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Piracetam tablet composition with high drug loading capacity and preparation method thereof

A technology of piracetam tablet and high drug loading, which is applied in the field of pharmaceutical composition and its preparation, which can solve the problems of inconvenient use, difficulty in swallowing, and occurrence of fragments for patients, so as to ensure effectiveness and safety, The operation process is simple and smooth, and the size is suitable for the effect

Active Publication Date: 2020-06-19
CHANGZHOU PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injections need to be injected by medical staff, and it is inconvenient for patients to use at home, which further limits the clinical promotion of injections
In comparison, piracetam tablets have greater advantages in clinical application. The dosage of piracetam tablets currently on the market in China is 0.4g / tablet, 2-3 tablets at a time, 3 times a day, taking tablets too many, easy to forget
The dose of piracetam tablets marketed abroad is 0.8g / tablet or 1.2g / tablet, which increases the drug loading and also increases the size of the tablet, making it difficult for patients to swallow
[0004] At the same time, in the process of increasing the drug loading of piracetam in the tablet from 0.4g / tablet to 0.8g / tablet, it was found that due to the poor compressibility of the piracetam raw material itself, it often Phenomena such as falling powder, fragments, and cracks appear, resulting in friability close to the upper limit of the standard, far higher than the standard of the National Pharmacopoeia (standard regulation: tablet friability should not be greater than 1.0%)
The tablet is too brittle, which is not conducive to tablet coating, and during the storage and transportation of the drug, the tablet is prone to incomplete, edge wear, and even fragments, which makes it difficult to control the dosage and indirectly affects the effectiveness of the product and security
In addition, due to the poor compressibility of tablets, the phenomenon of unqualified products is serious, and the production efficiency is low, which is not conducive to large-scale industrial production.
[0005] In view of the many defects of existing tablets, the development of a high-loaded piracetam tablet can not only control the size of the tablet, but also solve the problem of friability, which is of great significance to the safety of clinical medication

Method used

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  • Piracetam tablet composition with high drug loading capacity and preparation method thereof
  • Piracetam tablet composition with high drug loading capacity and preparation method thereof
  • Piracetam tablet composition with high drug loading capacity and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1—prescription of high-drug-loaded piracetam tablets (specification: 0.8 g) and its preparation method (based on 1000 tablets).

[0035]

[0036]

[0037] Preparation:

[0038] 1. Pass the piracetam raw material and magnesium stearate through a 40-mesh sieve to granulate;

[0039] 2. Add 800g of granulated piracetam API, 100g of highly moldable microcrystalline cellulose KG1000 and 40.5g of croscarmellose sodium into the hopper mixer according to the prescription ratio, and set the mixing speed to 10 rpm / minutes, start the machine and mix for 20 minutes, then add 9.5g magnesium stearate, set the mixing speed to 10 rpm, and mix for 5 minutes;

[0040] 3. Add the intermediate material obtained after mixing into the tablet press for tableting, control the tableting speed to 80,000 tablets / hour, and control the tablet hardness to 90-130N;

[0041] 4. Put the plain tablets into a high-efficiency coating machine, control the temperature of the tablet bed at 3...

Embodiment 2

[0042] Example 2—prescription of high-drug-loaded piracetam tablets (specification: 1.2 g) and its preparation method (calculated as 1000 tablets).

[0043]

[0044]

[0045] Preparation:

[0046] 1. Pass the piracetam bulk drug, colloidal silicon dioxide, and magnesium stearate through a 40-mesh sieve to granulate;

[0047] 2. According to the prescription ratio, add 1200g of piracetam bulk drug, 75g of high-formability microcrystalline cellulose KG802, 150g of high-formability microcrystalline cellulose UF711 and 45g of croscarmellose sodium into the hopper for mixing In the machine, set the mixing speed at 15 rpm, start the machine and mix for 25 minutes, then add 15 g of colloidal silicon dioxide and 15 g of magnesium stearate, set the mixing speed at 10 rpm, and mix for 5 minutes;

[0048] 3. Put the intermediate material obtained after mixing into the tablet machine for tableting, control the tableting speed to 100,000 tablets / hour, and control the tablet hardness...

Embodiment 1-4

[0063] Example 1-4 High drug-loaded piracetam tablet friability test

[0064] Equipment: FT-2000 friability tester

[0065] Test product: the uncoated tablet prepared in Example 1, Example 2, Comparative Example 1-2 Test method: the weight of each test product tablet is >0.65g, and 10 tablets are taken. Use a hair dryer to blow off the falling powder, weigh it accurately, put it in a cylinder, and rotate it 100 times. Take it out, remove the powder in the same way, weigh it precisely, and calculate the weight loss. ("Chinese Pharmacopoeia" 2015 Edition Four General Rules 0923).

[0066] Results and Discussion: The information summary and friability test results of each test product are shown in the table below.

[0067]

[0068]

[0069] As can be seen from the test results, the piracetam tablet brittleness prepared by the high drug-loaded piracetam tablet composition provided by the invention and its preparation method is less than 0.1-0.3 (far lower than the Chinese...

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Abstract

The invention provides a piracetam tablet composition with high drug loading capacity and a preparation method thereof. The piracetam tablet composition comprises 80-90% of piracetam, 10-20% of high-formability microcrystalline cellulose (CEOLUSTM), 2-5% of a disintegrating agent, 0.5-2% of a lubricant and 0-4% of a gastric-soluble film coating premix. The composition can effectively improve the drug loading capacity of a piracetam tablet and improve the problem of poor friability of a product due to improvement of the drug loading capacity. In addition, the invention also provides a preparation method for the piracetam tablet with the high drug loading capacity. The method provided by the invention is simple and convenient in process operation, high in production efficiency and applicableto industrial production.

Description

[0001] Technical field: the present invention relates to a kind of pharmaceutical composition and preparation method thereof, be specifically related to a kind of piracetam tablet composition and preparation method thereof. Background technique: [0002] Piracetam is a drug for improving brain metabolism, which belongs to the cyclic derivative of r-aminobutyric acid, can promote ATP in the brain, can promote the synthesis of acetylcholine and positively enhance the conduction of nerve excitation, and has the effect of promoting metabolism in the brain. It can resist brain function damage caused by physical and chemical factors, improve retrograde amnesia caused by hypoxia, enhance memory and improve learning ability. It is clinically used to treat senile dementia and is the first-line drug for the treatment of senile dementia. [0003] Piracetam preparations have been marketed worldwide, and currently there are two dosage forms of injection and oral tablet on the market in Chi...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4015A61K47/38A61P25/28
CPCA61K31/4015A61K9/2054A61K9/282A61P25/28
Inventor 丁盛张卫香张晓炎
Owner CHANGZHOU PHARMA FACTORY
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