99 results about "Cinoxacine" patented technology

The invention discloses a preparation method of moxifloxacin hydrochloride, comprising the steps of: reacting the 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinoline carboxylic acid and the S,S-2,8-diazabicyclo[4.3.0]nonane to prepare the moxifloxacin in the presence of organic base in organic solvent under the reaction temperature of 60 to 85 DEG C; separating the moxifloxacin, processing the moxifloxacin by concentrated hydrochloric acid in organic solvent under the reaction temperature of 60 to 85 DEG C to obtain the moxifloxacin hydrochloride.

The invention discloses a preparation method for moxifloxacin and hydrochloride thereof. A conventional process has the following defects that a one-pot material addition process has safety hidden troubles such as bumping materials and explosion which are caused by suddenly increased temperature, and a great amount of wastewater is produced because ice water is employed in a separation process of a borane chelate to perform crystallization process to separate the chelate. The method provided by the invention is characterized in that in a chelating reaction, solid boric acid is added in acetic anhydride in a continuous feeding manner to form a chelating agent through reaction, the chelating agent reacts with 1-cyclopropyl-6,7-difluoro-8-methoxyl-1,4-dihydro-4-oxo quinoline-3-ethyl carboxylate to prepare the borane chelate, and the borane chelate is purified through crystallization and separation by using an organic solvent. The preparation method is simple in process, mild in conditions and safe in the chelating reaction process and solves the problem of the great amount of the wastewater in a preparation process of the chelate. The method has high yield, good selectivity and high product purity and is suitable for industrialized production.

The invention provides an aspartate quinolone antibiotics water-soluble salt and the injection formulation thereof, including sparfloxacin, gatifloxacin, rufloxacin, pefloxacin, tosufloxacin, moxifloxacin, and so on; the invention improves the water solubility of quinolone antibiotics and enhances the anti-bacterial effect of quinolone antibiotics. Compared with the oral liquid of quinolone drugs of the prior art, the invention has the advantages that: water solubility of the drug is good, as the drug enters the blood directly, the invention can not only achieve treatment function rapidly, but can also be absorbed by the human body fully, and the invention has significant effects in the two aspects of fast onset of action and low consumption. Compared with the injection of the quinolone drugs of the prior art, the invention has the advantages that: due to the existence of the L-aspartate, the antibacterial activity of quinolone drugs can be enhanced.

The invention discloses a high selectivity method for synthesizing moxifloxacin. The method comprises the following steps of: reacting boric anhydride with trifluoro acetic anhydride to obtain a chelant; reacting 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid ethyl ester with the chelant, cooling to room temperature, adding ice water, performing suction filtration, and washing a filter cake with water until neutrality to obtain a 1-ethyl-7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid methyl ester trifluoroacetic anhydride boronized chelate; and reacting the 1-ethyl-7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid methyl ester trifluoroacetic anhydride boronized chelate with (S,S)-2,8-diazabicyclo[4,3,0]nonane to obtain a 1-cyclopropyl-6-fluoro-7-([S,S]-2,8-diazabicyclo[4,3,0]nonane-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid ethyl ester trifluoroacetic anhydride boronized chelate, recycling a solvent under reduced pressure, adding alkali, refluxing, discoloring, filtering, freezing, performing suction filtration, and drying a filter cake. The method is simple, mild in conditions, and high in selectivity, avoids difficultly separated impurities, is high in reaction yield and product purity, and is suitable for industrial production.

Topical ophthalmic and otic solution compositions of moxifloxacin and dexamethasone phosphate are disclosed.

The invention discloses a stable moxifloxacin hydrochloride medicinal composition and a preparation method thereof. The stable moxifloxacin hydrochloride medicinal composition consists of moxifloxacin hydrochloride, hydroxypropyl betacyclodextrin, mannitol, microcrystalline cellulose 12 and magnesium stearate. The stable moxifloxacin hydrochloride medicinal composition is high in stability, has the obvious advantages of improving the yield of products, reducing cost and implementing industrialization and is better applied clinically, and preparations of the stable moxifloxacin hydrochloride medicinal composition have high stability.

