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Novel crystal form of tigecycline and preparation method thereof

A tigecycline and crystal form technology, applied in the field of drug crystal form, can solve the problems of uncomfortable drug preparation, solubility, hygroscopicity, poor stability, etc.

Active Publication Date: 2017-02-22
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the crystal forms disclosed in the existing literature have the problems of poor solubility, hygroscopicity, and stability, and are not suitable for the preparation of drugs.

Method used

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  • Novel crystal form of tigecycline and preparation method thereof
  • Novel crystal form of tigecycline and preparation method thereof
  • Novel crystal form of tigecycline and preparation method thereof

Examples

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Embodiment 2

[0029] The preparation of embodiment two tigecycline crystal forms

[0030] Add 23g of crude tigecycline to 115ml of dimethylformamide, stir to dissolve, add dropwise to 700ml of isopropyl ether, add 0.2g of seed crystals, cool to 0-5°C and stir for 2h after the dropwise addition, filter, Washed with isopropyl ether and dried under vacuum at 40°C to obtain 18.3 g of tigecycline crystal form.

Embodiment 3

[0031] The preparation of embodiment three tigecycline crystal forms

[0032] Add 17g of crude tigecycline to 85ml of dimethylacetamide, stir to dissolve, add dropwise to 500ml of butyl acetate, add 0.15g of seed crystals, cool to 0-5°C after dropwise addition, stir for 2h, filter, Washed with butyl acetate and dried under vacuum at 40°C to obtain 11.2 g of tigecycline crystal form.

Embodiment 4

[0033] The preparation of embodiment four tigecycline crystal forms

[0034] Add 21g of crude tigecycline into 105ml of N-methylpyrrolidone, stir to dissolve and add dropwise into 600ml of isopropyl ether, add 0.2g of seed crystals when about 10ml is added, and cool to 0-5°C after dropping Stir for 2 hours, filter, wash with isopropyl ether, and dry under vacuum at 40°C for 18 hours to obtain 13.5 g of tigecycline crystal form.

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Abstract

The invention relates to a novel crystal form of tigecycline and a preparation method thereof. An X-ray powder diffraction spectrum of the crystal form has a diffraction peak at the position of 2theta + / - 0.2 which is 3.9, 4.4, 7.8, 9.3, 12.8, 18.1, 20.4 and 23.8. The crystal form is stable in property, especially solvent residues all conform to the stipulations of pharmacopoeia, and security assurance is provided for marketed preparations.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms, and in particular relates to a new crystal form of tigecycline, a preparation method and application thereof. Background technique [0002] Tigecycline (Tigecycline, developed by Wyeth Drug Company of the United States) is a new type of broad-spectrum active intravenous antibiotic, which is also active against drug-resistant methicillin-resistant Staphylococcus aureus. first drug. Its chemical name is: (4S,4aS,5aR,12aS)-4,7-bis(dimethylamino)-9-[(tert-butylamino)acetamido]-3,10,12,12a-tetrahydroxy -1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide, the chemical structure is as follows: [0003] [0004] It has been found that tigecycline has multiple crystal form patents, mainly applied by Wyeth, Teva and Sandoz AG, and more than ten crystal forms are protected. Among them, Wyeth's patent CN101248038 protects five crystal forms of I~V . [0005] However,...

Claims

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Application Information

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IPC IPC(8): C07C237/26C07C231/24A61P31/04
Inventor 徐士伟乔智涛周炳城冯芮茂
Owner JIANGSU HANSOH PHARMA CO LTD
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