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Cefotiam hydrochloride compound, and preparation method and pharmaceutical composition thereof

A technology for cefotiam hydrochloride and a compound, which is applied in the field of cefotiam hydrochloride compounds, can solve problems such as poor storage stability of cefotiam hydrochloride, and achieve the effects of good storage stability, high safety performance and low impurity content

Active Publication Date: 2014-04-09
GUANGZHOU LIXIN PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The storage stability of cefotiam hydrochloride in the above-mentioned patents and the prior art is relatively poor, and its related substances will increase significantly in light and humid environments. In order to obtain a cefotiam hydrochloride compound with better performance, this invention

Method used

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  • Cefotiam hydrochloride compound, and preparation method and pharmaceutical composition thereof
  • Cefotiam hydrochloride compound, and preparation method and pharmaceutical composition thereof
  • Cefotiam hydrochloride compound, and preparation method and pharmaceutical composition thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] The preparation of cefotiam hydrochloride compound:

[0046] Dissolve 50 g of cefotiam hydrochloride crude drug in dimethyl sulfoxide at 60°C to make a saturated solution, keep warm and stir for 20 minutes, then slowly add water at 60°C, the volume of water used is 1 / 1 of the volume of dimethyl sulfoxide 10. Continue to heat and stir for 20 minutes, and flow the solution through a 0.5T DC magnetic field at a speed of 5m / s. The direction of the magnetic field is perpendicular to the flow direction of the solution. Activated carbon is added to the treated solution for decolorization. 0.2% g / ml by volume, stirred for 20 minutes, filtered to obtain a clear solution, and acetone was added dropwise to the clear solution, the volume ratio of acetone to dimethyl sulfoxide was 5:1, cooled to 5°C, filtered, Obtain a filter cake, wash the filter cake, and then dry under reduced pressure for 4 hours to obtain a light yellow microcrystalline powder. The yield is 68.8%, and the HPLC...

Embodiment 2

[0049] The preparation of cefotiam hydrochloride compound:

[0050] Dissolve 50 g of cefotiam hydrochloride crude drug in dimethyl sulfoxide at 70°C to make a saturated solution, keep warm and stir for 30 minutes, then slowly add water at 70°C, the volume of water used is 1 / 1 of the volume of dimethyl sulfoxide 12. Continue to heat and stir for 30 minutes, and flow the solution through a 0.5T DC magnetic field at a speed of 10m / s. The direction of the magnetic field is perpendicular to the flow direction of the solution. Add activated carbon to the treated solution for decolorization. 0.3% g / ml by volume, stirred for 20min, filtered to obtain a clear solution, decolorized by activated carbon, filtered, and acetone was added dropwise to the clear solution, the volume ratio of the acetone to dimethyl sulfoxide was 3:1, and the temperature was lowered to Filter at 0°C to obtain a filter cake, wash the filter cake, and dry under reduced pressure for 2 hours to obtain a light yello...

Embodiment 3

[0053] Preparation of Cefotiam Hydrochloride Sterile Powder Injection:

[0054] Weigh 100 g of cefotiam hydrochloride and 20 g of sodium carbonate prepared in Example 1 under aseptic conditions, place them in a solid powder mixer and mix them evenly, and the raw materials obtained are transferred to a sterile preparation workshop for precise metering and packaging. Each bottle contains hydrochloric acid Cefotiam 0.25g, stoppered and capped, the finished product is packaged for storage and sent for inspection.

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Abstract

The invention provides a cefotiam hydrochloride compound, the structural formula of which is shown in the specification. The X-ray powder diffraction spectrogram of the cefotiam hydrochloride compound obtained by using Cu-Ka ray measurement is shown in figure 1. The invention further provides a preparation method of the cefotiam hydrochloride compound and a pharmaceutical composition containing the cefotiam hydrochloride compound. The cefotiam hydrochloride compound is in a form of sterile powder-injection and freeze-dried powder injection. Compared with the prior art, the cefotiam hydrochloride compound and the pharmaceutical composition thereof have better storage stability, so that the medication safety of patients is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a cefotiam hydrochloride compound, a preparation method of the cefotiam hydrochloride compound and a pharmaceutical composition thereof. Background technique [0002] Cefotiam hydrochloride, the English name is Cefotiam Hydrochoride, and its chemical name is ((6R,7R)[2-(2-amino-1,3-thiazol-4-yl)acetamido]-3[[1-( 2-Dimethylaminoethyl)-1H-tetrazol-5-yl]thiomethyl]-8-oxo-5-thio-1-nitrobicyclo[4.2.0]oct-2-ene-2-carboxy acid dihydrochloride); molecular weight 562.08. [0003] Cefotiam is a second-generation semi-synthetic cephalosporin developed by Takeda Corporation of Japan and first launched in Japan in 1981. The effect of this product on Gram-positive bacteria is close to that of cefazolin, and it has better effect on Gram-negative bacteria, such as Haemophilus, Escherichia coli, Klebsiella, and Proteus mirabilis. , Citrobacter, and indole-positive Proteus also hav...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/12A61K31/546A61P31/04
Inventor 闫晓晔梁宏平
Owner GUANGZHOU LIXIN PHARM CO LTD