Oxiracetam compound and pharmaceutical composition thereof

A compound and composition technology, applied in the field of medicine, can solve the problems of reduced solubility, unstable structure, and decreased stability of preparations, and achieve the effect of less content and controllable quality

Active Publication Date: 2012-07-04
江西新先锋医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The molecular conformation of oxiracetam has two situations where the hydroxyl group and carbonyl group are located on the same side and the opposite side of the pyrrole ring. Due to the low lattice energy of oxiracetam, its structure is unstable. When the hydroxyl group and carbonyl group of oxiracetam are simultaneously When located on the same side of the pyrrole ring, under the influence of high temperature and light, it is easy to form intramolecular hydrogen bonds, which will cause the solubility and stability of oxiracetam preparations to decrease during long-term storage. Oxiracetam liquid dosage form will appear crystallization phenomenon, and the resolubility of oxiracetam solid dosage form becomes worse
The above patent does not solve the problem of poor stability of oxiracetam

Method used

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  • Oxiracetam compound and pharmaceutical composition thereof
  • Oxiracetam compound and pharmaceutical composition thereof
  • Oxiracetam compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Add 50g of oxiracetam, 600ml of N,N-dimethylformamide and 300ml of ethylene glycol into the liquid mixing tank, stir until they are completely dissolved, adjust the pH value of the liquid to 4.5 with triethylamine or acetic acid, and then add Activated carbon, stirred and adsorbed, decarburized by filtration with 0.45μm microporous membrane, and then sterilized with 0.2μm membrane for the first time and terminal sterilization filtration with 0.2μm membrane for the second time to obtain a clarified solution, and then the clarified solution was transferred to the pressure In the container, seal the pressure vessel, heat it in a water bath at 60-70°C, and adjust the pressure inside the pressure vessel to 1Mpa. Under this condition, slowly add 1800ml of isopropyl ether to produce a white precipitate, take out the mixture in the pressure vessel, and filter , washed with methanol and deionized water in sequence, and dried under reduced pressure for 3 hours to obtain the oxirac...

Embodiment 2

[0042] Add 50g of oxiracetam, 675ml of N,N-dimethylformamide and 225ml of ethylene glycol into the liquid mixing tank, stir until they are completely dissolved, adjust the pH value of the liquid to 5.0 with triethylamine or acetic acid, and then add Activated carbon, stirred and adsorbed, decarburized by filtration with 0.45μm microporous membrane, and then sterilized with 0.2μm membrane for the first time and terminal sterilization filtration with 0.2μm membrane for the second time to obtain a clarified solution, and then the clarified solution was transferred to the pressure In the container, seal the pressure vessel, heat it in a water bath at 60-70°C, and adjust the pressure in the pressure vessel to 1Mpa. Under this condition, slowly add 2700ml of isopropyl ether to produce a white precipitate, take out the mixture in the pressure vessel, and filter , washed with methanol and deionized water in sequence, and dried under reduced pressure for 3 hours to obtain the oxiracetam...

Embodiment 3

[0047] Using the oxiracetam compound prepared in Example 1 or 2 of the present invention and commercially available mannitol as raw materials, the prescription of the pharmaceutical composition in Table 1 is adopted:

[0048] Table 1

[0049]

[0050] A total of 1000 bottles were made

[0051] Preparation Process:

[0052] Under aseptic conditions, accurately weigh the oxiracetam compound and sterile mannitol according to the prescriptions of the first group to the fourth group in Table 1, and place the oxiracetam compound and sterile mannitol in a solid powder mixer After uniform mixing, the obtained raw materials are transferred to the aseptic preparation workshop, accurately measured and distributed into 1000 bottles, and capped to obtain the aseptic powder injection of the composition containing the oxiracetam compound.

[0053] Accurately weigh the oxiracetam compound and mannitol according to the prescription of the fifth group in Table 1, add 1500ml of water for in...

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Abstract

The invention relates to an oxiracetam compound, which has two crystal water molecules. In X-ray powder diffraction pattern obtained through Cu-Kalpha ray measurement, the characteristic peaks of the oxiracetam compound are shown in positions wherein 2theta is 17.3 degrees, 19.1 degrees, 21.6 degrees, 23.2 degrees, 27.0 degrees, 28.4 degrees, 30.0 degrees, 31.0 degrees, 31.7 degrees, 33.2 degrees, 36.9 degrees, 39.3 degrees, 40.2 degrees, 45.7 degrees and 51.2 degrees. The invention also relates to a preparation method of the oxiracetam compound, and a pharmaceutical composition containing the oxiracetam compound. The oxiracetam compound and the pharmaceutical composition thereof provided by the invention have the characteristic of high stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oxiracetam compound and a pharmaceutical composition thereof. Background technique [0002] Oxiracetam Molecular Formula C 6 h 10 N 2 o 3 , molecular weight 158.16, chemical name: 4-hydroxy-2-oxo-1-pyrrole acetamide, white microcrystalline powder obtained by crystallization from methanol, without crystal water, melting point 165~168℃. [0003] Oxiracetam is a new generation of drug for improving brain metabolism, which is a new type of pyrrolidone (cyclic GABOB) derivatives. Have good curative effect. Oxiracetam selectively acts on the cerebral cortex, stimulates specific neural pathways in the hippocampus, activates, protects and repairs brain nerve cells, but has no central sedative or exciting effect. Oxiracetam is safe and well tolerated by patients. [0004] Patent 02114302.1 discloses the prescription and preparation method of oxiracetam freeze-dried ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/273A61K31/4015
Inventor 夏智红
Owner 江西新先锋医药有限公司
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