rate; eliminating safe hidden danger; saving manufacturing cost effectively.

The invention relates to the organic amine salt or hydrate for Nishibayashi compound used for treating bacteria infection, and the chemical formula is demonstrated in (I). It comprises azlocillin organic amine salt, amoxicillin organic amine salt, ampicillin organic amine salt, oxacillin organic amine salt, furbenicillin organic amine salt, cloxacillin organic amine salt, mezlocillin organic amine salt, mecillin organic amine salt, piperacillin organic amine salt, ticarcillin organic amine salt, flucloxacillin organic amine salt, hetacillin organic amine salt, ortho-chlorocillin organic amine salt, penicillin organic amine salt and their hydrate. The invention provides the medical compound taking compound in formula (I) as active element and its application to preparation of medicine for treating bacteria infection.

The invention discloses a method for compounding flucloxacillin sodium-hydrate, which belongs to the technical field of drug synthesis, and comprises the steps: 6-aminopenicillanic acid (6-APA) is salified, then 3-(2-chloro-6-fluorophenyl)-5- methyl isoxazole-4-formyl chloride or equivalents thereof are added to do an acylation reaction, and then acids are added drop by drop to adjust a potential of hydrogen (pH) value to obtain flucloxacillin acid aqueous solutions. Organic solution is used to extract, and organic phases are washed, dried and filtered to obtain flucloxacillin acid solutions through saturated salt water, then white solids are dissolved out in the flucloxacillin acid solutions which are added with sodium iso-octoate solutions, and products are obtained by controlling temperature and crystallizing. The method for compounding the flucloxacillin sodium-hydrate does not separate intermediate flucloxacillin acids, obtained flucloxacillin acids are directly salified with sodium iso-octoate after being extracted trough the organic solution, reduces separation steps and operation process, also reduces usage amount and times of organic solution simultaneously, greatly reduces discharge amount of organic solution relative to patent documentation CN 102964356A, reduces production cost above 20%, and obviously improves economic and environmental values.

The invention relates to flucloxacillin sodium and amoxicillin sodium for injection, in particular to a stable flucloxacillin sodium and amoxicillin sodium pharmaceutical composition for injection. The composition comprises flucloxacillin sodium and amoxicillin sodium, wherein flucloxacillin sodium is counted as flucloxacillin, amoxicillin sodium is counted as amoxicillin; and the weight ratio of flucloxacillin to amoxicillin is 1:(0.5-1.5). The pharmaceutical composition has an excellent pharmaceutical performance.

The invention discloses a secondary zinc oxide recycling method which comprises the following steps of a, mixing fly ash and soft coal in an iron and steel plant, feeding into a rotary kiln, and roasting; b, alkaline-washing and leaching roasted cooling material in the step a through a pure alkaline liquor, and separating to obtain a leaching agent; c, adding hydrogen peroxide into the leaching agent, and filtering to remove precipitated substances; d, adding zinc and copper sulfate into the leaching agent, and filtering to move precipitated substances; e, carrying out ion exchange treatment on the leaching agent; and f, electrolyzing a solution obtained after ion exchange, and precipitating zinc. According to the secondary zinc oxide recycling method provided by the invention, flucloxacillin and other impurities contained in secondary zinc oxide can be effectively removed, and the operation cost is low.

The invention relates to a flucloxacillin sodium suspension and a new application thereof. The invention provides the flucloxacillin sodium suspension containing 1 part by weight of flucloxacillin sodium, 3-14 parts by weight of surfactant and 2-20 parts by weight of freeze-drying support agent. The invention further discloses the new application of the flucloxacillin sodium suspension in the preparation of drugs for treating pityrosporum folliculitis.

The invention discloses regulating type stirring equipment for preparation of amoxicillin sodium and flucloxacillin sodium for injection. The equipment consists of a lifting component, two sets of filtering components, a moving component and two sets of stirring components. Lifting oil cylinders of the lifting component are used for lifting mounting plates. The two sets of filtering components aredisposed on a base plate, and the housing of each filtering component contains a filtering screen. Lead screws of the moving component are disposed on the mounting plates, and drive the horizontal movement of a mobile plate by a motor. The two sets of stirring components are disposed at two ends at the top of the mobile plate, and the housing of each stirring component is internally equipped witha stirring part in charge of liquid stirring. The housing cavity bottom ends of the two sets of stirring components are respectively communicated with the housing cavity top ends of the correspondingfiltering components through hoses respectively. The stirring equipment provided by the invention has good stirring effect, is convenient for experiment or actual production use, has wide scope of applicable preparation environment, is suitable for popularization and use, and improves the preparation efficiency of amoxicillin sodium and flucloxacillin sodium for injection.

