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Brivaracetam controlled-release preparation and preparation method thereof

A technology of membrane control and excipient, applied in the field of anti-epileptic drug briracetam controlled-release tablet and its preparation, can solve the problems of solvent residual environment and pollution, etc.

Inactive Publication Date: 2020-07-14
JIANGSU ALICORN PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Traditional single-chamber osmotic pump tablets are coated with rigid semi-permeable membrane coating materials such as cellulose acetate and ethyl cellulose. There is no need to use acetone and ethanol organic solvents during the coating process, which will cause solvent residues and environmental pollution.

Method used

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  • Brivaracetam controlled-release preparation and preparation method thereof
  • Brivaracetam controlled-release preparation and preparation method thereof
  • Brivaracetam controlled-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Cellulose acetate as film-forming material

[0028]

[0029] Process:

[0030] (1) After pre-mixing polyoxyethylene as a hydrophilic matrix with mannitol for 5 minutes, add the bulk drug of crystal form A and mix for 5 minutes, then add talc powder and magnesium stearate in sequence, mix for 2 minutes and 1 minute respectively, and press into tablets. That is the tablet core.

[0031] (2) Add polyethylene glycol and cellulose acetate in sequence to the acetone solution, stir and dissolve to obtain a semi-permeable membrane coating solution.

[0032] (3) Place the tablet core in a high-efficiency coating machine for semi-permeable membrane coating, spray pressure 0.1mPa, host speed 10rpm, air inlet temperature 35-40°C, material temperature 28-32°C, liquid spray rate 4-40°C 6g / min, take out the coated tablet when the coating weight gain reaches 5%, place it in a 40°C oven for static aging for 24 hours, and punch a hole in the center of the front of the coated special-s...

Embodiment 2

[0034] Acrylic resin polymer as film-forming material

[0035]

[0036] Process:

[0037] (1) After premixing hypromellose as a hydrophilic matrix with sorbitol and microcrystalline cellulose for 5 minutes, add the raw material drug of crystal form A and mix for 5 minutes, and then add colloidal silicon dioxide and magnesium stearate in sequence , mixed for 2 minutes and 1 minute respectively, and pressed into tablets to obtain tablet cores.

[0038] (2) Pour talcum powder and triethyl citrate into water, homogenize with a high-shear homogenizer, pour into Eudragit RL30D / RS30D water dispersion before use, and filter through a 40-mesh sieve. Stir continuously during the coating process to obtain a semi-permeable membrane coating solution.

[0039] (3) Place the tablet core in a high-efficiency coating machine for semi-permeable membrane coating, spray pressure 0.1mPa, host speed 10rpm, air inlet temperature 35-40°C, material temperature 28-32°C, liquid spray rate 4-40°C 6...

Embodiment 3

[0040] Embodiment 3 Drug release hole position research

[0041] Using the prescription process in Example 2, holes were respectively punched on the side of the short axis and the side of the long axis of the coated special-shaped tablet (12.6*5.4 mm), with a hole diameter of 0.6 mm.

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PUM

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Abstract

The invention relates to a brivaracetam oral controlled-release preparation and a preparation method thereof. The controlled-release preparation is a single-chamber osmotic pump controlled-release preparation, and is composed of a drug tablet core, a membrane-controlled coating system and a drug-release hole. The drug tablet core comprises 30-60wt% of brivaracetam, and the membrane-controlled coating accounts for 3-8 (w / w, %) of the total preparation. The controlled-release preparation disclosed by the invention has an in-vitro zero-level constant-speed drug release curve, can form a sphericalpreparation after water absorption swelling, and is not prone to being adhered to the wall of a digestive tract to cause too high local drug concentration.

Description

technical field [0001] The invention relates to an antiepileptic drug briracetam controlled-release tablet and a preparation method thereof, which can be used for adjuvant treatment of partial seizures with or without secondary generalized seizures in adults and adolescent epilepsy patients aged 16 and above. Background technique [0002] Briracetam is a racetam derivative with extensive antiepileptic activity and high safety. The drug can exert antiepileptic effect by binding to synaptic vesicle protein 2A (SV2A). More than 3,000 people have participated in clinical trials of brivaracetam, and provided some patients with more than 8 years of clinical experience. In 2016, it was approved for marketing in the European Union and the US FDA. The trade name is: BRIVIACT, a third-generation new epilepsy drug (levetiracetam and lacosamide) designed and developed by UCB Pharm in Belgium. International Patent Application Publication No. WO 01 / 62726 discloses 2-oxo-1-pyrrolidine der...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/44A61K9/36A61K9/32A61K31/4015A61P25/08
CPCA61K31/4015A61K9/2072A61K9/2018A61K9/2866A61K9/284A61P25/08
Inventor 舒欣陆平波高超
Owner JIANGSU ALICORN PHARMATECH CO LTD
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