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Novel crystal formations of levogyration oxiracetam and preparation method thereof

A technology of crystal form and crystallization temperature, applied in the field of new crystal form of levoxiracetam, preparation method and pharmaceutical composition

Active Publication Date: 2012-08-01
南京斯帕克医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is a huge market demand for oxiracetam, but it has been disclosed that there are certain stability problems in the compounds, so it is necessary to develop a more stable new crystal form of oxiracetam

Method used

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  • Novel crystal formations of levogyration oxiracetam and preparation method thereof
  • Novel crystal formations of levogyration oxiracetam and preparation method thereof
  • Novel crystal formations of levogyration oxiracetam and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Preparation of Levoxiracetam

[0032] According to the method disclosed in TETRAHEDRON: ASYMMETRY 1992, 3(11), 1431-40, 503.0 g of levoxiracetam was prepared, and the HPLC purity was 99.1%.

[0033] Example 2: Preparation of L-Oxiracetam crystal form A

[0034] 10.0 g of S-oxiracetam was prepared from Example 1, heated with methanol to dissolve it completely, and concentrated to dryness under reduced pressure to obtain crystal form A of levoxiracetam.

[0035] Example 3 Preparation of L-Oxiracetam crystal form A

[0036] take Example 1 10.0 g of Levoxiracetam was prepared, which was completely dissolved by heating with isopropanol, and concentrated to dryness under reduced pressure to obtain crystal form A of Levoxiracetam.

[0037] Example 4 Preparation of L-Oxiracetam crystal form A

[0038] take Example 1 15.0 g of Levoxiracetam was obtained, which was completely dissolved by heating with DMF, and concentrated to dryness under reduced pressure to obtain crystal f...

Embodiment 7

[0043] Example 7 Preparation of L-Oxiracetam crystal form B

[0044] take Example 1 Prepare 50.0g of L-Oxiracetam, dissolve it by heating with a mixed solvent of n-butanol and water (volume ratio 15:1), then cool to 20℃, stir to crystallize, filter with suction, and finally vacuum at 45~55℃ After drying, 40.5 g of L-Oxiracetam crystal form B was obtained with a yield of 81.0%.

Embodiment 8

[0045] Example 8 Preparation of L-Oxiracetam crystal form B

[0046] take Example 1 Prepare 50.0 g of levoxiracetam, dissolve it by heating with a mixed solvent of DMF and water (10:1 by volume), then cool to 35°C, stir to crystallize, filter with suction, and finally vacuum dry at 45-55°C. 36.2g of L-Oxiracetam crystal form B was obtained with a yield of 72.4%.

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PUM

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Abstract

The invention relates to novel crystal formations of levogyration oxiracetam, including a crystal formation A, a crystal formation B and a crystal formation C, which have excellent stability and are very suitable for the preparation of common formulations of levogyration oxiracetam. The invention further discloses a preparation method and characterization of the crystal formations, as well as a pharmaceutical composition containing the crystal formations.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical technology, in particular to a new crystal form, preparation method and pharmaceutical composition of L-Oxiracetam. Background technique [0002] Oxiracetam (CAS No.: 62613-82-5) is chemically named 4-hydroxy-2-oxo-1-pyrrolidine acetamide. It is an anti-deficiency compound first synthesized by ISFS.PA in Italy in 1974. Oxygen nootropics (compounds disclosed in US4118396) are cyclic GABOB derivatives, which can promote the synthesis of phosphorylcholine and phosphorylethanolamine, promote brain metabolism, penetrate the blood-brain barrier, and stimulate specific central nervous pathways. It can improve intelligence and memory, and has a good effect on cerebrovascular diseases, brain trauma, brain tumors, intracranial infections, brain degenerative diseases, etc., and the drug has extremely low toxicity, no mutagenic, carcinogenic effects and reproductive toxicity. [0003] [0004] Giorgio et al. d...

Claims

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Application Information

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IPC IPC(8): C07D207/273A61K31/4015A61P25/00
Inventor 车晓明李上花耀高曹卫晁阳叶海
Owner 南京斯帕克医药科技有限公司
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