Pregabalin sustained-release tablet medicinal composition and preparation method thereof

A technology of pregabalin and its composition, which is applied in the field of medicine, can solve the problems of uneven appearance of tablets, affecting the quality of sustained-release tablets, rough edges of tablets, etc., and achieves improved drug stability, simple composition, and simple and easy process Effect

Inactive Publication Date: 2017-05-03
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since pregabalin is an amino acid derivative (three-position isobutyl substitution of γ-aminobutyric acid) and is easily soluble in water, starch, dextrin or purified water for starch dextrin are mostly used in traditional wet granulation. Dissolving and punching slurry is used as binding agent, easily causes mold sticking in tablet process, causes the edge roughness of tablet or has flaw, has a strong impact on sustained-release tablet quality (the inventor attempts to use the prescription that above-mentioned CN101663025A, CN1857244A, CN103585098A disclose Such problems have occurred in the preparation of pregabalin sustained-release tablets and methods, and the tablet appearance is uneven, bright and clean)

Method used

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  • Pregabalin sustained-release tablet medicinal composition and preparation method thereof
  • Pregabalin sustained-release tablet medicinal composition and preparation method thereof
  • Pregabalin sustained-release tablet medicinal composition and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0039] Pregabalin Sustained Release Tablet Pharmaceutical Composition Prescription Composition: Pregabalin 1000g, Methylcellulose A4C 1350g, Methylcellulose SM-100 750g, Lactose 5500g, Mannitol 100SD 2000g, Silicon Dioxide 30g, Magnesium Stearate 30g, film coating powder (stomach-soluble type) 56g.

[0040]Preparation:

[0041] (1) Put methylcellulose A4C, methylcellulose SM-100, lactose, and pregabalin into a three-dimensional rocking mixer, control the speed at 10 rpm, and mix for about 20 minutes;

[0042] (2) Put silicon dioxide and magnesium stearate into the above-mentioned three-dimensional rocking mixer, control the rotating speed at 10 rpm, and continue mixing for about 5 minutes;

[0043] (3) Use ZP33 rotary tablet press, Φ8.5mm circular concave punching tablet;

[0044] (4) The film coating powder (stomach-soluble type) purchased from Shanghai Colorcon Coating Technology Co., Ltd. is added to the stirred 30% ethanol solution to form a film-coating powder (stomach-...

Embodiment 2

[0048] Prescription composition: Pregabalin 825g, hypromellose K100M 3000g, carbomer 971P 400g, mannitol 200SD2825g, microcrystalline cellulose PH102 2800g, magnesium stearate 150g.

[0049] Preparation:

[0050] (1) Mix 400g Carbomer 971P and 400g Hypromellose K100M in a mixer for about 3 minutes, and pass through a 18-20 mesh sieve;

[0051] (2) Put the mixed material of Carbomer 971P and hypromellose K100M, microcrystalline cellulose PH102, remaining hypromellose K100M, pregabalin, and mannitol 200SD into the three-dimensional shaking mixer, and control the speed at 10 rpm / min, mixing for about 20 minutes;

[0052] (3) Magnesium stearate is dropped into the above-mentioned three-dimensional rocking mixer, and the control speed is 10 rpm, and the mixture is continued for about 5 minutes;

[0053] (4) Tablets were compressed with a rotary tablet press, the die was a 20.5×10.5mm special-shaped punch, the tablet weight was controlled within ±4% of the theoretical tablet weig...

Embodiment 3

[0057] Prescription composition: Pregabalin 1650g, Hypromellose K100M 1500g, Hypromellose E50 1500g, Carbomer 971P 400g, Mannitol 200SD 2000g, Microcrystalline Cellulose PH102 2800g, Magnesium Stearate 150g.

[0058] Preparation:

[0059] (1) Mix 400g Carbomer 971P and 400g Hypromellose K100M in a mixer for about 3 minutes, and pass through a 18-20 mesh sieve;

[0060] (2) Put the mixture of carbomer 971P and hypromellose K100M, microcrystalline cellulose PH102, hypromellose E50, remaining hypromellose K100M, pregabalin, and mannitol 200SD into three-dimensional shaking and mixing In the machine, control the speed at 10 rpm, and mix for about 20 minutes;

[0061] (3) Magnesium stearate is dropped into the above-mentioned three-dimensional rocking mixer, and the control speed is 10 rpm, and the mixture is continued for about 5 minutes;

[0062] (4) Tablets were compressed with a rotary tablet press, the die was a 20.5×10.5mm special-shaped punch, the tablet weight was control...

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Abstract

The invention provides a pregabalin sustained-release tablet medicinal composition and a preparation method of the pregabalin sustained-release tablet medicinal composition. The composition is prepared from the following components in parts by weight: 10-80 parts of pregabalin, 20-80 parts of a sustained-release material, 70-140 parts of a filler, 1-6 parts of a lubricant, and 1-5 parts of film coating powder. The preparation method comprises the following steps: mixing the components, carrying out direct tabletting, and carrying out coating, thus obtaining the sustained-release tablet. For the composition provided by the invention, the auxiliary materials are simple in composition, the powder is good in flowability and strong in adhesion resistance, during tabletting, the adhesion to the mould can not be caused, the process is simple, convenient and feasible, the cost is low, and the method is suitable for industrial production.

Description

technical field [0001] The invention relates to a pregabalin sustained-release tablet pharmaceutical composition and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] The chemical name of pregabalin ((s)-3-(aminomethyl)-5-methylhexanoic acid) is a new type of γ-aminobutyric acid (GABA) receptor agonist, which can block It can block voltage-dependent calcium channels and reduce the release of neurotransmitters. It is mainly used clinically for the treatment of peripheral neuralgia and auxiliary treatment of localized partial seizures. [0003] Only pregabalin capsules are currently on the market for this product, which is mainly used for the treatment of neuralgia and adjuvant treatment of epilepsy. Pregabalin has a relatively short half-life (about 6 hours), and it is administered multiple times a day, which will cause significant fluctuations in the blood drug concentration of the drug. Frequent dosing is necessary t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/22A61K31/197A61K47/38A61K47/32A61P25/02A61P25/08
Inventor 陈九龙赵亮
Owner SICHUAN HAISCO PHARMA CO LTD
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