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A kind of vonoprazan fumarate composition and its preparation method

A technology of vonoprazan fumarate and citric acid, which is applied in the direction of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problem of not achieving the sterilization effect, not obtaining, not adding fumarate vonoprazan Issues such as technical means and effects

Active Publication Date: 2019-03-01
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Prior art CN 201410154778.8 discloses the new water-soluble organic acid salt of Wonorazan and the injection of the water-soluble organic acid salt and its preparation method, but this type of new water-soluble organic acid salt and the active ingredient fuma Compared with vonoprazan fumarate, its effect has not been supported by clinical experiments and pharmaceutical practice, and there is no technical means and effect to increase the water solubility of vonoprazan fumarate, and the injection uses 100 ° C steam Sterilize for 30 minutes. This method is not terminal sterilization and cannot achieve a better sterilization effect.

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  • A kind of vonoprazan fumarate composition and its preparation method
  • A kind of vonoprazan fumarate composition and its preparation method
  • A kind of vonoprazan fumarate composition and its preparation method

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specific Embodiment approach

[0081] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0082] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0083] In the present invention, min means minute, h means hour, mg means milligram, g means gram, mL means milliliter, W means weight, and V means volume.

Embodiment 1

[0084] Example 1: Solubilization of Vonoprazan Fumarate Using Hydroxypropyl-β-Cyclodextrin (HP-β-CD).

[0085] Add a certain volume (about 75% of the final volume of the solution) of purified water into the beaker, add hydroxypropyl-β-cyclodextrin, stir and dissolve with a magnetic stirrer; after the hydroxypropyl-β-cyclodextrin dissolves, , add voronoprazan fumarate, stir, visually observe the dissolution of voronoprazan fumarate, stir until voronoprazan fumarate is completely dissolved; add purified water to make up to 20 mL. A short-term stability study was carried out on the solution (the stability storage condition is to first place the sample at 40° C. for a certain period of time, and then place the sample at 60° C. for a certain period of time). The prescription is shown in Table 1-1.

[0086] Table 1-1

[0087]

[0088] Results of Example 1: After stirring for 20 minutes, the API was completely dissolved. The results of short-term stability studies confirmed tha...

Embodiment 2

[0092] Example 2: Different dosages of HP-β-CD solubilized vonoprazan fumarate.

[0093] Add a certain volume (about 75% of the final volume of the solution) of purified water into two beakers, add different amounts of HP-β-CD respectively, stir and dissolve with a magnetic stirrer; after the HP-β-CD dissolves, Add voronoprazan fumarate, stir, visually observe the dissolution of voronoprazan fumarate, stir until voronoprazan fumarate is completely dissolved; add purified water to make up to 20mL. See Table 2-1 and 2-2 for the prescription.

[0094] table 2-1

[0095]

[0096] Table 2-2

[0097]

[0098] Results of Example 2: When the amount of HP-β-CD is 240 mg, that is, when the mass ratio to API is 3:1, the API is added to the HP-β-CD solution, stirred for 60 minutes, and the API is completely dissolved; when the HP-β-CD The dosage is 400mg, that is, when the mass ratio of API to API is 5:1, API is added to HP-β-CD solution, stirred for 20min, and API is completely ...

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Abstract

The invention relates to a vonoprazan fumarate composition and a preparing method thereof. The composition includes vonoprazan fumarate, a solubilizer, a buffer agent, a pH adjusting agent and a solvent, wherein the solubiliser can significantly increase solubility of the vonoprazan fumarate, stability of the composition is good, and stability of the composition is not obviously changed after the buffer agent and the pH adjusting agent are added. In addition, the preparing method of the vonoprazan fumarate composition is also provided. The method is simple, economical and suitable for industrial production.

Description

technical field [0001] The invention relates to a fumaric acid vonoprazan composition, in particular to a safe and stable fumaric acid vonoprazan composition containing substituted β-cyclodextrin and a preparation method thereof, belonging to the technical field of pharmacy. Background technique [0002] Vonoprazan fumarate (Vonoprazan fumarate) used to be code-named TAK-438, which is a new type of gastric acid secretion inhibitor developed by Takeda Corporation of Japan. In the final step of secretion, by inhibiting the K + to H + -K + - The combination of ATPase (proton pump) also has an early termination effect on gastric acid secretion. Vonorazan fumarate was first launched in Japan in 2014 under the trade name Takecab. [0003] The chemical name of vonoprazan fumarate is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylformazan Amine fumaric acid monosalt, the structural formula is as follows: [0004] [0005] Currently, the marketed dosa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/4439A61K47/69A61P1/04
CPCA61K9/0019A61K9/08A61K31/4439
Inventor 牟丽秋赵步文黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD