Linezolid crystal form B and preparation method and application thereof

A technology of linezolid and linezolid hydrochloride, applied in the field of medicine, can solve the problems of complicated preparation process of linezolid crystal form, affecting the personal safety of operators, difficult mixing of active substances and auxiliary materials, etc. Solubility and dissolution rate, uniform distribution, good drug dissolution effect

Active Publication Date: 2016-04-20
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] This process dissolves linezolid by adding hydrochloric acid, and crystallizes linezolid by adding alkali at low temperature to obtain crystal form VI. This process uses a large amount of hydrochloric acid, which is easy to pollute the water body and is not conducive to workshop operation.
[0015] The crystalline form of linezolid reported in the above literature not only has complicated preparation process and low safety, but also the obtained crystalline form has large particle size and uneven distribution
As we all know, the solubility of linezolid in water is small and only slightly soluble. In order to improve the solubility of linezolid, it is often necessary to adopt the method of crushing and sieving to obtain particles with smaller particle sizes, but it is easy to produce during the crushing process. A large amount of dust not only seriously affects the personal safety of operators, but also causes waste of materials
Moreover, in the process of preparation production, if the particle size of the active substance is large and the distribution is uneven, it is easy to appear that the active substance and the excipients are difficult to mix.

Method used

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  • Linezolid crystal form B and preparation method and application thereof
  • Linezolid crystal form B and preparation method and application thereof
  • Linezolid crystal form B and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Preparation of Linezolid Form B

[0046] Put 2.5g of linezolid hydrochloride into a reaction flask, add 100ml of water, heat to 50°C under stirring, dissolve the solid, add dropwise 10% potassium carbonate solution, and adjust the pH of the reaction solution to 9-10. The reaction solution was stirred and crystallized, cooled naturally to room temperature, and filtered. The resulting filter cake was vacuum-dried at 40-50°C for 4-6 hours to obtain Linezolid Form B, and its XRD pattern was basically as follows: figure 1 shown.

Embodiment 2

[0047] Example 2 Preparation of Linezolid Form B

[0048] 2.2 g of linezolid hydrochloride was placed in a reaction flask, 100 ml of water was added, and the reaction liquid was heated to 40° C. while stirring, and the solid dissolved. 10% potassium carbonate solution was added dropwise to adjust the pH of the reaction solution to 8-9. The reaction solution was stirred and crystallized, cooled naturally to room temperature, and filtered. The resulting filter cake was vacuum-dried at 40-50°C for 4-6 hours to obtain Linezolid Form B, and its XRD pattern was basically as follows: figure 1 shown.

Embodiment 3

[0049] Example 3 Crystal Form Stability Investigation

[0050] Place the linezolid crystal form B sample of the present invention in an environment with a temperature of 25°C and a relative humidity of 60%, and regularly observe the appearance changes of the crystals and detect the content of linezolid. The experimental results are shown in Table 2 :

[0051] Table 2

[0052]

[0053] The experimental results show that the crystal form B of linezolid of the present invention is stable and controllable, convenient for storage and transportation, and meets the requirements for medicinal use.

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Abstract

The invention provides a linezolid crystal form B. In a powder X-ray diffraction pattern of the crystal form, characteristic absorption peaks exist in the 9.43-degree position, the 11.29-degree position, the 13.27-degree position, the 14.13-degree position, the 15.55-degree position, the 16.69-degree position, the 19.04-degree position, the 21.92-degree position and the 22.35-degree position of the diffraction angle 2theta (+/-0.2 degree). The crystal form has the advantages of being small in grain diameter, good in dissolution rate and the like. The invention further provides a preparation method of the crystal form, a medicine composition containing the crystal form in the treatment effective dose, and an application of the medicine composition in treating skin infection caused by various germs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a linezolid crystal form B and a preparation method thereof, as well as a pharmaceutical composition containing a therapeutically effective amount of the crystal form and its application in treating skin infections caused by various bacteria. Background technique [0002] Linezolid, chemical name: (S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl] Methyl]acetamide, the first synthetic oxazolidinone antimicrobial drug for clinical use, is used to treat infections caused by Gram-positive (G+) cocci, including suspected or confirmed hospital-acquired infections caused by MRSA Acquired pneumonia (HAP), community-acquired pneumonia (CAP) complicated skin or skin and soft tissue infection (SSTI), and vancomycin-resistant enterococcus (VER) infection, its molecular formula is C 16 h 20 FN 3 o 4 , have the structure of following formula (I): [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D263/20A61K31/5377A61P31/04
CPCC07B2200/13C07D263/20
Inventor 杨勇盛志辉周炳城乔智涛陈安丰
Owner JIANGSU HANSOH PHARMA CO LTD
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