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Freeze-dried composition containing dextrorotation oxiracetam 1/2 aquo-complex and preparation method of freeze-dried composition

A composition and freeze-drying technology, applied in the directions of drug combinations, medical preparations containing active ingredients, freeze-dried delivery, etc., can solve the problems of short validity period of drugs, accelerated water degradation, and increase of related substances, and achieve long freeze-drying time. , The effect of smooth water vapor circulation and low moisture absorption

Inactive Publication Date: 2019-10-11
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In fact, the stability of Dexoxiracetam is greatly affected by the water content and hygroscopicity of the product. The test results on the factors affecting the raw material drug show that the weight gain of the product is very obvious under the relative humidity of 75%. , under the influence of moisture, the degradation of moisture is accelerated, resulting in a decrease in content and an increase in related substances
During the research process, it was found that the prepared dexoxiracetam freeze-dried injection was prone to spray bottle, bottle sticking phenomenon, hole filling, umbrella shape and other bad shapes and poor stability when drying, and the drug had a short validity period.

Method used

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  • Freeze-dried composition containing dextrorotation oxiracetam 1/2 aquo-complex and preparation method of freeze-dried composition
  • Freeze-dried composition containing dextrorotation oxiracetam 1/2 aquo-complex and preparation method of freeze-dried composition
  • Freeze-dried composition containing dextrorotation oxiracetam 1/2 aquo-complex and preparation method of freeze-dried composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dexoxiracetam was dissolved in a mixed solvent (volume ratio isopropanol:ethyl acetate=1:1), wherein the mass volume ratio (g / mL) of dexoxiracetam to the mixed solvent was 1: 5. Filtrate, cover and seal the filtrate, stir at a speed of 100-150r / min for 15h, filter again, after filtration, let the filtrate stand in a desiccator to evaporate the solvent to form crystals, collect the crystals, and store the collected crystals at 25°C, relatively The humidity is 70-75% under the condition of drying 4h, vested.

[0028] Elemental analysis, determined that the crystal molecular formula is C 6 h 10 N 2 o 3 0.5H 2 O. The moisture in the Dexoxiracetam compound of the present invention was measured by Karl Fischer method to be 5.53% (theory: 5.52%).

[0029] Differential scanning thermal analysis (DSC) chart determination:

[0030]Test equipment and conditions: DSC test adopts NETZSCH DSC200PC tester. The test method is to accurately weigh a certain amount (1 ~ 2mg) of the...

Embodiment 2

[0032] Dissolve dexoxiracetam in a mixed solvent (volume ratio isopropanol:petroleum ether=1:3), wherein the mass volume ratio (g / mL) of dexoxiracetam to the mixed solvent is 1:3 , filter, seal the filtrate with a cover, stir at a speed of 100-150r / min for 20h, and filter again. After filtration, the filtrate is left in a desiccator to evaporate the solvent to form crystals, collect the crystals, and store the collected crystals at 20 ° C, relative humidity Drying for 6h under the condition of 60-65%, vested.

[0033] Elemental analysis, determined that the crystal molecular formula is C 6 h 10 N 2 o 3 0.5H 2 O. The moisture in the Dexoxiracetam compound of the present invention was measured to be 5.58% (theory: 5.52%) by the Karl Fischer method.

Embodiment 3

[0036] prescription

[0037]

[0038] Preparation:

[0039] Take 400ml of boiled water for injection, add the prescribed amount of calcium sodium edetate and mannitol, stir to dissolve, add the prescribed amount of Dexoxiracetam 1 / 2 hydrate and stir to dissolve, and add 0.1M diphosphate diphosphate Adjust the pH value of the sodium hydrogen solution to 5.0, add 0.2% activated carbon for needles according to the prepared amount, heat the liquid medicine to about 55°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.

[0040] Freeze-drying process:

[0041] Pre-freezing stage: lower the temperature of the shelf to -45°C, quickly put the product in, and when the temperature of the product reaches -35±2°C, continue to keep warm for 4 hours, and keep the vacuum in the box at 10±2Pa;

[0042] Primary drying stage: keep the vacuum degree in the ...

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Abstract

The invention provides a freeze-dried composition containing a dextrorotation oxiracetam 1 / 2 aquo-complex. The molecular formula of the dextrorotation oxiracetam 1 / 2 aquo-complex is C6H10N2O3.0.5H2O,the water content is 5.41-5.63%, loss of crystal water is caused at 72.9+ / -2 DEG C, and melting decomposition is conducted at 137.5+ / -2 DEG C. The prepared dextrorotation oxiracetam freeze-dried powerinjection is low in hygroscopicity and good in stability, the freeze-dried aquatic product is good in dissolubility, before freezing, the appearance of a solution is clear, and the freeze-dried powerinjection is good in clarity, low in impurity content, good in stability and controllable in quality. According to the freeze-dried composition containing the dextrorotation oxiracetam 1 / 2 aquo-complex, in the freeze-drying process, vapor circulation is smooth, it can be avoided that during drying, the phenomena of violent spraying into a bottle and attachment to the bottle are caused, and undesirable shapes such as a pore shape and an umbrella shape are formed, and the rate of finished products is increased.

Description

technical field [0001] The present invention relates to a dexoxiracetam pharmaceutical composition, in particular to a freeze-dried composition containing dexoxiracetam 1 / 2 hydrate 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 as a nootropic drug. 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 d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/26A61P25/08A61P25/28C07D207/273
CPCA61K9/0019A61K9/19A61K31/4015A61K47/26A61P25/08A61P25/28C07B2200/07C07B2200/13C07D207/273
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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