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S-oxiracetam-containing orally disintegrating tablets and preparation method thereof

A technology of orally disintegrating tablets and disintegrants, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, and pill delivery, which can solve problems such as difficulty in obtaining uniformly mixed granules, unfavorable preparation production, and increased difficulty in granulation , to achieve the effect of ensuring production compliance, cheap auxiliary materials, and low cost

Inactive Publication Date: 2018-05-25
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When repeating the patent, it was found that due to the excellent water solubility and strong hygroscopicity of levo-oxiracetam, the material is easy to agglomerate during the wet granulation process, and most of the material sticks to the wall of the granulation pot, resulting in uneven particles. It increases the difficulty of granulation, it is difficult to obtain granules with uniform mixing and narrow particle size distribution, and the compressibility is poor, which is not conducive to the production of preparations

Method used

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  • S-oxiracetam-containing orally disintegrating tablets and preparation method thereof
  • S-oxiracetam-containing orally disintegrating tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] (1), preparation of solid dispersion

[0050] Dissolve 1 part of levoxiracetam and 1-8 parts of succinic acid evenly in 20-50 parts of absolute ethanol, stir for 5-25 minutes, recover the solvent with a rotary evaporator until no more liquid drips, and let it dry naturally , crushed, and passed through a 100-mesh sieve to obtain a solid dispersion.

[0051] (2), preparation of orally disintegrating tablet

[0052] The orally disintegrating tablet contains 0.8-14% levoxiracetam solid dispersion, 55-70% filler (a mixture of compressible starch and mannitol, wherein the weight ratio of compressible starch: mannitol=1-3: 1), 8-25% disintegrant (a mixture of low-substituted hydroxypropyl cellulose and cross-linked polyvinylpyrrolidone, wherein the weight ratio of low-substituted hydroxypropyl cellulose: cross-linked polyvinylpyrrolidone is 2-5:1 ), 1-5% lubricant (micronized silica gel), 0.1-1% flavoring agent (sucralose or aspartame);

[0053] The specific preparation pr...

Embodiment 2

[0056] (1) Preparation of solid dispersion:

[0057] Evenly dissolve 10g of levoxiracetam and 50g of succinic acid in 350mL of absolute ethanol, stir for 20-22min, recover the solvent with a rotary evaporator until no more liquid drips, dry naturally, crush, and pass through 100 mesh Sieve to obtain the solid dispersion of levoxiracetam.

[0058] (2) Preparation of orally disintegrating tablets:

[0059] The levoxiracetam solid dispersion (8g) obtained by sieving in step (1) is added to a filler (a mixture of 45g of compressible starch and 18g of mannitol), 40% to 50% of a disintegrating agent (low-substituted hydroxypropyl Base cellulose 18g and cross-linked polyvinylpyrrolidone 7g), use absolute ethanol as wetting agent, wet granulate through 100 mesh sieve, dry at 30-45°C, granulate, add remaining disintegrant, flavoring agent ( Aspartame 1g), lubricant (micronized silica gel 3g), compressed into tablets.

Embodiment 3

[0061] (1) Preparation of solid dispersion:

[0062] Evenly dissolve 5g of levoxiracetam and 40g of succinic acid in 250mL of absolute ethanol, stir for 20-22min, recover the solvent with a rotary evaporator until there is no more liquid dripping, dry naturally, crush, and pass through 100 mesh Sieve to obtain the solid dispersion of levoxiracetam.

[0063] (2) Preparation of orally disintegrating tablets:

[0064] The levoxiracetam solid dispersion (5g) obtained by sieving in step (1) is added to a filler (a mixture of compressible starch 35g and mannitol 30g), 40% to 50% of a disintegrant (low-substituted hydroxypropyl Base cellulose 22g and cross-linked polyvinylpyrrolidone 5g), use absolute ethanol as wetting agent, wet granulate through 100 mesh sieve, dry at 30-45°C, granulate, add remaining disintegrant, flavoring agent ( Sucralose 0.5g), lubricant (micronized silica gel 2.5g), compressed into tablets.

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Abstract

The invention provides S-oxiracetam-containing orally disintegrating tablets. The tablets are prepared from S-oxiracetam solid dispersion as an active component and a pharmacologically acceptable required excipient, can rapidly disintegrate in the oral cavity without water (or with only little water) and enter the digestive tract with the swallowing action, have the in-vivo behaviors consistent with common tablets and are very suitable for patients with difficulty in swallowing. The prepared S-oxiracetam-containing disintegrating tablets basically completely disintegrate in the oral cavity within 35 s, have good stability and the hardness of 30-40 N and are very suitable for production, transportation, packaging and storage; a preparation method is simple, requires no special equipment andis short in production cycle, low in cost and suitable for industrial production.

Description

technical field [0001] The invention relates to levo-oxiracetam, in particular to a levo-oxiracetam orally disintegrating tablet and a preparation method thereof. Background technique [0002] Levo-Oxiracetam (S-Oxiracetam), the chemical name is (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide. Studies have shown that it can promote the synthesis of phosphorylcholine and phosphorylethanolamine, promote brain metabolism, stimulate the specific central nervous system through the blood-brain barrier, and have a significant effect on the recovery of nerve function in patients. Dementia, senile dementia and various cerebrovascular diseases, brain injury, intracranial infection and other diseases have better curative effect. Its structure is as follows: [0003] [0004] Levoxiracetam [0005] Although levoxiracetam has good curative effect and high safety, its pharmaceutical preparation is still in the research and development stage. The research on levoxiracetam preparations ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/36A61K47/26A61K47/38A61K47/32A61K31/4015A61P25/00A61P9/10A61P31/00
CPCA61K9/0056A61K9/2018A61K9/2027A61K9/2054A61K9/2059A61K9/2095A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD