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Oxiracetam compound with steady crystal form

A compound and crystal technology, applied in the field of medicine, can solve the problems of oxiracetam's poor stability, material content preference, and influence on use, and achieve the effects of reducing side reactions, low content of related substances, and high yield

Active Publication Date: 2013-11-06
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The poor stability of oxiracetam, especially its strong hygroscopicity, affects its use, so it is made into pharmaceutically acceptable salts, such as sodium salt, hydrochloride, nitrate, tartrate, fumarate acid, mucate, etc., but there are still some defects
[0014] In the existing preparation method of oxiracetam, the crystallization process during refining is only to dissolve the crude product of oxiracetam and then filter it and cool it directly. The lack of fine filtration, crystal growth and other steps lead to the preference of related substance content and low yield of the product

Method used

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  • Oxiracetam compound with steady crystal form
  • Oxiracetam compound with steady crystal form
  • Oxiracetam compound with steady crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Add the crude oxiracetam to 99% methanol, heat to 75°C to dissolve it, add activated carbon for 30 minutes, filter while it is hot, continue to pass the filtrate through a 0.45um microporous membrane, collect the filtrate, and then Continue to heat up the filtrate to 75°C, slowly cool down to about 40°C, control the temperature at 38-42°C for 2.5 hours, keep the crystal for 2.5 hours, then continue to cool down to 4-10°C for 2.5 hours, then slowly cool down, cool and crystallize, and finally collect the crystals , Yield: 92.1%, content 100.2%.

Embodiment 2

[0058] Add the crude oxiracetam to 80% methanol, heat to 80°C to dissolve it, add activated carbon for 30 minutes, filter while it is hot, continue to pass the filtrate through a 0.45um microporous membrane, collect the filtrate, and then Continue to heat up the filtrate to 80°C, slowly cool down to about 40°C, control the temperature at 38-42°C for 3 hours, keep the crystal for 3 hours, then continue to cool down to 4-10°C for 3 hours, then slowly cool down, cool and crystallize, and finally collect the crystals , Yield: 91.8%, content 100.1%.

Embodiment 3

[0060] Add the crude oxiracetam to 95% methanol, heat it to 65°C to dissolve it, add activated carbon for 30 minutes, filter while it is hot, continue to pass the filtrate through a 0.45um microporous membrane, collect the filtrate, and then Continue to heat up the filtrate to 65°C, slowly cool down to about 40°C, control the temperature at 38-42°C for 2 hours, keep the crystal for 2 hours, then continue to cool down to 4-10°C for 3 hours, then slowly cool down, cool and crystallize, and finally collect the crystals , Yield: 91.1%, content 100.0%.

[0061] The oxiracetam compound obtained by the present invention has high purity, high yield, and low impurity content, which effectively improves the therapeutic effect of the product and reduces side reactions; meanwhile, the yield is improved, the cost is reduced, and higher benefits are created .

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to an oxiracetam compound. The oxiracetam compound provided by the invention contains semi-crystalline water. The oxiracetam compound has the advantages that related substances are small, the purity is high, the stability is good, and a moisture-absorption and weight-gaining effect is not obvious even if under a high humidity condition.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oxiracetam compound and a preparation method thereof. Background technique [0002] Generic name: Oxiracetam; [0003] English name: Esomeprazole Sodium; [0004] Chemical name: 4-hydroxy-2-oxo-1-pyrrolidineacetamide; [0005] Its structural formula is as follows: [0006] [0007] Molecular formula: C 6 h 10 N 2 o 3 ; [0008] Molecular weight: 158.16; [0009] Indications: It is used for the treatment of brain injury and the resulting neurological function loss, memory and intellectual impairment. [0010] Type of pharmacological action: Oxiracetam is a cholinergic nootropic drug acting on the central reticular structure. [0011] Pharmacological mechanism: Oxiracetam can promote the synthesis of phosphorylcholine and phosphorylethanolamine, increase the ratio of ATP / ADP in the brain, and increase the synthesis of protein and nucleic acid in the bra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/273
Inventor 严洁黄欣
Owner TIANJIN HANKANG PHARMA BIOTECH
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