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Preparation comprising vonoprazan

A preparation technology of vonoprazan fumarate, which is applied to medical preparations containing active ingredients, medical preparations without active ingredients, pill delivery, etc., and can solve problems such as hindering rapid dissolution

Pending Publication Date: 2020-02-21
TAKEDA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when the pharmaceutical active ingredient has a strong bitter taste, the thick coating that masks this bitter taste hinders rapid dissolution, making it difficult to achieve both effects at the same time

Method used

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  • Preparation comprising vonoprazan
  • Preparation comprising vonoprazan
  • Preparation comprising vonoprazan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0195] Preparation of compound A coating solution

[0196] To purified water (399.8 g) was added hypromellose 2910 (also known as hypromellose (2910), TC-5E, manufactured by Shin-Etsu Chemical Co., Ltd., the same below) (24.3 g), adding Compound A (180.3 g), and fully stirring the mixture to obtain Compound A coating solution.

[0197] Preparation of Compound A Coated Particles

[0198] Lactose / crystalline cellulose spherical granules (NONPAREIL 105T, manufactured by Freund Corporation, hereinafter the same) (300.5 g) were placed in a microparticle coating granulator / Wurster (FD-MP-01 (SPC / SFP / FD), produced by POWREX Manufacturing, hereinafter the same) and fluidized therein; Compound A coating liquid (570.0g) was sprayed under the following conditions: the spray air pressure was 0.5MPa, the spray air flow rate was 60NL / min, and the inlet air temperature was 65-75 ℃, the inlet air velocity is 0.4-0.5m 3 / min, the spray liquid feed rate is 5g / min; the particles are dried...

Embodiment 2

[0211] Preparation of compound A coating solution

[0212] Hydroxypropylmethylcellulose 2910 (24.21g) was dissolved in purified water (399.8g) to obtain a hydroxypropylmethylcellulose solution. Next, compound A (180.0 g) was uniformly dispersed in the hydroxypropylmethylcellulose solution to obtain a compound A coating solution.

[0213] Preparation of organic acid coating solution

[0214] Hydroxypropylmethylcellulose 2910 (33.59g) was dissolved in purified water (673.9g) to obtain a hydroxypropylmethylcellulose solution. Next, the previously spray-milled fumaric acid (100.8 g) was suspended in the hydroxypropyl methylcellulose solution to obtain an organic acid coating liquid.

[0215] Preparation of Organic Acid Coated Particles

[0216] Lactose / crystalline cellulose spherical granules (300.0 g) were placed in a microparticle coating granulator / Wurster and fluidized therein; the compound A coating solution (555.0 g) was sprayed under the following conditions: spray...

Embodiment 3

[0226] Preparation of water-insoluble polymer-coated particles

[0227] In the preparation step of the water-insoluble polymer-coated particles of Example 2, sampling was performed while spraying the water-insoluble polymer coating liquid (225.0 g), and sprayed particles (3.4 g) were obtained. Next, the sprayed particles were dried and cured in a forced convection constant temperature oven at 60° C. for 14 hours. The dried and solidified particles were sieved with a sieve with a pore size of 350 μm to obtain sieved particles, that is, particles coated with a water-insoluble polymer.

[0228] Preparation of orally disintegrating tablets comprising particles coated with a water-insoluble polymer

[0229] Water-insoluble polymer-coated particles (1076.9 mg), outer layer particles obtained in Example 2 (2523.0 mg), aspartame (21.0 mg), l-menthol (13.1 mg), acesulfame Potassium (5.3 mg), sodium stearyl fumarate (31.5 mg), strawberry essence (4.2 mg), and crystalline cellulose...

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Abstract

The present invention aims to provide a preparation expected, to improve the bitter taste of an organic acid salt of vonoprazan and permit rapid dissolution of the organic acid salt of vonoprazan after administration. The present invention provides a preparation containing fine granules or granules containing (1) a core granule containing an organic acid salt of vonoprazan, (2) an intermediate layer containing the same organic acid as the organic acid forming the salt of vonoprazan in (1), or a salt thereof, and (3) a coating layer containing a water-insoluble polymer.

Description

technical field [0001] The present invention relates to a preparation which can improve the bitterness of the organic acid salt of vonoprazan. Background technique [0002] With the aging of the population and changes in the living environment, it is required to develop an orally disintegrating tablet that can be easily taken without water anytime and anywhere and that can maintain the ease of handling that characterizes the tablet. [0003] When the pharmaceutical active ingredient or other additive is a substance having an unpleasant taste such as bitterness or the like, it is preferable to mask such an unpleasant taste by coating it from the viewpoint of medication compliance. On the other hand, it is desired that a pharmaceutically active ingredient dissolves rapidly after administration to express a pharmacological effect. However, when the pharmaceutical active ingredient has a strong bitter taste, the thick coating that masks this bitter taste hinders rapid dissoluti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/20A61K9/50A61K31/4439
CPCA61K9/0056A61K9/2018A61K9/2054A61K9/2081A61K9/5026A61K9/5078A61K31/4439A61K9/2846A61K9/2013A61K9/2886A61K9/14A61K9/2027A61K47/12
Inventor 藤井博之铃木彰
Owner TAKEDA PHARMA CO LTD