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Eutectic of Piperacillin sodium and Sulbactam sodium, preparation method thereof, pharmaceutical composition containing eutectic and application of pharmaceutical composition

A technology of piperacillin sodium and sulbactam sodium, which is applied in the field of co-crystallization of compound drugs, can solve the problems of short validity period and poor stability, and achieve the effects of constant antibacterial activity, low hygroscopicity, and avoiding large variations

Active Publication Date: 2014-12-24
XIANGBEI WELMAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystal can effectively solve the problems existing in the prior art such as poor stability and short validity period of the current compound preparation of piperacillin sodium and sulbactam sodium

Method used

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  • Eutectic of Piperacillin sodium and Sulbactam sodium, preparation method thereof, pharmaceutical composition containing eutectic and application of pharmaceutical composition
  • Eutectic of Piperacillin sodium and Sulbactam sodium, preparation method thereof, pharmaceutical composition containing eutectic and application of pharmaceutical composition
  • Eutectic of Piperacillin sodium and Sulbactam sodium, preparation method thereof, pharmaceutical composition containing eutectic and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Add 40g (0.074mol) of piperacillin sodium (calculated as salt) and 20g (0.078mol) of sulbactam sodium (calculated as salt) to a mixed solution of 40mL acetone+32mL DMF+12mL water (mixed solution 1) , then add 280mL of acetone (high-purity ketone 1), filter out the insoluble matter, let it stand at 5°C for 24 hours, filter out the generated crystals, and then mix with 72mL of acetone + 6.8mL of DMF + 2.4mL of water Solution (mixed solution 2) and 120mL acetone (high-purity ketone 2) wash the crystals filtered out after the above-mentioned standing to obtain white crystals, namely piperacillin sodium and sulbactam sodium cocrystal A, its X-ray powder diffraction Spectrum such as Figure 1-a (see Table 1 for the corresponding data, see the attached Figure 1-b ), its DSC spectrum is as image 3 As shown, its IR spectrum is the same as Figure 4 shown.

[0068] Table 1: X-ray powder diffraction data of cocrystal A

[0069]

[0070]

Embodiment 2

[0072] Add 400g (0.74mol) of piperacillin sodium (calculated as salt) and 179g (0.70mol) of sulbactam sodium (calculated as salt) to a mixed solution of 400mL acetone+300mL DMF+120mL water (mixed solution 1) , and then add 2800mL acetone (high-purity ketone 1), filter out the insoluble matter, let it stand at 5°C for 24 hours, filter out the generated crystals, and then successively use the mixed solution of 700mL acetone+60mL DMF+20mL water ( Mixed solution 2), and 1200mL acetone (high-purity ketone 2) wash the above-mentioned crystals filtered out after standing to obtain white crystals, namely piperacillin sodium and sulbactam sodium cocrystal A, its X-ray powder diffraction spectrum , DSC spectrum and IR spectrum are similar to Figures 1, 3 and 4 respectively, which can show that the cocrystal A is prepared.

Embodiment 3

[0074] Add 420g (0.78mol) of piperacillin sodium (calculated as salt) and 200g (0.78mol) of sulbactam sodium (calculated as salt) to a mixed solution of 500mL acetone+350mL DMF+120mL water (mixed solution 1) , and then add 3000mL acetone (high-purity ketone 1), after filtering out the insoluble matter, let it stand at 5°C for 24 hours, filter out the generated crystals, and then successively use the mixed solution of 800mL acetone+60mLDMF+20mL water (high Purity ketone 2), and 1400mL acetone (high-purity ketone 2) wash the crystals filtered out after the above-mentioned standing to obtain white crystals, namely piperacillin sodium and sulbactam sodium cocrystal A, its X-ray powder diffraction spectrum , DSC spectrum and IR spectrum are similar to Figures 1, 3 and 4 respectively, which can show that the cocrystal A is prepared.

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Abstract

The invention relates to an eutectic of Piperacillin sodium and Sulbactam sodium, a preparation method thereof, a pharmaceutical composition containing the eutectic and an application of the pharmaceutical composition on treating infection of super bacteria producing NDM-1 and other drug-resistance bacteria. The eutectic of the Piperacillin sodium and the Sulbactam sodium comprises diffraction angles of 14.24 DEG, 16.58 DEG, 16.79 DEG, 17.77 DEG, 19.20 DEG, 20.21 DEG, 20.39 DEG, 23.06 DEG, 27.86 DEG and 32.16 DEG represented by 2[theta] in an X-ray powder diffraction analysis spectra. The eutectic provided by the invention is excellent in solubility, low in hygroscopicity, relatively small in powder volume, high in purity, low in content of related substances, and easy to filter and dry during industrial production. A compound preparation prepared by the eutectic has obviously improved stability; not only is the shelf life of the products prolonged, but also the product safety is improved, thereby reducing potential adverse risks of the drugs and further protecting the health of patients.

Description

technical field [0001] The invention relates to the field of co-crystals of compound medicines, in particular to co-crystals of antibacterial drugs piperacillin sodium and sulbactam sodium and a preparation method thereof, and a drug combination comprising the co-crystals of piperacillin sodium and sulbactam sodium Drugs and their application in the treatment of NDM-1-producing "super bacteria" and other drug-resistant bacterial infections. Background technique [0002] NDM-1 is the English abbreviation of New Delhi metallo-β-lactamase-1 (New Delhi metallo-β-lactamase-1), an article published in the famous British medical journal "The Infectious Diseases" on August 11, 2010 as reported. Because the bacteria carrying this gene can produce a special β-lactamase, and the active part is a metal ion, it first appeared in New Delhi, the capital of India, so it is named: NDM-1. The bacteria producing NDM-1 are generally Escherichia coli and Klebsiella pneumoniae, which can cause ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D499/68C07D499/86C07D499/04A61K31/496A61K31/43A61P31/04
Inventor 不公告发明人
Owner XIANGBEI WELMAN PHARMA CO LTD
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