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A kind of lacosamide crystal form II tablet and its preparation method and application

A technology of lacosamide and its crystal form, which is applied in lacosamide crystal form II tablet and its preparation and application field, which can solve problems such as easy generation of large dust, layering of materials, poor fluidity, etc., and improve production efficiency , stable quality, and the effect of simplifying the production process

Active Publication Date: 2021-01-26
SPH NO 1 BIOCHEM & PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In the prior art, lacosamide has poor fluidity, the raw materials become abnormally loose after crushing, and the static electricity is large. When the raw and auxiliary materials are mixed, it is easy to cause material stratification, and a large amount of dust is easy to be generated during the production process.

Method used

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  • A kind of lacosamide crystal form II tablet and its preparation method and application
  • A kind of lacosamide crystal form II tablet and its preparation method and application
  • A kind of lacosamide crystal form II tablet and its preparation method and application

Examples

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Effect test

Embodiment 1

[0062]Example 1: Lacosamide crystal form II tablets

[0063]Tablet core prescription (1000 tablets)

[0064]

[0065]Preparation Process:

[0066](1) Prepare hydroxypropyl cellulose into a 5 wt% binder aqueous solution for use.

[0067](2) Put the prescription amount of 80 mesh lacosamide crystal form II, microcrystalline cellulose, low-substituted hydroxypropyl cellulose and cross-linked povidone into the fluidized bed granulator, and turn on the fluidization The bed granulator is preheated, the inlet air temperature is set to 60℃, and the inlet air volume is 2000m3 / h to keep the material in a better fluidized state. When the temperature of the material reaches 42°C, turn on the feed pump, set the flow rate of the binder aqueous solution to 180g / min, and spray the binder aqueous solution to continue stirring during the granulation process. After the adhesive water solution is sprayed, the air inlet air volume and the material temperature are kept unchanged, the material is dried, and the moisture...

Embodiment 2

[0071]Example 2: Lacosamide crystal form II tablets

[0072]Tablet core prescription (1000 tablets)

[0073]

[0074]Preparation Process:

[0075](1) Prepare hydroxypropyl cellulose into a 5 wt% binder aqueous solution for use.

[0076](2) Put lacosamide crystal form II, lactose, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and cross-linked povidone with a prescription amount of 80 mesh or more into the fluidized bed granulator and turn on The fluidized bed granulator is preheated, and the inlet air temperature is set to 60℃, and the inlet air volume is 2000m.3 / h to keep the material in a better fluidized state. When the temperature of the material reaches 42°C, turn on the feed pump, set the flow rate of the binder aqueous solution to 180g / min, and spray the binder aqueous solution to continue stirring during the granulation process. After the adhesive water solution is sprayed, the inlet air volume and the material temperature are kept unchanged, the material is dried, an...

Embodiment 3

[0079]Example 3: Lacosamide crystal form II tablets

[0080]Tablet core prescription (1000 tablets)

[0081]

[0082]Preparation Process:

[0083](1) Prepare hydroxypropyl cellulose into a 5 wt% binder aqueous solution for use.

[0084](2) Put the prescription amount of Lacosamide Form II, microcrystalline cellulose, and crospovidone of 80 mesh or more into the fluidized bed granulator, and turn on the fluidized bed granulator for preheating. Set the inlet air temperature to 60℃, and the inlet air volume to 2000m3 / h to keep the material in a better fluidized state. When the temperature of the material reaches 42°C, turn on the feed pump, set the flow rate of the binder aqueous solution to 180g / min, and spray the binder aqueous solution to continue stirring during the granulation process. After the adhesive water solution is sprayed, the inlet air volume and the material temperature are kept unchanged, the material is dried, and the moisture content of the material is controlled to 2% to 5%, and th...

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Abstract

The invention discloses a lacosamide crystal form II tablet, a preparation method and application thereof. The lacosamide crystal form II tablet includes a tablet core and a film coating layer, and the tablet core includes the following raw and auxiliary materials in mass percentages: lacosamide crystal form II 10% to 60%, microcrystalline cellulose 10% %-60%, lactose 0-40%, crospovidone 3-12%, low-substituted hydroxypropyl cellulose 0-10%, hydroxypropyl cellulose 0.5%-10%, silicified microcrystalline cellulose 0.1% ~5% and magnesium stearate 0.3%~3%. One-step granulation using fluidized bed. The lacosamide crystal form II tablet can be used as an antiepileptic drug. Compared with the lacosamide raw material and crystal form I, the crystal form II provided by the present invention is easier to pulverize, the micropowder obtained by pulverization has less static electricity, is easier to mix with auxiliary materials, reduces the loss of medicine, and has a high content of the prepared medicine. Good dissolution rate, high stability, low total impurity content.

Description

Technical field[0001]The invention relates to a lacosamide crystal form II tablet and a preparation method and application thereof.Background technique[0002]Epilepsy (Epilepsy) is a chronic disease in which the sudden abnormal discharge of brain neurons leads to transient brain dysfunction. The most common neurological diseases worldwide are second only to cerebrovascular diseases and the second most common neurological diseases. According to statistics, the prevalence of the disease is 0.3% to 0.7% in developed countries, while it is as high as 1.5% to 3.5% in developing countries. The prevalence rate in my country is about 0.5%. There are about 6 million people with epilepsy each year. About 650,000 to 700,000 new cases have appeared. Approximately 75% of them can obtain satisfactory effects through conventional first-line anti-epileptic drugs, and approximately 25% have intractable epilepsy. There are more than 1.5 million intractable epilepsy in the country. There are a large nu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/32A61K47/38A61K31/16C07C237/22A61P25/08
CPCA61K9/2054A61K9/284A61K31/16A61P25/08C07B2200/13C07C237/22
Inventor 顾春燕陈辰周辉黄臻辉
Owner SPH NO 1 BIOCHEM & PHARMA CO LTD