The invention discloses a preparation method and application of a moxifloxacin analogue Y shown in a figure. The preparation method comprises the following steps: taking moxifloxacin as a raw material, firstly protecting a protection group on a secondary amino group on a 7-position side chain, then performing acyl chlorination and ethyl ester esterification on a 3-bit carboxyl group and removing an amino-group protective agent to obtain the moxifloxacin analogue Y. The preparation of the analogue Y provides a reference substance for moxifloxacin hydrochloride-related substances.

The invention provides a Moxifloxacin capsule, which comprises Moxifloxacin or its salts and/or hydrate, at least a disintegrating agent and at least a lubricating agent, the shell of the capsule contains hydroxy propyl ethyl cellulose. The invention also discloses the process for preparing the capsule.

The invention relates to a pharmaceutical composition containing 9%-40% of mannitol moxifloxacin hydrochloride and/or other hydrates, at least one diluent, at least one disintegrating agent and at least one lubricant and a preparation method thereof. Moxifloxacin hydrochloride tablets prepared according to a formula have the advantages of bioavailability without dissolution limitation, satisfied fragility, good liquidity and production feasibility.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a moxifloxacin hydrochloride sodium chloride injection and a preparation method thereof. The preparation method comprises the following steps: adding moxifloxacin hydrochloride, sodium chloride and a pH regulator into water for injection, stirring for dissolving, filtering through 3 or 4 groupsof polyether sulfone filter elements with sequentially reduced pore diameters, performing filling, and sterilizing to obtain the moxifloxacin hydrochloride sodium chloride injection. The injection provided by the invention is stable in batch content, low in related substance content, high in effectiveness and safety and good in stability.

The invention discloses a method for separating moxifloxacin hydrochloride and impurities thereof by high performance liquid chromatography. The method comprises the following steps: taking alkyl bonded silica gel or phenyl bonded silica gel as a filler; wherein a mixed solution of a water phase and an organic phase is used as a mobile phase, the water phase is an aqueous solution of fluorinated organic acid, and the organic phase is methanol or acetonitrile; gradient elution is performed; the method has good specificity, linearity and system durability, can be used for detecting nine impurities including impurities A, B, C, D, E, H, I and J and an impurity M introduced in the moxifloxacin hydrochloride synthesis process, and has certain practicability.

The invention discloses a preparation method of a moxifloxacin intermediate 6-benzyl-octahydro-pyrrolo[3,4-b]pyridine (as shown in formula I). The preparation method is to adopt an NaBH4/H2SO4 reducing system to reduce 6-benzyl-hexahydro-pyrrolo[3,4-b]pyridine-5,7-dione (as shown in formula II), so as to obtain the target product. The method can be processed at normal temperature and normal pressure to take reaction with high total recovery; the raw material is cheap, easy to get, and easy to store; the operation is simple; the safety is high.

The invention discloses a method for detecting an antibacterial agent in serum by an ultra-high performance liquid chromatography-tandem mass spectrometry technology. The antibacterial agent containssulbactam (SBT), imipenem (IPN), linezolid (LNZ), melopenem (MPN), moxifloxacin (MXC), piperacillin (PRC), tigecycline (TGC), cefoperazone (CFZ), vancomycin (VCM) and teicoplanin (TCL). The method comprises the steps: detecting the content of the antibacterial drug in the pretreated serum by adopting an ultra-high performance liquid chromatography tandem mass spectrometry method, quantifying by utilizing a mass spectrometry isotope internal standard method, establishing a calibration curve by taking the concentration ratio of a standard substance to an internal standard substance as an X axisand the peak area ratio of the standard substance to the internal standard substance as a Y axis, and calculating the concentration of a target drug in the serum. According to the method, the pretreatment process is simple, the sensitivity is high, the specificity is high, separation and detection of the antibacterial agent are completed within 5 min, and a reliable detection method is provided for monitoring the treatment concentration of the antibacterial agent clinically.

The invention relates to a small-volume moxifloxacin hydrochloride injection and a preparation method thereof. The preparation method comprises the following steps of: regulating the PH value of 0.01-0.04/ml of moxifloxacin hydrochloride water solution for injection to 4.2-4.7, adding activated carbon for absorption, treating by a filter membrane of 0.22mu m, filling nitrogen, encapsulating and sterilizing to prepare 10ml of small-volume injection. The injection product does not have sub-visible particles, is good in clarity and safe in medication, can be conveniently mixed with injections such as glucose, mannitol and the like, and is not restricted to a sodium chloride injection. The invention solves the problem that the sodium chloride injection can not be used for some patients having specific physiques.

