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Vigabatrin solid preparation and preparation method thereof

A technology of vigabatrin and solid preparations, applied in pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Active Publication Date: 2021-05-04
WUHAN WUYAO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Considering the important therapeutic effect of vigabatrin, the quality control of vigabatrin is very important, but in the prior art, there are few studies on impurity control of vigabatrin preparations

Method used

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  • Vigabatrin solid preparation and preparation method thereof
  • Vigabatrin solid preparation and preparation method thereof
  • Vigabatrin solid preparation and preparation method thereof

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Experimental program
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preparation example Construction

[0047] The present invention also provides a method for preparing vigabatrin tablets, the preparation method comprising: dissolving the adhesive in the first anhydrous alcohol solvent to obtain an adhesive solution; dissolving vigabatrin, filler, disintegrant etc. (also including alginic acid) are mixed with the binding solution, granulated, and dried to obtain dried granules; the dried granules and lubricant are mixed and compressed to obtain the described Vigabatrin tablets.

[0048] In some other embodiments of the present invention, the present invention provides a method for preparing a vigabatrin coated tablet, the preparation method comprising: dissolving the binder in the first anhydrous alcohol solvent, so as to obtain A binding solution; mixing vigabatrin, fillers, disintegrants, etc. (also including alginic acid) with the binding solution, granulating, and drying to obtain dried granules; The lubricant is mixed and pressed into tablets, so as to obtain vigabatrin t...

Embodiment 1

[0054] Embodiment 1 provides a vigabatrin film-coated tablet and a preparation method thereof, wherein the ingredients of the vigabatrin film-coated tablet are shown in Table 1 below:

[0055] Table 1 Composition of vigabatrin film-coated tablets

[0056]

[0057]

[0058] The preparation method of this vigabatrin film-coated tablet is as follows:

[0059] (1) According to Table 1, ethyl cellulose and povidone K30 were weighed and dissolved in wetting agent absolute ethanol to prepare a 10% by mass adhesive solution.

[0060] (2) According to Table 1, weigh the raw materials vigabatrin, microcrystalline cellulose, sodium carboxymethyl starch, and alginic acid and place them in a wet mixing granulator, mix for a few minutes until uniform, and then add the above-mentioned ethyl cellulose containing Adhesive solution of polyvinyl alcohol and povidone K30, cutting and stirring while adding to make soft material.

[0061] (3) Pass the prepared soft material through a 24-mes...

Embodiment 2

[0066] Embodiment 2 provides a vigabatrin film-coated tablet and a preparation method thereof, wherein the ingredients of the vigabatrin film-coated tablet are shown in Table 2 below:

[0067] Table 2 Composition of vigabatrin film-coated tablets

[0068]

[0069]

[0070] Preparation:

[0071] (1) According to Table 2, ethyl cellulose and povidone K30 were weighed and dissolved in anhydrous isopropanol as a wetting agent to prepare a binding solution with a mass percentage of 12%.

[0072] (2) According to Table 2, the raw materials vigabatrin, mannitol, sodium carboxymethyl starch, and alginic acid were weighed and placed in a wet mixing granulator, mixed for a few minutes until uniform, and then added the above-mentioned The bonding solution of povidone K30 is cut and stirred while adding to make soft materials.

[0073](3) Pass the prepared soft material through a 24-mesh sieve, granulate, and then put it into an oven at 45° C. for drying.

[0074] (4) Take out th...

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to avigabatrin solid preparation and a preparation method thereof. The preparation method of the hexenoic acid solid preparation comprises the following steps: dissolving an adhesive in a first anhydrous alcohol solvent to obtain an adhesive solution; and mixing the vigabatrin, pharmaceutically available auxiliary materials and the adhesive, performing granulation and drying to prepare the vigabatrin solid preparation. The invention further provides a vigabatrin solid preparation obtained according to the preparation method. The provided vigabatrin solid preparation or the vigabatrin solid preparation prepared according to the provided preparation method has good stability, low impurity A content and low total impurity content.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a vigabatrin solid preparation and a preparation method thereof. Background technique [0002] Epilepsy is a disease characterized by central nervous system dysfunction caused by recurrent abnormal discharge of neurons. It is one of the common clinical diseases and frequently-occurring diseases, which seriously affects the daily life of patients. While traditional antiepileptic drugs can control most of the epilepsy, but 20-30% can not be effectively controlled. [0003] Vigabatrin, whose chemical name is 4-amino-5-hexenoic acid, selectively inhibits γ-aminobutyric acid (GABA) transaminase, thereby increasing the concentration of GABA in the brain and producing antiepileptic effects. In 2009, vigabatrin was designated by the FDA as an adjuvant drug for the treatment of infantile spasms and partial complex seizures of adult refractory epilepsy, which is a drug for rare ...

Claims

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Application Information

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IPC IPC(8): A61K31/197A61K9/36A61K47/38A61K47/36A61P25/08A61P21/02
CPCA61K31/197A61K9/2866A61K9/2059A61P25/08A61P21/02
Inventor 张美娜王亚军冯小路郭婷婷殷晶莉杨波
Owner WUHAN WUYAO SCI & TECH