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Cefoperazone sodium novel crystal form and its preparation method

A technology of cefoperazone sodium and crystal form, which is applied in the field of preparation of three subtypes, can solve problems such as unqualified content of cefoperazone sodium, and achieve good stability

Active Publication Date: 2009-08-26
SHANGHAI NEW ASIA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The results show that the unqualified content is the main reason for the unqualified domestic cefoperazone sodium for injection products, and the 8 batches of products that did not meet the requirements in this inspection were all drawn from the circulation area

Method used

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  • Cefoperazone sodium novel crystal form and its preparation method
  • Cefoperazone sodium novel crystal form and its preparation method
  • Cefoperazone sodium novel crystal form and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Classification of Cefoperazone Sodium Crystalline Samples

[0042] When powder X-ray diffraction analysis was performed on 112 batches of domestic cefoperazone sodium for injection, it was found that they were both crystalline samples but had two different diffraction patterns. The distribution positions and intensities of the diffraction peaks of the two were different. See figure 1 . It is suggested that the crystalline form of cefoperazone sodium may have two different crystal forms, which we call the A crystal form and the B crystal form respectively. The I / I 0 , 2θ, and d / n values ​​(d / n values ​​are calculated by Bragg equation 2d sinθ=nλ) are listed in Table 1 respectively. It can be seen that the d / n values ​​of crystal form A and crystal form B are significantly different, further indicating that there are two different crystal forms of crystalline cefoperazone sodium.

[0043] Table 1 Powder X-ray diffraction data of two different crystal forms of...

Embodiment 2

[0045] Embodiment 2 Comparison of the stability of crystal form A and crystal form B

[0046] 2.1. Lattice stability

[0047] 2.1.1 High temperature powder X-ray diffraction experiment

[0048] High-temperature powder X-ray diffraction experiments were carried out on the two crystal forms of cefoperazone sodium A and B, and it was found that when the crystal form A was heated to 120°C, the peak intensity of the diffraction peak began to weaken; The single peak is then divided into two diffraction peaks with lower intensity; when the temperature reaches 140°C, the positions and intensities of each diffraction peak do not change much in the diffraction pattern, indicating that the crystal lattice has not changed much, and the thermal stability is relatively high. it is good. The high-temperature powder X-ray diffraction patterns of cefoperazone sodium A and B crystal forms are shown in figure 2 and image 3 .

[0049] 2.1.2 Thermal analysis experiment

[0050] The melting...

Embodiment 3

[0056] Example 3 Cluster Analysis of Cefoperazone Sodium Form A Samples

[0057] A total of 24 batches of cefoperazone sodium crystal form A samples obtained by different production processes were selected for powder X-ray diffraction experiments, and the spectra were analyzed by random RISM.Qualitative Analysis software to obtain the average diffraction peak position (2θ) of 10 strong peaks and the spectra of each sample The corresponding peak intensity (I), the results are shown in Table 2-1, and the relative peak intensity (I / I 0 ), the results are shown in Table 2-2. Using the systematic clustering method provided by SPSS software to classify the A crystal form samples, the A crystal form cefoperazone sodium samples can be further divided into 5 subtypes: the samples numbered 13, 14, 15, 6 and 7 are the first subtype; Samples numbered 4, 17, 12, 19, 11, 8, 10, 1, 2, 3, 16, and 24 were subtype II; samples numbered 5, 20, and 18 were subtype III; samples numbered The sampl...

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Abstract

The invention provides a stable new crystal form of cefoperazone sodium, which is composed of one or more of subtypes I, II and III of crystal form A, and the invention also provides a preparation method of the three subtypes, And the application of these three subtypes in the preparation of anti-infective drugs. The crystal form of the present invention has better stability than the crystal form of the prior art.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a stable crystal form of cefoperazone sodium, as well as preparation methods and applications of three subtypes of the crystal form. Background technique [0002] Cefoperazone sodium (cefoperazone sodium), its chemical name is: (6R, 7R)-3-[[(1-methyl-1H-tetrazol-5yl)sulfur]methyl]-7-[(R)-2- (4-Ethyl-2,3-dioxo-1-piperazinecarbonylamino)-2-p-hydroxyphenyl-acetylamino]-8-oxo-5-thia-1-azabicyclo[ 4.2.0] Oct-2-ene-2-carboxylic acid sodium salt. It belongs to the third-generation cephalosporin antibiotics. It has the advantages of broad antibacterial spectrum and strong antibacterial effect. It is widely used in clinical practice, such as cefoperazone sodium for injection, and the compound preparation made with sulbactam is cefoperazone sodium and sulbactam sodium for injection. [0003] At present, cefoperazone sodium is produced on a large scale at home and abroad. In order to fully underst...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36C07D501/02A61P31/00A61K9/08
Inventor 侯秉章胡昌勤魏瑞萍薛晶
Owner SHANGHAI NEW ASIA PHARMA
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