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Novel crystal form of p-aminosalicylic acid as well as preparation method and applications thereof

A technology of p-aminosalicylic acid and crystal form, applied in the field of medicinal chemistry, can solve the problems of high manufacturing cost and use cost, unstable aminosalicylic acid, etc., achieve high manufacturing cost and use cost, easy processing, The effect of short process steps

Active Publication Date: 2015-03-11
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the instability of aminosalicylic acid, more stringent requirements are put forward for the processing, storage and transportation of the preparation, which ultimately makes the manufacturing cost and use cost of the product remain high

Method used

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  • Novel crystal form of p-aminosalicylic acid as well as preparation method and applications thereof
  • Novel crystal form of p-aminosalicylic acid as well as preparation method and applications thereof
  • Novel crystal form of p-aminosalicylic acid as well as preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Add 500ml of ethyl acetate into a clean and dry reaction bottle, start stirring, protect the reaction system with nitrogen, then add 108g of p-aminosalicylic acid, then heat up to control the temperature of the reaction solution at 50±2°C, and stir to dissolve. Filter, lower the temperature to -10±2°C, stir and crystallize for 1.0 hour, filter, and dry the obtained material at 50±2°C to obtain 91.8g of p-aminosalicylic acid crystal form A with a purity of 99.91% and a yield of 85%. X-ray powder diffraction test pattern see attached figure 1 shown.

[0072] The X-ray powder diffraction characteristic absorption peak of p-aminosalicylic acid crystal form A obtained in Example 1 of Table 1

[0073] 2θ

Embodiment 2

[0075] Add 500ml of ethyl acetate into a clean and dry reaction bottle, start stirring, protect the reaction system with nitrogen, then add 108g of p-aminosalicylic acid, then heat up to control the temperature of the reaction solution at 50±2°C, and stir to dissolve. Filter, cool to 0±2°C, stir and crystallize for 1.0 hour, filter, and dry the obtained material at 50±2°C to obtain 89.6g of p-aminosalicylic acid crystal form A with a purity of 99.92% and a yield of 83%. The X-ray powder diffraction pattern is within the error range and figure 1 unanimous.

Embodiment 3

[0077] Add a mixed solvent of 350ml of tetrahydrofuran and 105ml of dichloromethane into a clean and dry reaction bottle, start stirring, protect the reaction system with nitrogen, then add 40g of p-aminosalicylic acid, then heat up to control the temperature of the reaction solution at 50±2°C, and stir dissolve clear. Filter, lower the temperature to -5±2°C, stir and crystallize for 1.0 hour, filter, and dry the obtained material at 50±2°C to obtain 29.6g of p-aminosalicylic acid crystal form A with a purity of 99.92% and a yield of 74%. The X-ray powder diffraction pattern is within the error range and figure 1 unanimous.

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Abstract

The invention relates to the field of pharmaceutical chemistry, in particular to a novel crystal form of p-aminosalicylic acid and a preparation method thereof. A crystal in the novel crystal form is subjected to X-ray powder diffraction, diffraction peak positions 2theta are used as spectrogram characteristic parameters, and 2theta are 7.36+ / -0.2, 14.61+ / -0.2, 17.01+ / -0.2, 21.91+ / -0.2 and 29.28+ / -0.2 sequentially. The preparation of the crystal comprises steps of mixing p-aminosalicylic acid and an organic solvent, then utilizing a temperature differential method for crystallization, carrying out solid-liquid separation, drying solid, and obtaining the crystal in the novel crystal form. The invention further relates to preparations or compositions containing the novel crystal form, and applications of the novel crystal form to preparations of drugs for treating tuberculosis. The novel crystal form of p-aminosalicylic acid is good in stability, and not only has storage and transportation advantages, but also greatly facilitates industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new crystal form of p-aminosalicylic acid used for treating tuberculosis and a preparation method thereof. Background technique [0002] Tuberculosis is a chronic infectious disease caused by Mycobacterium tuberculosis infection. The Chinese name of Mycobacterium tuberculosis is Mycobacterium tuberculosis (M.tuberculosis). The cell wall of Mycobacterium tuberculosis contains lipids, which can prevent the loss of water in the bacteria, so it is particularly resistant to drying. Adhesions remain infectious for 8-10 days on dust and 6-8 months in dried sputum. Mycobacterium tuberculosis can undergo variations in morphology, colony, virulence, immunogenicity, and drug resistance. At present, rifampicin, isoniazid, ethambutol, and streptomycin are mostly used as the first-line drugs in the treatment of tuberculosis. Combination of rifampicin and isoniazid can reduce drug resist...

Claims

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Application Information

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IPC IPC(8): C07C229/64C07C227/18A61K31/606A61P31/06
Inventor 邓青均刘德钦
Owner CHONGQING HUAPONT PHARMA
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