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Cefathiamidine compound

A cefathiamidine and compound technology, which is applied in the field of cefathiamidine compounds, can solve the problems such as the need to improve the crystal purity of cefathiamidine, and achieve the effects of safety, reliability, good stability and high stability in clinical application.

Active Publication Date: 2014-06-04
YOUCARE PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Patent application 201010596929.7 A preparation method of crystalline cefathiamidine discloses a preparation method of crystalline cefathiamidine, but the purity of the cefathiamidine crystal still needs to be improved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: the preparation of cefathiamidine compound

[0034] 1. Prepare 5 L of saturated aqueous solution of cefathiamidine crude product;

[0035] 2. In a sound field with a frequency of 28KHz and an output power of 50W, under the condition of nitrogen filling, add 20L of a mixed solution of dichloroethylene and cyclohexane at 0°C while stirring, and the addition speed is 100ml / min. The volume ratio of ethylene and cyclohexane is 1:3; after adding the mixed solution, adjust the frequency of the sound field to 18KHz, cool down to 0°C, and the cooling rate is 1°C / hour; grow crystals for 6 hours, remove the sound field after the crystals are precipitated , washed and dried to obtain the cefathiamidine compound.

[0036] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.96%, and the yield is 95.6%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows image 3 Shown; Observation by s...

Embodiment 2

[0037] Embodiment 2: the preparation of cefathiamidine compound

[0038] 1. Prepare 5 L of saturated aqueous solution of cefathiamidine crude product;

[0039] 2. In a sound field with a frequency of 25KHz and an output power of 40W, under the condition of nitrogen filling, add 15L of a mixed solution of dichloroethylene and cyclohexane at 5°C while stirring, and the addition speed is 75ml / min. The volume ratio of ethylene and cyclohexane is 1:4; after adding the mixed solution, adjust the frequency of the sound field to 15KHz, cool down to 0°C, and the cooling rate is 1°C / hour, grow crystals for 6 hours, remove the sound field after the crystals are precipitated , washed and dried to obtain the cefathiamidine compound.

[0040] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.96%, and the yield is 95.6%; the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement is as follows image 3 Shown; Observation by sc...

experiment example 1

[0041] Experimental example 1: Influencing factor experiment

[0042] 1. High temperature test

[0043] Take three batches 101, 102, and 103 of the cefathiamidine crystalline compound prepared in Example 1, put them in simulated market packaging, place them in a sealed clean container, and place them at a temperature of 40±2°C for 10 days. Sampling was carried out on day 0, tested according to key stability inspection items, and the test results were compared with those on day 0.

[0044] 2. High humidity test

[0045] Take three batches 101, 102, and 103 of the cefathiamidine crystalline compound prepared in Example 1, put them in simulated market packaging, put them in a sealed clean container, and place them at 25±2°C for 10 days at a relative humidity of 90%±5%. , samples were taken on the 5th and 10th days, tested according to the key investigation items of stability, and the test results were compared with those on day 0.

[0046] 3. Strong light irradiation test

[00...

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Abstract

The invention relates to the field of medicines, and particularly relates to a cefathiamidine compound. The cefathiamidine is a compound which is obtained by virtue of Cu-K alpha ray measurement and shown as an X-ray powder diffraction pattern 3. The main particle size of the cefathiamidine compound is 650-950mu m, and the distribution width of the cefathiamidine compound is 450-1150mu m. The prepared cefathiamidine crystal compound is excellent in stability, the color of the cefathiamidine compound solution is thinner than a No.3 yellow green colorimetric solution after six-month accelerated test, the hygroscopicity is lower than that of the prior art, the bioavailability is improved, and the cefathiamidine compound is more suitable for clinical use.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cefathiamidine compound. Background technique [0002] Cefathiamidine, chemical name: (6R,7R)-3[(acetoxy)methyl]-7-[α-(N,N'-diisopropylamidinothio)-acetamido]8- Oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid betaine. Its structural formula is: [0003] [0004] Cefathiamidine is the first-generation cephalosporin, and its antibacterial spectrum is similar to that of cephalothin. It has a strong effect on Staphylococcus aureus, Streptococcus viridans, and pneumococcus, and has unique antibacterial activity against Enterococcus. It is mainly used for Staphylococcus aureus , Respiratory tract infection caused by pneumococcus and streptococcus, biliary tract infection, urinary tract infection, gynecological infection, sepsis, pneumonia, meningitis and other infections. [0005] Cefathiamidine is white or off-white crystalline powder; almost odorless, hygroscopic. This prod...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/28C07D501/12
CPCC07D501/12C07D501/28
Inventor 李琦杨磊
Owner YOUCARE PHARMA GROUP
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