L-alpha-glycerophosphoryl choline film-coated tablet and preparation method thereof

A technology of glycerophosphocholine and film-coated tablets, which is applied in the fields of pharmaceutical formulations, nervous system diseases, drug combinations, etc., can solve the problems of small particle density, difficult granulation, and increased cost, and achieve improved hygroscopicity and stability Sexuality, the effect of improving production efficiency

Inactive Publication Date: 2012-07-04
徐奎
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this process is that the raw material of L-α-glycerophosphorylcholine is highly hygroscopic, and the environmental humidity must be strictly controlled during the crushing and sieving process, usually below 30%.
In addition, because L-α-glycerophosphorylcholine has good solubility in water, ordinary wet granulation can only use alcohol as a solvent for the binder, and when the binder uses water as the solvent, the raw material will appear dissolves, difficult to granulate
This not only increases the cost, but also requires explosion-proof equipment
The boiling granulation process can use water as a solvent binder, but because the raw material of L-α-glycerophosphocholine is light in weight and has severe static electricity after crushing, the resulting granules have low density and are difficult to fill

Method used

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  • L-alpha-glycerophosphoryl choline film-coated tablet and preparation method thereof
  • L-alpha-glycerophosphoryl choline film-coated tablet and preparation method thereof
  • L-alpha-glycerophosphoryl choline film-coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1 Weigh 400g of L-alpha-glycerophosphorylcholine, 327g of microcrystalline cellulose, 60g of lactose, and 7.9g of silicon dioxide, mix them, add 7.9g of magnesium stearate, mix them evenly, and press them into tablets. Tablets, tablet weight 0.8g, tablet hardness control 6-7kg; premix made of 6.6g hydroxypropylmethylcellulose and ethylcellulose film-forming materials, dissolved in 76ml of 95% ethanol solution to prepare isolation layer coating solution, stirred for 45 minutes, and evenly sprayed on the surface of L-α-glycerophosphorylcholine tablet core by spray gun to prepare L-α-glycerophosphorylcholine isolation-coated tablet; 20g polyvinyl alcohol film-forming material was made into The premix was dispersed in 95ml of distilled water, prepared as a moisture-proof layer coating solution, stirred for 45 minutes, and evenly sprayed on the surface of the L-α-glycerophosphocholine isolation coating tablet through a spray gun; detection and packaging.

Embodiment 2

[0020] Example 2 Weigh 400g of L-alpha-glycerophosphorylcholine, 255g of microcrystalline cellulose, 25g of pregelatinized starch, 18g of hydroxypropyl cellulose, 11g of silicon dioxide, and 25g of talcum powder, and add magnesium stearate Mix 7.3g, mix evenly, and compress into 1000 tablets, the tablet weight is 0.74g, and the tablet hardness is controlled at 6-7kg; 3.1g of premixed film-forming materials containing ethyl cellulose and polyvinylpyrrolidone material, dissolved in 36.8ml of 95% ethanol solution to prepare an isolation layer coating solution, stirred for 45 minutes, and evenly sprayed on the surface of L-alpha-glycerophosphorylcholine tablet core through a spray gun to prepare L-alpha-glycerophosphocholine Film-coated tablet: Disperse 12.2g of the premix made of methacrylic acid copolymer film-forming material in 100ml of distilled water, prepare a moisture-proof layer coating solution, stir for 45 minutes, and spray evenly on L-α-glycerophosphate through a spray...

Embodiment 3

[0021] Example 3 Weigh 400g of L-alpha-glycerophosphorylcholine, 327g of microcrystalline cellulose, 12g of hydroxypropyl cellulose, 18g of lactose, 3.9g of silicon dioxide, and 3.9g of polyethylene glycol, mix them, and add stearic acid Magnesium 7.8 mixed, mixed evenly, tableted, 1000 tablets, tablet weight 0.773g, tablet hardness controlled at 6-7kg; premix made of 9.6g hydroxypropyl methylcellulose film-forming material, dissolved in 95 % ethanol solution 111.5ml was prepared as an isolation layer coating solution, stirred for 45 minutes, and was evenly sprayed on the surface of the L-α-glycerophosphorylcholine tablet core by a spray gun to prepare an L-α-glycerophosphorylcholine isolation coating tablet; The premix made of 16g ​​of ethyl cellulose film-forming material was dispersed in 73ml of distilled water to prepare a moisture-proof layer coating solution, stirred for 45 minutes, and evenly sprayed on the surface of L-α-glycerophosphorylcholine isolation coating tablet...

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Abstract

The invention discloses an L-alpha-glycerophosphoryl choline film-coated tablet, which is applied to the pharmaceutical industry. The L-alpha-glycerophosphoryl choline film-coated tablet comprises an L-alpha-glycerophosphoryl choline tablet core and a coating layer, wherein the L-alpha-glycerophosphoryl choline tablet core comprises the following components in percentage by weight: 45-55wt% of L-alpha-glycerophosphoryl choline, 40-50wt% of filler, 0.5-5wt% of flow aid and 0.5-3wt% of lubricant; the coating layer is divided into an isolated coat layer and a moisture-proof coat layer; the filler is one or several of microcrystalline cellulose, lactose, calcium hydrophosphate, hydroxypropyl cellulose and pregelatinized starch; the flow aid is one or several of silicon dioxide and talc powder; the lubricant is one or several of magnesium stearate, polyethylene glycol and leucine; and the isolated coat layer of the coating layer is one or several of film-forming materials of hydroxypropyl methyl cellulose, ethyl cellulose and polyvinylpyrrolidone or premix comprising the above film-forming materials. According to prescription screening, the L-alpha-glycerophosphoryl choline film-coated tablet core is prepared by a direct tableting technology and is easy to operate and control, the processes of smashing and screening raw materials are omitted, the phenomenon that the raw materials are easy to adsorb moisture after being smashed is avoided, the technology is simplified, the production cost is lowered, and the production technology is improved.

Description

1. Technical field [0001] The invention relates to L-alpha-glycerophosphorylcholine film-coated tablets in the medical and health industry and a preparation method thereof 2. Background technology [0002] L-α-glycerophosphorylcholine was developed by LPB (Novartis / Italfarmaco) as a nootropic drug, which is effective for aging memory loss. It functions as a precursor of acetylcholine in cerebral cortex neurons and phospholipids in neuronal membranes (Company communication, Italfarmaco, Mar 1992). The drug was listed for the first time in Italy (1990) by LPB under the trade name Delecit. In Italy, it is also distributed by Novartis and Italfarmaco under the trade names Brezal and Gliatilin respectively. In Poland, the drug was listed by Italfarmaco (1993), with the trade name Gliatilin; in Argentina, it was listed by Montpellier (1995), with the trade name Gliatilin; in South Korea, it was listed by Dong Wha (1996, the trade name was Gliatilin) The listed company in Russia...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/30A61K9/36A61K9/32A61K31/661A61K47/38A61P25/00
Inventor 徐奎
Owner 徐奎
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