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Dextro-oxiracetam sterile powder for injection and preparation method thereof

A technology for sterile powders and injections, which is applied in powder delivery, medical preparations containing no active ingredients, medical preparations containing active ingredients, etc. It can solve problems such as unfavorable drug safety, achieve good clarity and simple preparation process , good stability

Inactive Publication Date: 2019-10-29
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the research, the inventors found that the existing raw materials of Dexoxiracetam are easy to absorb moisture, and the relevant substances increase significantly during the storage process after being made into sterile powder, which is not conducive to drug safety

Method used

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  • Dextro-oxiracetam sterile powder for injection and preparation method thereof
  • Dextro-oxiracetam sterile powder for injection and preparation method thereof
  • Dextro-oxiracetam sterile powder for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Dissolve the commercially available dexoxiracetam in formic acid with a mass concentration of 85%, the weight ratio of formic acid to dexoxiracetam is 5:1, keep stirring at a stirring speed of 200r / min, and heat up to 95°C Insulate for 45 minutes, add activated carbon for decolorization, filter, adjust the pH value of the filtrate to 6.0 with 20% sodium hydroxide aqueous solution, concentrate to a supersaturated solution, crystallize at 2°C, filter with suction, collect the filter residue, and store at 30°C, relatively The humidity is 75% and dried for 4 hours.

[0020] Test instrument conditions: Bruker D2 PHASER powder diffractometer is used for normal temperature test, the test conditions are: Cu Ka It is the light source, the voltage is 30kV, the current is 10mA, the test step is 0.014°, the scanning speed is 0.1s / step, and the scanning range is 5-40° (2θ). After testing, the D-oxiracetam crystal prepared in Example 1 has diffraction angles 2θ of 10.54±0.2°, 13.76...

Embodiment 2

[0024] Dissolve 10 g of commercially available Dexoxiracetam in 40 mL of 82% formic acid (w / w), raise the temperature to 90°C and keep it warm for 50 min, then add 0.01 g of activated carbon for decolorization, filter while it is hot, and add 10% hydrogen to the filtrate after it is cooled to room temperature Sodium oxide aqueous solution (w / w) adjusted the pH to 5.5, concentrated into a supersaturated solution, crystallized at 0°C, filtered with suction, collected the filter residue, dried at 35°C for 4 hours at a relative humidity of 85%, and obtained 8.0 g of Oxiracetam crystals. The determination method in Example 1 is used to detect that the crystalline compound of Dexoxiracetam prepared in Example 2 is the same crystal form of Dexoxiracetam in Example 1.

Embodiment 3

[0026] Dissolve 10 g of commercially available Dexoxiracetam in 50 mL of 89% formic acid (w / w), raise the temperature to 110°C and keep it warm for 30 min, then add 0.02 g of activated carbon for decolorization, filter while it is hot, and add 20% hydrogen after cooling the filtrate to room temperature Sodium oxide aqueous solution (w / w) adjusted the pH to 6.5, concentrated into a supersaturated solution, crystallized at 5°C, filtered with suction, collected the filter residue, dried at 25°C for 3 hours at a relative humidity of 70%, and obtained 8.5g Oxiracetam crystals. The assay method in Example 1 was used to detect that the crystalline dexoxiracetam compound prepared in Example 3 was the same crystal form of Dexoxiracetam as in Example 1.

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Abstract

The invention provides dextro-oxiracetam sterile powder for injection. The dextro-oxiracetam sterile powder is prepared from dextro-oxiracetam in a crystal form and L-arginine in a specific proportion, wherein the dextro-oxiracetam has diffraction peaks when the reflection angle 2*theta is 10.54+ / -0.2 degrees, 13.76+ / -0.2 degrees, 14.14+ / -0.2 degrees, 16.64+ / -0.2 degrees, 17.76+ / -0.2 degrees, 18.72+ / -0.2 degrees, 20.16+ / -0.2 degrees, 21.20+ / -0.2 degrees, 21.52+ / -0.2 degrees, 23.25+ / -0.2 degrees, 24.17+ / -0.2 degrees, 25.88+ / -0.2 degrees, 27.61+ / -0.2 degrees, 28.57+ / -0.2 degrees, 29.24+ / -0.2 degrees and 31.40+ / -0.2 degrees; and hygroscopicity is low, stability is good, and the quality of the dextro-oxiracetam sterile powder is kept advantageously. Under the commercially available back condition, the dextro-oxiracetam sterile powder is subjected to an acceleration test for 6 months at 35+ / -5 DEG C and subjected to a long-term test for 12 months at the room temperature to be investigated,all indexes are not changed remarkably and are within the range prescribed by the quality standard, and the stability is good; and a preparation process is simple, short in operation time, high in production efficiency and suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation of dexoxiracetam, in particular to a sterile powder of dexoxiracetam for injection and a preparation method thereof. Background technique [0002] Oxiracetam, whose chemical name is 4-hydroxy-2-oxo-1-pyrrolidineacetamide, was first developed and synthesized by the Italian ISF S.P.A company in 1974, and was first listed in Italy in 1987. Clinically, it is widely used in mild to moderate vascular dementia, senile dementia, various cerebrovascular diseases, brain injury, intracranial infection and other diseases, with definite curative effect and good safety. Studies have shown that the chiral isomer of oxiracetam, D-oxiracetam, has good anti-epileptic activity, especially as a drug for the treatment of epileptic generalized seizures, partial epileptic seizures and status epilepticus. , is expected to be developed into a new type of low toxicity antiepileptic drug. As we all know, in the clinical treatment of epile...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/18A61K31/4015A61P25/28C07D207/273
CPCA61K9/0019A61K9/145A61K31/4015A61P25/28C07D207/273
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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