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Sustained-release oral preparation of brivaracetam, and preparation method thereof

A sustained-release preparation, the technology of brivaracetam, applied in the field of pharmaceutical preparations, can solve the problems of large drug release, long dissolution time, and unfavorable patients

Inactive Publication Date: 2017-05-24
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN200980120221 provides a preparation method of Buvaracetam sustained-release tablet, but because the dissolution time is too long, the amount of drug released in a short time after taking the drug is too large, which is unfavorable for patients who need to take a large amount of medicament

Method used

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  • Sustained-release oral preparation of brivaracetam, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 The raw material of brivaracetam was pulverized by airflow, so that the particle size distribution range of more than 85% was less than 30 microns, and more than 99% was less than 50 microns, and was set aside. Weigh 50 grams of processed brivaracetam raw materials, 200 grams of lactose monohydrate, 25 grams of microcrystalline cellulose, and 12 grams of crospovidone according to 1000 tablets and mix them uniformly. Add an appropriate amount of 5% hypromellose as Prepare wet granules with binder, dry them, add 2 grams of magnesium stearate and 2 grams of micropowder silica gel after granulation, mix evenly, press into tablets, the pressure is controlled at 4.5kg to 10kg, and each tablet is about 300mg.

[0023] Hardness: 6.4kg

[0024] Appearance: ++++

Embodiment 2

[0026] The raw material of buvaracetam is pulverized by air flow, so that the particle size distribution range of more than 85% is less than 30 microns, and more than 99% is less than 50 microns, and is ready for use. Weigh 50 grams of processed brivaracetam raw materials, 150 grams of starch, 180 grams of microcrystalline cellulose, and 18 grams of sodium carboxymethyl starch according to 1000 tablets, mix evenly, and add an appropriate amount of starch slurry with a concentration of 10% as a binder Prepare wet granules, dry them, add 4 grams of magnesium stearate and 2 grams of micro-powdered silica gel after sizing, mix evenly, press into tablets, the pressure is controlled at 4.5kg to 10kg, and each tablet is about 423mg.

[0027] Hardness: 4.8kg

[0028] Appearance: +++ Example 3 The raw material of brivaracetam is jet-milled, so that the particle size distribution range of more than 85% is less than 30 microns, and more than 99% is less than 50 microns, and is set aside....

Embodiment 4

[0032] The raw material of buvaracetam is pulverized by air flow, so that the particle size distribution range of more than 85% is less than 30 microns, and more than 99% is less than 50 microns, and is ready for use. Weigh 150 grams of processed buvaracetam raw materials, 100 grams of hydroxypropyl cellulose, 110 grams of microcrystalline cellulose, 10 grams of starch, and 10 grams of crospovidone according to 1000 pieces and mix them evenly, and the concentration of addition is 5%. (W / V) povidone ethanol solution, appropriate amount is used as a binder to prepare wet granules, dry, add 6 grams of magnesium stearate and 2 grams of micropowder silica gel after granulation, mix evenly, press into tablets, and the pressure is controlled at 4.5kg~ 10kg, about 400mg per tablet.

[0033] Hardness: 7.1kg

[0034] Appearance: +++

[0035] Dissolution release test results

[0036]

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Abstract

The invention specifically relates to a sustained-release oral preparation of brivaracetam, and a preparation method thereof, belonging to the technical field of medicinal preparations containing organic effective components. The sustained-release oral preparation of brivaracetam is composed of brivaracetam, a filler, a disintegrating agent, a lubricant, a flow aid and a binder, wherein special treatment is carried out brivaracetam so as to allow brivaracetam to have an ultrafine particle size, 85% of the treated brivaracetam has a particle size of 30 [mu]m or below, 99% of the treated brivaracetam has a particle size of 50 [mu]m or below, and distribution is narrow, so the dissolvability, stability, dissolving-out and dissolving-out speed of the preparation are greatly improved. The sustained-release oral preparation of brivaracetam can be effectively and rapidly released without any cosolvent, so the bioavailability of brivaracetam is substantially improved; and the preparation method is suitable for large-scale production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations containing organic active ingredients, in particular to an oral sustained-release preparation of buvaracetam and a preparation method thereof. Background technique [0002] Epilepsy, commonly known as "shorn wind" or "epilepsy", is a chronic disease in which the sudden abnormal discharge of brain neurons leads to transient brain dysfunction. According to the latest epidemiological data in China, the overall prevalence rate of epilepsy in China is 7.0‰, the annual incidence rate is 28.8 / 100,000, and the prevalence rate of active epilepsy with seizures within one year is 4.6‰. Based on this, it is estimated that there are about 9 million epilepsy patients in China, of which 5 to 6 million are active epilepsy patients, and about 400,000 new epilepsy patients are added every year. In China, epilepsy has become the second most common disease in neurology after headache. sick. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/52A61K31/4015A61P25/08
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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