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Orm C of avibactam sodium

一种阿维巴坦钠、晶型的技术，应用在阿维巴坦钠的晶型C及其制备领域

Active Publication Date: 2018-04-17
SANDOZ LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, reliable industrial production of the anhydrous form B appears to be very challenging

Method used

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  • Orm C of avibactam sodium
  • Orm C of avibactam sodium
  • Orm C of avibactam sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0177] Example 1: Form C of Avibactam Sodium

[0178] Sodium avibactam (160 mg, for example the crystal form D prepared according to Example 5 of WO 2011 / 042560 A1) was dissolved in 2 mL of water. To this solution was added 3 mL of isobutanol, and the biphasic mixture was heated to a bath temperature of 119° C. to remove water azeotropically. After removal of water, precipitation occurred. The suspension was allowed to cool to room temperature and the solid was collected by filtration and blotted dry on the filter.

[0179] Yield: 98 mg (61% of theoretical value), DSC (10K / min): exothermic, initial temperature is 227 ° C,

[0180] TGA (10K / min): 0.5% mass change by weight from about 25 to 200°C

[0181] The powder X-ray diffraction pattern of the obtained material is as figure 1 As shown, the reflection list is shown in Table 1.

[0182]

[0183] Table 1: List of reflections and corresponding relative intensities for Form C at 2.0 to 30.0° 2-theta

[0184] The obtaine...

Embodiment 2

[0187] Example 2: Form C of Avibactam Sodium

[0188] Avibactam sodium (164 mg, crystal form D, prepared for example according to Example 5 of WO 2011 / 042560 A1) was dissolved in 2 mL of water. To this solution was added 3 mL of 2-butanol, and the biphasic mixture was heated to a bath temperature of 135° C. to remove water azeotropically. Precipitation occurs after removal of water. The suspension was allowed to cool to room temperature and the solid was collected by filtration and blotted dry on the filter. Powder X-ray diffraction confirmed Form C.

[0189] Yield: 102 mg (62% of theory),

Embodiment 3

[0190] Example 3: Stress Test

[0191] Form C (prepared according to Example 1 herein) was stored in a desiccator at room temperature with an open opening, and different relative humidity was generated in a saturated saline solution. The samples were analyzed by powder X-ray diffraction and the results are summarized in Table 2 below:

[0192]

[0193]

[0194] Table 3: Summary of stress tests performed with Form C as starting material

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PUM

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Abstract

The present invention relates to crystalline form C of avibactam sodium and to a process for its preparation. The invention also concerns a pharmaceutical composition comprising form C and one or moreantibacterial agents, wherein at least one antibacterial agent is a beta-lactam antibiotic. The pharmaceutical composition of the present invention can be used as medicament, in particular for treatment and / or prevention of bacterial infections.

Description

technical field [0001] The invention relates to crystal form C of avibactam sodium (avibactam sodium) and a preparation method thereof. The present invention also relates to a pharmaceutical composition comprising Form C and one or more antibacterial agents, wherein at least one antibacterial agent is a beta-lactam antibiotic. The pharmaceutical composition of the invention can be used as a medicament, especially for the treatment and / or prevention of bacterial infections. Background of the invention [0002] Avibactam sodium belongs to the class of non-β-lactam β-lactamase inhibitors and is intended to be used in combination with β-lactam antibiotics for the treatment of bacterial infections. It protects β-lactam antibiotics from degradation by β-lactamase, thus maintaining the antibacterial activity of β-lactam antibiotics. [0003] WO 02 / 10172 A1 describes the racemic sodium salt of trans-7-oxo-6-sulfoxy-1,6-diazabicyclo[3.2.1]octane-2-carboxamide in crystalline form a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A01N43/90
CPCC07D471/04A61K31/439A61P31/04A61K31/551B01D9/0054
Inventor A·霍特V·阿达梅尔H·伦加尔
Owner SANDOZ LTD
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