The invention discloses a method for synthesizing a moxifloxacin degradation impurity. The method comprises the following steps: (1) enabling a compound of a formula 1 shown in the description to contact with p-methyl benzene sulfonic chloride so as to otbain a compound of a formula 2 shown in the description; (2) performing an oxidation on the compound of the formula 2 shown in the descrption soas to obtain a compound of a formula 3 shown in the description; (3) removing p-methyl benzene sulfonic chloride from the compound of the formula 3 shown in the description so as to obtain a compoundof a formula 4 shown in the description; (4) performing a substitution reaction on the compound of the formula 4 shown in the description and a compound of a formula 5 shown in the description so as to obtain a compound of a formula 6 shown in the description; and (5) performing acidic hydrolysis on the compound of the formula 6 shown in the description, so as to obtain a compound of a formula 7 shown in the description. The invention provides a method for orientated synthesis of the compound of the formula 7 shown in the description, by using the method, the compound of the formula 7 shown inthe description can be prepared, and meanwhile, the compound of the formula 7 shown in the description can be used as an impurity reference product for detecting related substances of the moxifloxacin degradation impurity.

The invention belongs to the field of pharmaceutical preparations and particularly relates to a moxifloxacin hydrochloride external preparation and a preparation method thereof. The external preparation specifically refers to a cream and comprises a combination of a skin penetration enhancer comprising N-trimethyl chitosan, menthol and isopropyl myristate, the external preparation can be directly acted on an infection part, the gastric and intestinal irritation caused by oral administration is avoided, and the skin is not irritated either. The cream further greatly improves the skin penetration rate of a medicine, so that the local absorption is fast, and the treatment effect is remarkable. To further enhance the anti-inflammatory and anti-allergic effects, a non-steroidal anti-inflammatory drug, namely butyl flufenamate, is further added in the cream. The preparation process of the cream is simple and feasible, is high in reproducibility, and is suitable for industrial production.

The invention discloses a preparation method of moxifloxacin hydrochloride and an intermediate thereof. The preparation method of the intermediate III of the moxifloxacin hydrochloride includes the following steps: making an intermediate II of the moxifloxacin hydrochloride and (S,S)-2,8-diazabicyclo[4,3,0]nonane have condensation reaction in an organic solvent in the presence of alkali to obtainthe intermediate III of the moxifloxacin hydrochloride. The preparation method is simple and safe in operation, does not require special equipment and avoids use of highly toxic materials and mild inreaction conditions. The obtained the moxifloxacin hydrochloride I has high purity and low production cost, and is suitable for industrial production. (img file='DDA0001750656940000011.TIF' wi='700' he='192'/).

The present invention features an antibacterial composition comprising 1) a composition A comprising polymyxin B and trimethoprim; and 2) an antibiotic agent selected from the group consisting of rifampicin, rifabutin, rifapentine, rifaximin, pefloxacin mesylate, sparfloxacin, sarafloxacin HCl, tobramycin, lomefloxacin, besifloxacin, danofloxacin mesylate, enrofloxacin, nadifloxacin and clinafloxacin, a topical pharmaceutical thereof, and a method of treating bacterial infections using mixtures of 1 and 2.

The invention discloses a synthetic method of moxifloxacin hydrochloride. The synthetic method comprises the following steps: under the protection of argon, taking gatifloxacin carboxylate and (S,S)-2,8-diazabicyclo[4.3.0]nonane as raw materials; taking an organic alkali or an inorganic alkali as an acid-binding agent and a Lewis acid as a catalyst; reacting in a certain solvent at a proper temperature; concentrating, processing by alkali liquor, separating out moxifloxacin monomers at an isoelectric point, reacting moxifloxacin monomers with an acid to form salt, concentrating to obtain a moxifloxacin hydrochloride crude product, re-crystallizing, filtering, washing and drying to obtain a refined moxifloxacin hydrochloride finished product. The preparation method is mild in reaction conditions, simple to operate, less in pollution, and high in yield and industrial production can be realized easily.