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Multi-unit sustained-release preparation of levetiracetam and preparation method thereof

A sustained-release preparation, multi-unit technology, applied in the field of multi-unit sustained-release preparations containing levetiracetam and its preparation, can solve the problem that the anti-epileptic advantages are not fully exerted, the blood drug concentration changes greatly, and the drug efficacy is unstable and other problems, to achieve the effect of prolonging the action time of the drug, reducing the number of administrations, and being suitable for a wide range of people.

Inactive Publication Date: 2009-12-16
WUXI DINGFU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, most of the levetiracetam preparations currently on the market are administered multiple times a day. Although the new oral long-acting tablet KEPPRA XR prolongs the drug action time, it still has the phenomenon of sudden release of the drug, large changes in blood drug concentration, and drug loss. Unstable efficacy and other shortcomings, its innate anti-epileptic advantages have not been fully utilized in practical applications

Method used

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  • Multi-unit sustained-release preparation of levetiracetam and preparation method thereof
  • Multi-unit sustained-release preparation of levetiracetam and preparation method thereof
  • Multi-unit sustained-release preparation of levetiracetam and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: Levetiracetam sustained-release pellets (filling 1000 capsule parts)

[0036] Prepare materials according to the following formula, pulverize raw materials and various pharmaceutical excipients, and pass through a 100-mesh sieve.

[0037] Levetiracetam (drug active ingredient) 500g

[0038] Microcrystalline cellulose (forming agent) 125g

[0039] Lactose (forming agent) 25g

[0040] Cross-linked sodium carboxymethyl starch (disintegrant) 25g

[0041] Water (wetting agent) appropriate amount

[0042] Eudragit NE 30D (functional coating material) 450g

[0043] Talc powder (anti-sticking agent) 135g

[0044] Opadry (non-functional coating material) 20g

[0045] Water (solvent / dispersion medium) make up to 225g

[0046] The prescription amount of levetiracetam, microcrystalline cellulose, lactose, and cross-linked carboxymethyl starch sodium are evenly mixed, and an appropriate amount of water is used as a wetting agent to prepare a soft material, which i...

Embodiment 2

[0048] Embodiment 2: Levetiracetam sustained-release pellets (filling 1000 capsule parts)

[0049] Prepare materials according to the following formula, pulverize raw materials and various pharmaceutical excipients, and pass through a 100-mesh sieve.

[0050] Levetiracetam (drug active ingredient) 500g

[0051] Microcrystalline cellulose (forming agent) 125g

[0052] Lactose (forming agent) 25g

[0053] Cross-linked sodium carboxymethyl starch (disintegrant) 25g

[0054] Water (wetting agent) appropriate amount

[0055] Hypromellose (non-functional coating material) 13.5g

[0056] Talc powder (anti-sticking agent) 8.1g

[0057] 95% ethanol (solvent / dispersion medium) appropriate amount

[0058] Eudragit NE 30D (functional coating material) 337.5g

[0059] Talc powder (anti-sticking agent) 112.5g

[0060] Opadry (non-functional coating material) 20g

[0061] Water (solvent / dispersion medium) make up to 225g

[0062] Mix the prescribed amount of levetiracetam, microcry...

Embodiment 3

[0064] Embodiment 3: Levetiracetam sustained-release granules (filling 1000 capsules)

[0065] Prepare materials according to the following formula, pulverize raw materials and various pharmaceutical excipients, and pass through a 100-mesh sieve.

[0066] Levetiracetam (drug active ingredient) 500g

[0067] Stearic acid (block material) 125g

[0068] Ethyl cellulose (retardation material) 25g

[0069] Proper amount of polyvinylpyrrolidone aqueous solution (binder)

[0070] Eudragit NE 30D (functional coating material) 337.5g

[0071] Talc powder (anti-sticking agent) 112.5g

[0072] Opadry (non-functional coating material) 20g

[0073] Water (solvent / dispersion medium) make up to 225g

[0074] Mix the prescribed amount of levetiracetam, stearic acid, and ethyl cellulose evenly, use polyvinylpyrrolidone aqueous solution as a binder to prepare a soft material, granulate with a wet mixing granulator and dry to obtain a drug-loaded core in the form of granules body; dispers...

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Abstract

The invention discloses a multi-unit sustained-release preparation of levetiracetam and a preparation method thereof, wherein the preparation is prepared by filling a plurality of independent sustained-release unit bodies with pharmacological activity into capsules. The sustained-release unit bodies consists of medicament carrying core bodies containing levetiracetam active components and coating layers enwrapped outside the medicament carrying core bodies, and the sustained-release unit bodies can also are prepared by adding a retardant material for retarding the medicament release into the medicament carrying core bodies, or adding a functional coating material for prolonging the medicament release time into the coating layers, or adopting the combination of the two modes. The multi-unit sustained-release preparation of the levetiracetam is released slowly, stably and uniformly in vivo due to the unique formulation and preparation method thereof, has no medicament burst release phenomena and is not influenced by foods so that the blood-medicament concentration is more smooth, the time for the medicament to take effect is longer, the untoward effect is obviously lightened, and the compliance of patients is greatly improved, thus the multi-unit sustained-release preparation of the levetiracetam is a novel and high-efficiency anti-epileptic pharmaceutical preparation.

Description

technical field [0001] The invention relates to a levetiracetam preparation, more specifically, a multi-unit slow-release preparation containing levetiracetam and a preparation method thereof. Background technique [0002] Levetiracetam (LEV) is levoethylpiracetam among piracetam derivatives, and its chemical name is (S)-α-ethyl-2-oxo-1-pyrrolidineacetamide, The target of action has been proved to be the synaptic vesicle protein 2 (SV2) A of the central nervous system, which has a new anti-epileptic mechanism. Levetiracetam has the characteristics of rapid onset of action, not affected by food, bioavailability close to 100%, protein binding rate <10%, no drug-drug interaction, mild adverse reactions, and good tolerance. The only antiepileptic drug with unique properties of preventing epileptic seizures, it is clinically used as a broad-spectrum antiepileptic drug. [0003] However, most of the levetiracetam preparations currently on the market are administered multiple ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/4015A61P25/08
Inventor 沈立新李斌刘福双邹济高
Owner WUXI DINGFU PHARMA