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Hydrochloric acid cefotiam crystalline compound, preparation method thereof and medicine combination containing compound

A technology of cefotiam hydrochloride and crystal compounds, applied in antibacterial drugs, organic chemistry, pharmaceutical formulations, etc., can solve the problems of increased risk of allergic reactions, increased polymer content, etc., to improve drug safety and Effectiveness, incidence reduction, high purity effect

Inactive Publication Date: 2012-09-12
HAINAN HERUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although the above-mentioned purification method has solved its purity problem to a certain extent, it has been found through further research that because cefotiam hydrochloride often undergoes degradation and polymerization reactions during storage, especially at high temperatures (>50°C). , as the storage time prolongs, its high polymer content increases, which increases the risk of allergic reactions in the human body

Method used

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  • Hydrochloric acid cefotiam crystalline compound, preparation method thereof and medicine combination containing compound
  • Hydrochloric acid cefotiam crystalline compound, preparation method thereof and medicine combination containing compound
  • Hydrochloric acid cefotiam crystalline compound, preparation method thereof and medicine combination containing compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] [embodiment 1] the preparation of cefotiam hydrochloride crystal

[0043] 1) Prepare the crude product solution: add 200 g of the crude product of cefotiam hydrochloride into 1500 ml of a mixed solvent prepared by methanol and tetrahydrofuran in a volume ratio of 5:1, stir to dissolve, and add 0.1% of the crude product of cefotiam hydrochloride by weight Activated charcoal decolorizes, filters, and obtains the crude product solution, for subsequent use;

[0044] 2) Preparation of crystallization solvent: prepare a crystallization solvent with acetone and ethyl acetate in a volume ratio of 2:10, and the volume of the crystallization solvent is 12 times the weight of the crude product of cefotiam hydrochloride;

[0045]3) Crystallization: under stirring, add the crystallization solvent obtained in step 2) to the crude product solution obtained in step 1), and solids are precipitated; after the addition is completed, continue to add chloroform dropwise under stirring until...

Embodiment 2-9

[0049]

[0050] The crystalline compound of cefotiam hydrochloride obtained in Examples 2-9 was measured by powder X-ray diffraction method, and the X-ray powder diffraction pattern represented by 2θ±0.2° diffraction angle was the same as in Example 1.

preparation Embodiment 1

[0051] [Preparation Example 1] Cefotiam Hydrochloride Sterile Powder for Injection

[0052] Specification:

[0053] Preparation:

[0054] 1. Inner packaging material treatment

[0055] Antibiotic glass bottles, rubber stoppers, and aluminum caps are cleaned, dried, and sterilized according to the conventional process, and set aside;

[0056] 2. Specific steps

[0057] (1) take by weighing the anhydrous sodium carbonate of recipe quantity and the prepared cefotiam hydrochloride crystal of embodiment 1, mix homogeneously in aseptic container;

[0058] (2) Inspection of intermediate products;

[0059] (3) Carry out aseptic subpackaging according to specifications;

[0060] (4) vacuuming, plugging and capping;

[0061] (5) Packaging, full inspection, and storage.

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Abstract

The invention relates to a hydrochloric acid cefotiam crystalline compound and a medicine combination containing the same. The crystalline compound is determined by a powder X-ray diffraction measurement method, and an X-ray powder diffraction pattern represented with a diffraction angle of 2theta+ / -0.2 degree shows characteristic diffraction peak at the positions of 5.9 degrees, 7.9 degrees, 9.3 degrees, 13.0 degrees, 13.6 degrees, 15.7 degrees, 16.8 degrees, 20.4 degrees, 25.7 degrees, 27.0 degrees, 30.9 degrees and 32.9 degrees. The crystalline compound is high in purity, has good heat stability, and can hardly absorb moisture. Simultaneously, the invention further provides a preparation method of the crystalline compound and the medicine combination containing the crystalline compound. The method is simple in process, high in yield, strong in repeatability and suitable for industrial production. The medicine combination containing the crystalline compound is good in stability, thereby improving medication safety and effectiveness and reducing occurrence rate of adverse reactions.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a crystal compound of cefotiam hydrochloride, a preparation method thereof and a pharmaceutical composition containing the compound. Background technique [0002] Cefotiam hydrochloride, cefotiam dihydrochloride, chemical name is (6R-trans)-7-[[(2-amino-4-thiazolyl)acetyl]amino]-3-[[[1 -[(2-(Dimethylamino)ethyl]-1H-tetrazol-5-yl]thiomethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]octane -2-ene-2-carboxylic acid dihydrochloride is a widely used cephalosporin clinically, and its structural formula is: [0003] [0004] Because cefotiam hydrochloride often undergoes degradation and polymerization reactions during storage, especially under high temperature (>50° C.), resulting in decreased content of active pharmaceutical ingredients, enhanced color and increased polymer impurity content. In addition, due to the long storage time of expired cefotiam hydrochloride, the content of a...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/12A61K31/546A61P31/04
Inventor 陶华英张金花
Owner HAINAN HERUI PHARMA
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