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Solid preparation with high stability and quick release, and preparation method thereof

A technology of solid preparation and diluent, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc. , low production efficiency and other problems, to achieve the effect of reduced water absorption, high production efficiency, and increased release speed

Active Publication Date: 2019-12-06
YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this patent uses wet granulation to have adverse effects on the active components of the drug (such as vonoprazan fumarate) under high temperature and high humidity conditions, reducing the stability of the obtained solid preparation and the purity of the active component of the drug.
Moreover, wet granulation needs to preheat the granulation first, and then spray the solution of chain organic acid. The process is complicated, the production efficiency is low, and it is not convenient for industrial production.

Method used

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  • Solid preparation with high stability and quick release, and preparation method thereof
  • Solid preparation with high stability and quick release, and preparation method thereof
  • Solid preparation with high stability and quick release, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 prepares sample 1

[0040] The composition ratio shown in Table 1 was used to prepare film-coated tablets containing vonoprazan fumarate.

[0041] The preparation method is: put fumaric acid vonoprazan (2156.2g) and fumaric acid (443.8g) into a single-arm mixer (model HSD-50, manufactured by Zhejiang Canaan Technology Co., Ltd.) and mix uniformly to obtain mixture H. Get 360g of the mixture H powder and adopt a jet mill (YQ50A, manufactured by Shanghai Zhikai Machinery) to pulverize, and the pulverization pressure is 0.40Mpa to obtain pulverized powder A co- pulverized by the sieved fumaric acid vonoprazan and fumaric acid. Co-grind powder A (322.2g), mannitol (1459.8g), microcrystalline cellulose (220g), hydroxypropyl cellulose (66g), croscarmellose sodium (110g), magnesium stearate ( 22 g) into a single-arm mixer (model HSD-50, manufactured by Zhejiang Canaan Technology Co., Ltd.) and mix evenly to obtain a mixed powder. Adopt rotary tabletting machine ...

Embodiment 2

[0047] Embodiment 2 prepares sample 2

[0048] The composition ratios shown in Table 2 were used to prepare film-coated tablets containing vonoprazan fumarate.

[0049] The preparation method is as follows: take 360 ​​g of the mixture H powder in Example 1 and use a jet mill (YQ50A, manufactured by Shanghai Zhikai Machinery) to pulverize, and the pulverization pressure is 0.25Mpa to obtain pulverized and sieved fumaric acid vonorazan and fumaric acid Malic acid co-grinds powder B, co-grinds powder B (322.2g), mannitol (1459.8g), microcrystalline cellulose (220g), hydroxypropyl cellulose (66g), croscarmellose sodium ( 110g), magnesium stearate (22g) were put into a single-arm mixer (model HSD-50, manufactured by Zhejiang Canaan Technology) and mixed evenly to obtain a mixed powder. Adopt rotary tabletting machine (model ZP10A, Beijing Sinopharm Longli manufacture), use 11*6mm ellipse punching die, the mixed powder is compressed into plain tablet tablet. Adopt high-efficiency ...

Embodiment 3

[0055] Embodiment 3 prepares sample 3

[0056] The composition ratio shown in Table 3 was used to prepare film-coated tablets containing vonoprazan fumarate.

[0057] The preparation method is as follows: take 360 ​​g of the mixture H powder in Example 1 and use a jet mill (YQ50A, manufactured by Shanghai Zhikai Machinery) to pulverize with a pulverization pressure of 0.20 Mpa to obtain pulverized and sieved fumaric acid vonoprazan and fumaric acid Malic acid co-grinds powder C, co-grinds powder C (322.2g), mannitol (1459.8g), microcrystalline cellulose (220g), hydroxypropyl cellulose (66g), croscarmellose sodium ( 110g), magnesium stearate (22g) were put into a single-arm mixer (model HSD-50, manufactured by Zhejiang Canaan Technology) and mixed evenly to obtain a mixed powder. Adopt rotary tabletting machine (model ZP10A, Beijing Sinopharm Longli manufacture), use 11*6mm ellipse punching die, the mixed powder is compressed into plain tablet tablet. Adopt high-efficiency co...

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Abstract

The invention discloses a solid preparation. The solid preparation is prepared from the following raw materials: co-pulverized powder, and excipients; and the co-pulverized powder is prepared by the steps of mixing active pharmaceutical ingredients with an organic acid, and carrying out co-pulverizing. Test results have proven that, film coated tablets containing vonoprazan fumarate prepared by the steps of co-pulverizing vorolazan fumarate and an organic acid so as to obtain co-pulverized powder with specific particle size distribution, mixing the co-pulverized powder with remaining excipients and carrying out direct tablet pressing have the beneficial effects of being improved in stability and purity, reduced in water absorption rate, and accelerated in active drug release rate. In addition, the preparation method of the solid preparation is simple in process, high in production efficiency and suitable for industrial use.

Description

technical field [0001] The invention belongs to the field of pharmaceutical engineering, and in particular relates to a high-stability, fast-release solid preparation and a preparation method thereof. Background technique [0002] Vonoprazan Fumarate, the molecular formula is: C17H16FN3O2S C4H4O4, the chemical name is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrole -3-yl]-N-methylmethylamine or its salt, or N-methyl-1-[5-(2-methylphenyl)-1-(pyridin-3-ylsulfonyl)-1H- Pyrrol-3-yl] methylamine fumarate (see the figure below for the structural formula). Developed by Takeda Pharmaceutical Co., Ltd., Japan, it is a kind of pyrrole derivative potassium-accumulating competitive acid blockers (P-CABs), which bind gastric H by competing with potassium ions + / K + -ATPase (proton pump) and inhibit its activity, thereby playing a role in inhibiting gastric acid secretion. Japan Takeda Pharmaceutical Co., Ltd. has applied for a compound patent, patent number ZL200680040789....

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/36A61K47/12A61K31/4439A61P1/04
CPCA61K9/145A61K9/2866A61K9/2013A61K31/4439A61P1/04
Inventor 梁力徐小伟胡彦霞刘畅张超
Owner YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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