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Lacosamidesolid preparation and preparation method thereof

A solid preparation, lacosamide technology, applied in the field of medicine, can solve the problems of low dissolution rate of preparations, many granulated fine powders, poor fluidity and the like

Active Publication Date: 2015-07-22
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the problem that the raw materials in the existing lacosamide immediate-release tablet technology are loose and light in weight, and easy to be layered when mixed; there are many granulated fine powders and poor fluidity; the dissolution rate of the preparation is low, and the inclusion technology requires special equipment. The process is cumbersome, which is not conducive to the problem of commercial production

Method used

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  • Lacosamidesolid preparation and preparation method thereof
  • Lacosamidesolid preparation and preparation method thereof
  • Lacosamidesolid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 (1000 pieces amount)

[0024] Lacosamide 100g

[0025] Microcrystalline Cellulose PH102 24g

[0026] Croscarmellose Sodium 24g

[0027] Hypromellose 2.4g

[0028] Crospovidone CL 24g

[0029] Optimized Microcrystalline Cellulose 60g

[0030] Colloidal silicon dioxide 2.4g

[0031] Magnesium Stearate 2.4g

[0032] Gastric soluble film coating premix 7.2g

[0033] making process:

[0034] (1) Put the prescribed amount of lacosamide, microcrystalline cellulose PH102, and croscarmellose sodium in a wet mixer, and take three samples from the upper, middle, and lower parts of the mixer in 15 minutes, and measure the content , to calculate the content uniformity. Granulate and dry to obtain Mixture 1.

[0035] (2) Add optimized microcrystalline cellulose, crospovidone CL, colloidal silicon dioxide and magnesium stearate to mixture 1, and mix them together.

[0036] (3) Compression, coating and packaging.

Embodiment 2

[0037] Embodiment 2 (quantity of 1000 pieces)

[0038] Lacosamide 100g

[0039] Microcrystalline Cellulose PH102 36g

[0040] Croscarmellose Sodium 12g

[0041] Hypromellose 2.4g

[0042] Crospovidone CL 12g

[0043] Optimized Microcrystalline Cellulose 72g

[0044] Colloidal silicon dioxide 2.4g

[0045] Magnesium Stearate 2.4g

[0046] Gastric soluble film coating premix 7.2g

[0047] making process:

[0048] (1) Put the prescribed amount of lacosamide, microcrystalline cellulose PH102, and croscarmellose sodium in a wet mixer, and take three samples from the upper, middle, and lower parts of the mixer in 15 minutes, and measure the content , to calculate the content uniformity. Granulate and dry to obtain Mixture 1.

[0049] (2) Add optimized microcrystalline cellulose, crospovidone CL, colloidal silicon dioxide and magnesium stearate to mixture 1, and mix them together.

[0050] (3) Compression, coating and packaging.

Embodiment 3

[0051] Embodiment 3 (quantity of 1000 pieces)

[0052] Lacosamide 100g

[0053] Microcrystalline Cellulose PH102 30g

[0054] Croscarmellose Sodium 18g

[0055] Hypromellose 2.4g

[0056] Crospovidone CL 18g

[0057] Optimized Microcrystalline Cellulose 66g

[0058] Colloidal silicon dioxide 2.4g

[0059] Magnesium Stearate 2.4g

[0060] Gastric soluble film coating premix 7.2g

[0061] making process:

[0062] (1) Put the prescribed amount of lacosamide, microcrystalline cellulose PH102, and croscarmellose sodium in a wet mixer, and take three samples from the upper, middle, and lower parts of the mixer in 15 minutes, and measure the content , to calculate the content uniformity. Granulate and dry to obtain Mixture 1.

[0063] (2) Add optimized microcrystalline cellulose, crospovidone CL, colloidal silicon dioxide and magnesium stearate to mixture 1, and mix them together.

[0064] (3) Compression, coating and packaging.

[0065] For the convenience of comparison ...

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Abstract

The invention discloses a lacosamide solid preparation and a preparation method thereof. The lacosamide solid preparation comprises lacosamide, an internally added disintegrating agent, an externally added disintegrating agent, an internally added attenuant, an externally added attenuant, an adhesive, a glidant and a lubricant. Through adoption of the preparation method, the defects, of the conventional lacosamide fast-release tablet, that raw materials are loose and light to cause high layering possibility after mixing, the conventional preparation is high in fine powder content and low in flowability, the dissolution rate of the conventional preparation is relatively low, special equipment is required due to adoption of the inclusion technology, the process is cumbersome, and commercialized production is inconvenient are overcome.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a lacosamide solid preparation and a preparation method thereof. Background technique [0002] Lacosamide is a new type of NMDA receptor antagonist at the glycine site, which belongs to a new class of functional amino acids. The research focuses on its antiepileptic and neuropathic effects. In vitro electrophysiological studies have shown that lacosamide selectively promotes the activity of slowly inactivated voltage-gated sodium ion channels, thereby stabilizing abnormally excited neuron cell membranes and inhibiting repeated triggering of neurons, but it does not affect the normal physiological excitability of neurons. The reduction of neuronal excitability is an important molecular mechanism in the treatment of epilepsy and neuropathic pain. In addition, lacosamide can bind to cerebrofalin-mediated regulatory protein-2 (CRMP-2, a phosphoprotein mainly distributed in the ner...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/165A61K47/38A61K47/36A61K47/34A61K47/32A61K47/10A61P25/08A61P25/00A61K47/26
Inventor 曲继广赵晓雷程彦超刘芳菊杨帆牛虹卫陈雪桃张伟丽张玉红
Owner SHIJIAZHUANG NO 4 PHARMA
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