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Dextrohydroxypyramide enteric-coated granules and preparation method thereof

A technology of dextropyridine and granules, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of reduced drug absorption, unstable pharmacological effects, Increased drug safety risks and other issues

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

Due to the instability of dexoxypyramide in the stomach, with the prolongation of the drug residence time in the stomach, the amount of drug decomposed by gastric acid gradually increases, resulting in a decrease in the effective absorption of drug in the intestinal tract, resulting in unstable pharmacological effects. Increased drug safety risk

Method used

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  • Dextrohydroxypyramide enteric-coated granules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Stir and dissolve 30mg / mL of dextropyridine with ethyl acetate, cover and seal, stir at a temperature of 20-25°C at a speed of 200-250r / min for 24-25h, filter, and let the filtrate stand for volatilization Crystallization, collecting crystals, drying at a temperature of 70-75° C. and a relative humidity of 20-25% for 4-5 hours, and collecting crystals. Carry out powder diffraction measurement (XRPD) to the crystallization that collects: Test instrument condition: use Bruker D2PHASER powder diffractometer to carry out normal temperature test, test condition is: with CuKa 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 diffraction angle 2θ is 12.6±0.2°, 14.04±0.2°, 15.1±0.2°, 16.66±0.2°, 17.54±0.2°, 19.42±0.2°, 20.68±0.2°, 21±0.2°, 22.16± There are diffraction peaks at 0.2°, 23.46±0.2°, 25.36±0.2°, 26.08±0.2°, 26.5±0.2°, 30.26±0.2°, 30.46±...

Embodiment 2

[0023] Stir and dissolve dextrooxypyridine at 70mg / mL with ethyl acetate, cover and seal, stir at a temperature of 12-15°C at a speed of 200-250r / min for 20-30h, filter, and let the filtrate stand for volatilization Crystallization, collecting crystals, drying at a temperature of 55-60° C. and a relative humidity of 10-20% for 3-4 hours, and collecting crystals. The test was carried out with reference to the method of Example 1, and the results showed that the dextrooxypyridine crystals prepared in Example 2 had the same crystal form as that in Example 1.

Embodiment 3

[0025]Stir and dissolve 21 mg / mL of dextrooxypyridamine with ethyl acetate, cover and seal, stir at a temperature of 25-30°C at a speed of 150-200r / min for 22-25h, filter, and let the filtrate stand for volatilization Crystallization, collecting crystals, drying at a temperature of 65-70° C. and a relative humidity of 15-20% for 4-5 hours, and collecting crystals. The test was carried out with reference to the method of Example 1, and the results showed that the dextrooxypyridine crystals prepared in Example 3 had the same crystal form as that in Example 1.

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Abstract

The invention provides dextrohydroxypyramide enteric-coated granules. A specific crystalline form of dextrohydroxypyramide is used as an active ingredient and supplemented with a specific proportion of auxiliary materials such as pregelatinized starch, sodium alginate and cellulose acetate phthalate, the dextrohydroxypyramide granules are prepared by a fluidized bed granulation method, the dextrohydroxypyramide granules are less soluble in the stomach, and mainly disintegrated and released in intestinal fluid, and the side effects caused by decomposition of drugs by gastric acid due to the dissolution of dextrohydroxypyramide in the stomach are reduced. The dextrohydroxypyramide enteric-coated granules are simple in preparation method and suitable for industrial production.

Description

technical field [0001] The invention relates to a dextrooxypyridine preparation, in particular to a dextroroxypyridine granule and a preparation method thereof. Background technique [0002] Hydroxypyramide is a new central nervous system drug launched in 1987, which can promote learning, enhance memory, and protect damaged nerve cells. Clinically, oxypyramide 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 neurosurgical patients, and undamaged brain in epilepsy patients. Tissue reconstruction and recovery of nerve function, intellectual impairment caused by mild and moderate Alzheimer's disease, and improvement of brain function in children with cerebral palsy. In addition, oxypyramide is also used in the treatment of vascular dementia and acute cerebral infarction. Studies have shown that the dextrorotatory form of oxypyridine ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/36A61K31/4015A61P25/08
CPCA61K9/1652A61K31/4015A61P25/08
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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