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A kind of levetiracetam sustained-release tablet and preparation method thereof

A technology for sustained-release tablets and tablet cores, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. and other problems, to achieve the effect of simple product prescription, simple preparation process and good fluidity

Active Publication Date: 2018-03-13
SHENYANG NO 1 PHARMA FACTORY DONGBEI PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The wet granulation process is a more commonly used process, with popular equipment and simple operation, but for this product, there are still the following problems in wet granulation: 1. Due to the strong viscosity of high-viscosity hypromellose, it is difficult to use water-based solvents. Adhesive, so polyvinylpyrrolidone alcohol solution is usually used as the adhesive to prepare granules (this method is used in Volume 35 of Pharmaceutical Progress 2011), this method not only increases the cost, but also brings many safety hazards to production
2. If the skeleton material high-viscosity hypromellose participates in the granulation process, changes in process parameters, such as stirring time, stirring speed, binder addition amount and addition method, will seriously affect the properties of the granules, thereby affecting the dissolution of the product
3. Levetiracetam has excellent water solubility. If the type of binder selected is not suitable, the granules made will easily harden after being placed, and the dissolution of the compressed tablet will be delayed.
Dry granulation needs to be completed with a dry granulator, but the dry granulator is more expensive, so this process is usually not the preferred process. Therefore, the development of a suitable levetiracetam sustained-release tablet and its preparation method is New issues to be solved urgently

Method used

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  • A kind of levetiracetam sustained-release tablet and preparation method thereof
  • A kind of levetiracetam sustained-release tablet and preparation method thereof
  • A kind of levetiracetam sustained-release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Table 1 Prescriptions using two different framework materials

[0021]

[0022] Preparation:

[0023] (1) Granulation: Weigh the prescribed amount of levetiracetam, add 25g of low-viscosity hypromellose (HPMC E50) 3% w / w aqueous solution to make soft material, granulate with 20 mesh sieve, boil and dry, 10 Mesh sieving;

[0024] The parameters of boiling drying are: fan power: 30-50Hz; back-blowing interval: 3-20 seconds; inlet air temperature: 40-60°C; material temperature: 30-40°C, measure the moisture of the mixture, and control the moisture at 0.5-1.5%;

[0025] (2) Mixing: Weigh the prescribed amount of levetiracetam particles, framework material, and glidant and mix for 15-20 minutes, then add lubricant and mix for 2-3 minutes;

[0026] (3) Tablet compression: The mixed materials are compressed into tablet cores with a tablet hardness of 13-15kg;

[0027] (4) Preparation of coating solution: Disperse 20g of Opadry 295F in 113g of water and stir for 40-50 minutes to prepare ...

Embodiment 2

[0031] Table 2 Formulations using a single skeleton material

[0032]

[0033] Preparation:

[0034] (1) Granulation: Weigh the prescribed amount of levetiracetam, add 25g of low-viscosity hypromellose (HPMC E50) 3% w / w aqueous solution to make soft material, granulate with 30 mesh sieve, boil and dry, 20 Mesh sieving;

[0035] The parameters of boiling drying are: fan power: 30-50Hz; back-blowing interval: 3-20 seconds; inlet air temperature: 40-60°C; material temperature: 30-40°C, measure the moisture of the mixture, and control the moisture at 0.5-1.5%;

[0036] (2) Mixing: Weigh the prescribed amount of levetiracetam particles, framework material, and glidant and mix for 15-20 minutes, then add lubricant and mix for 2-3 minutes;

[0037] (3) Tablet compression: The mixed materials are compressed into tablet cores with a tablet hardness of 13-15kg;

[0038] (4) Preparation of coating solution: Disperse 22g of Opadry 295F in 115g of water and stir for 40-50 minutes to prepare a 16% co...

Embodiment 3

[0041] Table 3 Prescriptions using different amounts of lubricant

[0042]

[0043] Preparation:

[0044] (1) Granulation: Weigh the prescribed amount of levetiracetam, add 25g of low-viscosity hypromellose (HPMC E50) 3% w / w aqueous solution to make soft material, granulate with 20 mesh sieve, boil and dry, 20 Mesh sieving;

[0045] The parameters of boiling drying are: fan power: 30-50Hz; back-blowing interval: 3-20 seconds; inlet air temperature: 40-60°C; material temperature: 30-40°C, measure the moisture of the mixture, and control the moisture at 0.5-1.5%;

[0046] (2) Mixing: Weigh the prescribed amount of levetiracetam particles, framework material, and glidant and mix for 15-20 minutes, then add lubricant and mix for 2-3 minutes;

[0047] (3) Tablet compression: The mixed materials are compressed into tablet cores with a tablet hardness of 13-15kg;

[0048] (4) Preparation of coating solution: Disperse 20g of Opadry 295F in 91g of water and stir for 40-50 minutes to prepare an 1...

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Abstract

A levetiracetam sustained-release tablet applied in the field of pharmaceutical preparations and a preparation method thereof, the sustained-release tablet is composed of a tablet core and a coating layer, and the tablet core is composed of levetiracetam and a skeleton Composition of materials, glidants, binders and lubricants, the weight percentage content of each component in the sustained-release tablet is 55%-80% of levetiracetam, 15%-35% of the skeleton material, and 0.05% of the binder ‑0.20%, glidant 0.8%‑2%, lubricant 2%‑7%, coating layer 2%‑4%. The preparation method comprises the following steps: (1) granulation; (2) mixing; (3) tabletting; (4) preparing coating solution; (5) coating. It has the characteristics of simple product prescription, good dissolution effect, good stability, the preparation method does not need to use organic solvents such as ethanol, the preparation process is simple, easy to operate, and the production cost is low. It is especially suitable for large-scale industrial production and will be widely used in the field of pharmaceutical preparations middle.

Description

Technical field [0001] The invention relates to a levetiracetam sustained-release tablet in the field of pharmaceutical preparations and a preparation method thereof. Background technique [0002] Levetiracetam is a pyrrolidone derivative, and its chemical structure is not related to existing antiepileptic drugs. The exact mechanism of the antiepileptic effect of levetiracetam is still unclear. The anti-epileptic effects of levetiracetam have been evaluated in various animal models of epilepsy. Levetiracetam has no inhibitory effect on simple epileptic seizures induced by the maximum stimulation of electric current or multiple convulsants, and shows only weak activity in submaximum stimulation and threshold tests. However, protective effects have been observed for pilocarpine and kainic acid-induced focal seizures secondary to generalized seizures. These two chemical convulsants can mimic the characteristics of complex partial seizures in some people with secondary generalized ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/28A61K31/4015A61K47/38
Inventor 姜海涛陈雅琴赵颖梅石秀芹赵娟王虹王金晶
Owner SHENYANG NO 1 PHARMA FACTORY DONGBEI PHARMA GRP
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