- Crystal form of flomoxef sodium, preparation method, pharmaceutical composition and application
-
The invention provides a crystal form of flomoxef sodium. An X-ray diffraction pattern of the crystal form comprises X-ray diffraction peaks as shown in the following 2[theta] angles: 5.2 +/-0.2 degrees and 16.2 +/-0.2 degrees. In addition, the invention also discloses a preparation method of the crystal form compound, a pharmaceutical composition and application of the crystal form compound and the pharmaceutical composition in preparation of anti-bacterial infection drugs. Compared with an amorphous product prepared by a freeze-drying process, the novel crystal form obtained by the preparation method disclosed by the invention has the advantages that the stability of the novel crystal form is obviously superior to that of the amorphous form, which means that the crystal form disclosed bythe invention has less degradation impurity generation and lower drug storage condition requirements within the validity period, and has a good medicinal use prospect.
- -
-
Paragraph 0050-0057
(2020/06/09)
-
- A method for the preparation of fluorine oxygen spore sodium
-
The invention belongs to a new flomoxef sodium preparation method, and particularly relates to a preparation method of flomoxef sodium. The method comprises the steps of: enabling a compound (I) to react with methyl alcohol to generate a compound (II) under the catalysis of ceric ammonium nitrate, next connecting with a tetrazole side chain to obtain a compound (III), removing an amino protection group and a hydroxyl protection group under enzymolysis to obtain a compound (IV), reacting with an intermediate of difluromethylation mercaptoacetic acid active ester to obtain a compound (V), removing the hydroxyl protection group under the effect of trifluoroacetic acid to obtain a compound (VI), and finally obtaining the flomoxef sodium (VII) through a formed sodium salt reaction. The reaction route is as follows. The method provided by the invention has the following advantages that the reaction operation is simple, convenient and reliable, the reaction route is short, the aims of going green and environmental protection, and high productivity are realized, the after-treatment is easy and high-purity flomoxef sodium is obtained.
- -
-
-
- Method for producing Flomoxef Sodium
-
Disclosed is a method of producing flomoxef sodium which is an oxacephem-based antibiotic and has a wide antibacterial activity against various flora. The method of producing flomoxef sodium comprises the steps of: making flomoxef acid react with a sodium ion source in an organic solvent; and crystallizing the flomoxef sodium, which is a reaction product, by filtering and drying a reactant of the previous reaction. Here, it is preferred that a solvent with a low solubility of the flomoxef sodium among the acetone, methyl ethyl ketone, isobutyl ketone, methyl acetate, ethyl acetate, diethyl ether, isopropyl ether, t-butyl methyl ether, tetrahydrofuran, dichloromethane, chloroform, acetonitrile, ethanol, isopropyl alcohol, and a mixture thereof is used as the organic solvent. According to the present invention, high purity flomoxef sodium can be obtained at a high yield.
- -
-
Paragraph 0024; 0025
(2017/06/02)
-
- PROCESS FOR PREPARING FLOMOXEF SODIUM
-
The present invention refers to oxa cephem (oxacephem) in antibiotics sodium [...] flow which is used in the crystallization method relates to desired colors and being obtained by method (flomoxef sodium), flow [...] acid dissolving the a solvent, the organic or inorganic sodium salt reacting a metal salt of the solution, and cooling the reaction mixture sodium [...] flow includes for crystallizing. According to of the present invention method, flow [...] sodium the time and expensive freeze drying is not since the producing crystallization method, freeze-dried first step molding machine and not general forwardly predominantly in production facilities easy to is sodium [...] flow in method may be obtained in a high yield.
- -
-
Paragraph 0029-0030
(2016/12/26)
-
