Dextro-oxiracetam dispersible tablet and preparation method thereof

A technology of dispersible tablets and mass percentage, applied in the field of dextro-oxiracetam dispersible tablets and its preparation, which can solve the problems of easily decomposed impurities, large differences in tablet weight, and poor powder fluidity

Inactive Publication Date: 2019-11-01
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the problems of dexoxiracetam’s strong hygroscopicity, poor fluidity, large difference in tablet weight, and easy decomposition to produce impurities, the powder direct compression method has disadvantages such as poor powder fluidity, large difference in tablet weight, and easy cracking caused by powder compression. , the present inventor has screened the types and dosages of active ingredients and auxiliary materials through a large number of experimental studies, so that the prepared mixture has good fluidity, compressibility and lubricity, and can meet the requirements of direct tableting. At the same time shorten the production cycle, improve the degree of industrial automation, greatly improve labor productivity, reduce production costs, reduce factors of unstable quality in the process of pharmaceutical processing, and ensure product quality

Method used

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  • Dextro-oxiracetam dispersible tablet and preparation method thereof
  • Dextro-oxiracetam dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Dissolve the amorphous Dexoxiracetam at 25mg / mL with sec-butanol and heat and stir, cover and seal, stir at 35°C at a speed of 200r / min for 24h, filter, let the filtrate stand for volatilization and crystallization, and collect the crystals , dried at a temperature of 60° C. and a relative humidity of 20% for 6 hours, and collected crystals. The obtained dextro-oxiracetam crystal is subjected to powder diffraction experiment: powder diffraction determination (XRPD): test instrument condition: use Bruker D2 PHASER powder diffractometer to carry out normal temperature test, test condition is: 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 prepared D-oxiracetam crystals have diffraction angles 2θ of 12.6±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...

Embodiment 2

[0023] Dissolve the amorphous Dexoxiracetam at 10mg / mL with sec-butanol, cover and seal, stir at 40°C for 20h at a speed of 300r / min, filter, let the filtrate stand for volatilization and crystallization, collect the crystals, Dry at a temperature of 50° C. and a relative humidity of 35% for 8 hours to collect crystals. As determined by powder diffraction, the crystalline form of dexoxiracetam prepared in Example 2 is the same as the crystalline form of dexoxiracetam prepared in Example 1.

Embodiment 3

[0025] Heat and stir the amorphous dexoxiracetam at 50 mg / mL with sec-butanol to dissolve, cover and seal, stir at 25°C at a speed of 100r / min for 20h, filter, let the filtrate stand for volatilization and crystallization, and collect the crystals , dried at a temperature of 70° C. and a relative humidity of 15% for 5 hours, and collected crystals. As determined by powder diffraction, the crystalline form of dexoxiracetam prepared in Example 3 is the same as the crystalline form of dexoxiracetam prepared in Example 1.

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Abstract

The invention provides a dextro-oxiracetam dispersible tablet. By taking dextro-oxiracetam in a specific crystalline form as an active component and through direct tabletting of powder, the dextro-oxiracetam dispersible tablet is prepared, a mixed material has good flowability, compressibility and lubricity, the hardness of the dispersible tablet is 5-9 kgf, and the disintegration time is less than 1 min; and in a phosphate buffer solution with pH being 6.8, 80% or above of the dextro-oxiracetam dissolves out within ten minutes, and the dissolution rate within 20 min is 95% or above. The preparation process of the dextro-oxiracetam dispersible tablet is simple, easy to control, convenient to operate and suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation of dexoxiracetam, in particular to a dispersible tablet of dexoxiracetam 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 company ISF S.P.A. It is widely used clinically for mild to moderate vascular dementia, elderly Dementia and various cerebrovascular diseases, brain injury, intracranial infection and other diseases, the curative effect is definite, and the safety is good. 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. Chinese patent CN101766596A discloses a solid preparation with Dexoxiracetam as an active ing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4015A61P25/08A61P25/28A61P9/10A61P25/00A61P31/00C07D207/273
CPCA61K9/0056A61K9/205A61K9/2054A61K9/2095A61K31/4015A61P9/10A61P25/00A61P25/08A61P25/28A61P31/00C07B2200/13C07D207/273
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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