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Dextrooracetam freeze-dried powder injection with good stability and preparation method thereof

A technology of freeze-dried powder injection and freeze-dried excipients, which is applied in the field of dexoxiracetam preparations, can solve the problems of unstable quality, high related substances, and high water content of freeze-dried preparations, and achieve good clarity, Good resolubility, considerable economic and social benefits

Inactive Publication Date: 2019-10-15
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the process of studying the freeze-dried preparation of Dexoxiracetam, the inventor found that the freeze-dried preparation obtained by the conventional preparation process has high water content, high related substances, and unstable quality

Method used

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  • Dextrooracetam freeze-dried powder injection with good stability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029]Purification of Dexoxiracetam: In 150mL of methanol, add 10g of Dexoxiracetam, stir continuously, heat to 50°C, dissolve completely, add 0.5g of activated carbon and stir for 30 minutes at a speed of 250r / min, filter , to obtain a methanol solution, the methanol solution was concentrated to a total volume of 20ml to obtain a saturated methanol solution, adding 30ml of ethanol, stirring and crystallizing at a speed of 250r / min in a 5°C environment, and filtering to obtain colorless sandy crystals. Dry at -70°C for 4-5 hours at a relative humidity of 20-25%, and collect crystals.

[0030] Powder Diffraction Determination (XRPD): Test Instrument Conditions: Use Bruker D2PHASER powder diffractometer to carry out normal temperature test, test conditions are: with 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 X-ray powder diffraction sp...

Embodiment 2

[0033] Prescription: Dexoxiracetam (200g), 0.1M sodium dihydrogen phosphate (appropriate amount), calcium sodium edetate (300mg), aspartic acid (50g), mannitol (100g), water for injection to 1000ml. Preparation method: Take 800ml of water for injection, add the prescription amount of aspartic acid, mannitol and calcium sodium edetate, stir to dissolve, add the prescription amount of dexoxiracetam and stir to dissolve, and use 0.1M diphosphate Adjust the pH value of the sodium hydrogen solution to 5.2, add 0.1% activated carbon for needles according to the prepared amount, heat the liquid medicine to about 48°C, stir for 30 minutes, filter and decarbonize, add water for injection to the total amount, and then use a 0.22 μm microporous filter membrane Fine filtration, filling, half stoppering.

[0034] Freeze-drying process: divided into three stages: pre-freezing, sublimation drying and desorption drying. In the pre-freezing stage: the temperature of the shelf is reduced to -5...

Embodiment 3

[0036] Prescription: Dexoxiracetam (100g), appropriate amount of 0.1M sodium dihydrogen phosphate, disodium edetate (200mg), arginine (100g), and add water for injection to 1000ml.

[0037] Preparation method: Take 700ml of water for injection, add the prescribed amount of arginine and edetate disodium, stir to dissolve, add the prescribed amount of Dexoxiracetam and stir to dissolve, adjust with 0.1M sodium dihydrogen phosphate solution pH value is 6.0, add 0.2% activated carbon for injection according to the prepared amount, heat the liquid medicine to about 45°C, stir for 25 minutes, filter and decarbonize, add water for injection to the total amount, and then use a 0.22μm microporous filter membrane for fine filtration, pour Pack, half stoppered.

[0038] Freeze-drying process: Freeze-drying is divided into three stages: pre-freezing, sublimation drying and desorption drying. In the pre-freezing stage: the temperature of the shelf is reduced to -50°C, and the product is qu...

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Abstract

The invention provides a dextrooracetam freeze-dried powder injection with good stability; the dextrooracetam freeze-dried powder injection is prepared by freeze-drying a solution prepared from crystalline-form dextrooracetam, a freeze-dried excipient, a metal ion chelating agent, a pH regulator and water for injection. The obtained freeze-dried powder injection sample has no obvious change in properties, related substances and content under the conditions of high humidity and high temperature through the investigation of influencing factors under the conditions of commercially available packaging, so as to indicate that the freeze-dried powder injection is relatively stable and can effectively prevent moisture. The preparation method is simple and suitable for industrial mass production.

Description

technical field [0001] The invention relates to a dexoxiracetam preparation, in particular to a stable dexoxiracetam freeze-dried powder injection and a preparation method thereof. Background technique [0002] Oxiracetam is a new generation of brain metabolism improving drug first synthesized in 1974 by the Italian Skelebechem Company and launched in 1987. It can promote learning, enhance memory, and protect damaged nerve cells. Clinically, oxiracetam is most commonly used to improve a variety of cognitive dysfunction, such as post-anesthesia cognitive dysfunction (POCD) in elderly patients, neurological deficits secondary to brain injury in neurosurgery patients, and undamaged brain tissue in epilepsy patients. Reconstruction and restoration of neurological function, intellectual impairment caused by mild and moderate Alzheimer's disease, and improvement of brain function in children with cerebral palsy. In addition, oxiracetam is also used in the treatment of vascular de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/26A61K47/18A61K47/42A61K31/4015A61P25/28A61P25/08C07D207/273
CPCA61K9/0019A61K9/19A61K31/4015A61K47/183A61K47/26A61K47/42A61P25/08A61P25/28C07D207/273
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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