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Preparation method of levorotatory oxiracetam orally disintegrating preparation

The technology of oral disintegration and disintegrating agent is applied in the field of preparation of oral disintegrating preparations of levooxiracetam, which can solve the problems of reducing the amount of absorbed drug, increasing the risk of drug safety, unstable pharmacological effect, etc. Small amount, small difference in tablet weight, ensuring the effect of drug efficacy

Inactive Publication Date: 2018-11-02
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventor found in the research that the orally disintegrating tablet prepared by the above method, the drug is mainly dissolved in the stomach, and with the prolongation of the drug residence time in the stomach, the amount of the drug decomposed by gastric acid gradually increases, which leads to the effective absorption of the drug in the intestinal tract The dose is reduced, resulting in unstable pharmacological effects, and also increases the risk of drug safety

Method used

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  • Preparation method of levorotatory oxiracetam orally disintegrating preparation
  • Preparation method of levorotatory oxiracetam orally disintegrating preparation
  • Preparation method of levorotatory oxiracetam orally disintegrating preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Get 20 parts of absolute ethanol, under stirring state, add 1 part of levoxiracetam chemical bulk drug (provided by Chongqing Dongze Pharmaceutical Technology Co., Ltd., purity 99.5%) and 6 parts of Eudragit E100 (Guangzhou Shuoheng Biotechnology Co., Ltd. Provided by the company), stirred until dissolved, and then spray-dried in a spray dryer (produced by Huawei Technology Co., Ltd.), the inlet air temperature of spray drying was 138°C, and the outlet air temperature was 79°C; Tan solid dispersion is pulverized to obtain.

[0033] Referring to the preparation method of Example 1, run Examples 2-5 according to the parameters in Table 1 below to prepare the levoxiracetam solid dispersion. The chemical bulk drug of levoxiracetam used is 1 part.

[0034] Table 1 Preparation of Levoxiracetam Solid Dispersion

[0035]

Embodiment 6

[0037] Prescription: Levoxiracetam solid dispersion prepared in Example 1 70g, pregelatinized starch 4g, mannitol 4g, croscarmellose sodium 4g, low-substituted hydroxypropyl cellulose 8g, polyvinylpyrrolidone 7g , xylitol 1g, micronized silica gel 2g.

[0038] Preparation:

[0039] (1) Material screening: levoxiracetam solid dispersion, pregelatinized starch, mannitol, croscarmellose sodium, low-substituted hydroxypropyl cellulose, polyvinylpyrrolidone, xylitol, Micropowder silica gel is passed through a 100-mesh sieve respectively, and set aside;

[0040] (2) Mixing and granulation: Add the sieved levoxiracetam solid dispersion, filler, and disintegrant into a wet granulator (Changzhou Yiyiyi Drying Equipment Co., Ltd.) and mix evenly, start the stirring paddle to mix 5 minutes; stop, add adhesive (polyvinylpyrrolidone ethanol solution prepared with an appropriate amount of ethanol) at one time, start the stirring paddle, mix the granulation paddle to prepare soft material ...

Embodiment 7

[0043] Prescription: Levoxiracetam solid dispersion prepared in Example 1 58g, pregelatinized starch 4g, mannitol 12g, croscarmellose sodium 3g, low-substituted hydroxypropyl cellulose 15g, polyvinylpyrrolidone 6g , sucralose 1g, magnesium stearate 1g.

[0044] Preparation:

[0045] (1) Material screening: solid dispersion of levoxiracetam, pregelatinized starch, mannitol, croscarmellose sodium, low-substituted hydroxypropyl cellulose, polyvinylpyrrolidone, sucralose, Magnesium stearate is passed through a 100-mesh sieve respectively, for subsequent use;

[0046] (2) Mixing and granulation: Add the sieved levoxiracetam solid dispersion and disintegrant into the wet granulator and mix evenly, start the stirring paddle to mix for 10 minutes; stop the machine, and add the binder at one time (polyvinylpyrrolidone ethanol solution prepared with an appropriate amount of ethanol), start the stirring paddle, mix the granulating paddle to prepare soft material for 10 minutes, and dis...

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Abstract

The invention provides a preparation method of a levorotatory oxiracetam orally disintegrating preparation. The levorotatory oxiracetam orally disintegrating preparation is prepared from48-88% of a levorotatory oxiracetam solid dispersion, 0-18% of a filler, 5-25% of a disintegrating agent, 2-10% of a binder, 1-3% of a correctant and 0-5% of a lubricant in percentage by mass by wet granulation andtabletting, wherein the levorotatory oxiracetam solid dispersion is prepared by spray drying of levorotatory oxiracetam, Eudragit E100 and a proper amount of anhydrous ethanol at an inlet air temperature of 118-166 DEG C and an outlet air temperature of 64-98 DEG C. The orally disintegrating preparation prepared by the method provided by the invention has a small release amount in a simulated gastric juice, and rapidly releases a large amount in a simulated intestinal juice, thereby increasing the absorption of levorotatory oxiracetam and ensuring the drug therapeutic effect. The levorotatoryoxiracetam particles prepared by the invention are fine and uniform, moderate in hardness and small in tablet weight difference. The preparation method provided by the invention is simple and suitable for industrial production.

Description

technical field [0001] The invention relates to levo-oxiracetam preparations, in particular to a preparation method of levo-oxiracetam orally disintegrating preparations. Background technique [0002] Oxiracetam (CAS No.: 62613-82-5) is an anti-hypoxic nootropic drug synthesized by Italy Spike Chem in 1974 (the compound is disclosed in US4118396), and it is mainly used clinically to treat brain Neurological deficits, memory and cognitive impairments caused by stroke and traumatic brain injury; mild to moderate Alzheimer's disease, vascular dementia, mixed dementia, etc. The pharmacological effects of oxiracetam mainly include the following aspects: in various behavioral experiments, it can improve thinking, memory and academic performance; it can reduce memory damage caused by electric shock; Decreased learning ability of rats with vascular injury; promotes the transport of acetylcholine in the cerebral cortex and hippocampus, increases the affinity for choline uptake and t...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/14A61K47/36A61K47/38A61K47/26A61K47/32A61K31/4015A61P25/28
CPCA61K9/0056A61K9/14A61K9/2018A61K9/2027A61K9/2054A61K9/2059A61K9/2095A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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