The invention discloses a flucloxacillin sodium freeze-dried powder injection composition and a preparation method thereof. The composition comprises the following components in parts by weight: 500 parts of flucloxacillin sodium, 10-20 parts of lecithin and 20-40 parts of L-lysine. The preparation method comprises the following steps: (1) dissolving L-lysine and flucloxacillin sodium into water for injection; (2) dissolving lecithin into medicinal ethanol; (3) uniformly mixing the two solutions, filtering the solutions by virtue of a microporous film with the aperture of 0.22 microns, adding the medicinal ethanol into filtrate for volume fixing, adjusting the pH to 5.0 by virtue of a NaOH solution, and performing filling, half tamponade, freeze-drying and tamponade to obtain the flucloxacillin sodium freeze-dried powder injection composition. The flucloxacillin sodium freeze-dried powder injection composition disclosed by the invention is high in stability and easy for realization of industrial production.

The invention discloses a new flucloxacillin sodium crystal form as well as a preparation method and an application thereof, and belongs to the field of medical technologies. An X-ray powder diffraction pattern of the new flucloxacillin sodium crystal form has a strongest diffraction peak namely I / I0=100 when 2theta=11.377 degrees; and an infrared spectrum has characteristic absorption at 792, 896, 1249, 1323, 1400, 1454, 1508, 1600, 1770, 2977 and 3367 cm<-1>. The preparation method comprises the following steps: dissolving flucloxacillin sodium into a ketone solvent, and filtering to obtain a solution A; adding an ether solvent into the solution A, stirring, and cooling to obtain a solution B; and adding an ester solvent into the solution B, stirring for crystallization, filtering, and performing vacuum drying to obtain the new crystal form. The invention also discloses the application of the new crystal form. The new crystal form is easy to dry, can effectively reduce the drying time and reduce the risk of impurity increase, and has a relatively good effect for quality control.

The invention discloses a synthetic method of flucloxacillin sodium. The synthetic method of the flucloxacillin sodium comprises the following steps: (I) under the actions of triethylamine and triethyl phosphite, carrying out condensation reaction on 3-(2-chloro-6-fluorophenyl)-5-methylisoxazole-4-methanoic acid and dibenzothiazyl disulfide in dichloromethane to obtain an active ester reaction solution; and (II) adding water and 6-aminopenicillanic acid in the active ester reaction solution obtained in step (I), then dropwise adding triethylamine for amidation, and after reaction is finished,carrying out aftertreatment to obtain the flucloxacillin sodium. By the synthetic method, an acyl chloride intermediate is avoided, meanwhile, the intermediate does not need to be purified, followed-up steps are carried out directly through a one-pot method, the synthetic method is simple and convenient to operate, the yield and purity of the product are high, and industrialization is facilitated.

The invention discloses flucloxacillin sodium taste-masking granules and a preparation method thereof, particularly relates to a taste masking method for preparing granules from water-soluble medicines (such as flucloxacillin sodium) with strong bitterness and large taking dosage, belongs to the technical field of medicines, and aims to realize masking of the bitterness of the medicines, keep or improve the water solubility and the stability of the medicines to improve the drug compliance of a clinical patient. The flucloxacillin sodium taste-masking granules comprise a master medicine and slave medicinal materials, and are prepared by dissolving or highly dispersing the master medicine into a carrier solution, and then preparing the medicines into granules by a conventional granulation mode, wherein the ratio of a carrier to the master medicines is 25-200 percent; the carrier is a molecular material with high film-forming property and high water solubility. A carrier solution medium is water or an ethanol solution with certain condition; the master medicine is a medicine which is represented by flucloxacillin sodium and is strong in bitterness, high in clinical dosage and high in water solubility.

The invention discloses flucloxacillin sodium taste-masking granules and a preparation method thereof, particularly relates to a taste masking method for preparing granules from water-soluble medicines (such as flucloxacillin sodium) with strong bitterness and large taking dosage, belongs to the technical field of medicines, and aims to realize masking of the bitterness of the medicines, keep or improve the water solubility and the stability of the medicines to improve the drug compliance of a clinical patient. The flucloxacillin sodium taste-masking granules comprise a master medicine and slave medicinal materials, and are prepared by dissolving or highly dispersing the master medicine into a carrier solution, and then preparing the medicines into granules by a conventional granulation mode, wherein the ratio of a carrier to the master medicines is 25-200 percent; the carrier is a molecular material with high film-forming property and high water solubility. A carrier solution medium is water or an ethanol solution with certain condition; the master medicine is a medicine which is represented by flucloxacillin sodium and is strong in bitterness, high in clinical dosage and high in water solubility.

The invention relates to a buccal tablet containing amoxicillin and flucloxacillin, the preparation method and the use. The invention aims to provide a buccal tablet with amoxicillin and flucloxacillin adopted as the medicinal ingredients. The buccal tablet can be dissolved among the salvia in the oral cavity and enter the oral cavity, the pharynx and pharyngeal tonsils to play the role of resisting bacteria. The invention adopts amoxicillin, flucloxacillin and salt derivatives as medicinal ingredients and can be made into various pharmaceutical formulations, such as buccal tablets, candies, dropping pills and so on. The buccal tablet containing amoxicillin and flucloxacillin has the characteristics of fast effect, excellent curative effect and convenient drug delivery, can directly improve the concentration of antibiotic drugs at the pathological part and enhance the antibacterial capacity of the pathological part, and is more suitable for majorities of patients.