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Vonoprazan fumarate enteric-coated composition and preparation method thereof

A technology of vonoprazan fumarate and enteric-coated layer, which is applied in the field of medicine, can solve problems such as unstable release of vonoprazan fumarate, and achieve the goal of improving bioavailability, increasing stability, and reducing adverse reactions Effect

Active Publication Date: 2015-11-11
DISHA PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Purpose of the invention: To provide a stable release vonoprazan fumarate preparation and its preparation method to solve the problem of unstable release of vonoprazan fumarate

Method used

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  • Vonoprazan fumarate enteric-coated composition and preparation method thereof
  • Vonoprazan fumarate enteric-coated composition and preparation method thereof
  • Vonoprazan fumarate enteric-coated composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 prescription:

[0028]

[0029] Preparation Process:

[0030] Preparation of Blank Ball Cores

[0031] Crush the sucrose and pass through an 80-mesh sieve. Under the condition of high-speed rotation in the centrifugal granulator, gradually spray the adhesive made by adding sucrose, then pass through a 50-mesh sieve, collect the wet blank sugar pellets, and then dry them;

[0032] Drug-containing layer preparation:

[0033] Slowly add hypromellose under stirring in purified water, add vonoprazan fumarate after dissolution is complete, add purified water to the required amount, stir evenly, pass through a 60-mesh sieve to obtain the coating solution, and blank The ball core is placed in a fluidized bed coating device to carry out bottom spraying and drug coating, drying, and passing through a 40-mesh sieve to obtain micro-pills of the main drug layer;

[0034] Isolation layer preparation:

[0035] Slowly add hypromellose under stirring in purified wat...

Embodiment 2

[0040] Example 2 Preparation of Vonorazan Fumarate Enteric-Coated Capsules

[0041]

[0042] The preparation of pellets and determination of the content of the active substance vonoprazan fumarate were the same as in Example 1, and they were filled into capsules with a specification of 20 mg.

Embodiment 3

[0043] Example 3 Preparation of Vonorazan Fumarate Enteric-Coated Capsules

[0044]

[0045] The preparation of pellets and determination of the content of the active substance vonoprazan fumarate were the same as in Example 1, and they were filled into capsules with a specification of 15 mg.

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Abstract

The invention relates to a vonoprazan fumarate enteric-coated capsule and a preparation method thereof, particularly relates to a pellet type vonoprazan fumarate enteric-coated capsule and a preparation method thereof, and belongs to the technical field of medicines. The vonoprazan fumarate enteric-coated capsule sequentially comprises a hollow pill core, a main drug layer, an isolation layer, an enteric layer and a capsule layer from inside to outside, wherein the weight of the main drug layer is 80-130 percent of that of the hollow pill core, the weight of the isolation layer is 10-30 percent of the total weight of the hollow pill layer and the main drug layer, and the weight of the enteric layer is 30-80 percent of the total weight of the hollow pill layer, the main drug layer and the isolation layer. Each capsule contains 10-20mg of vonoprazan. By adopting the technical scheme, the dispersion of vonoprazan fumarate is improved, and the dissolution rate is increased.

Description

technical field [0001] The invention relates to a vonoprazan fumaric acid enteric-coated composition and a preparation method thereof, in particular to a pellet-shaped vonoprazan fumaric acid capsule and a preparation method thereof, which belong to the technical field of medicine. Background technique [0002] Vonoprazan fumarate, its chemical name is: 1-[5-(2-fluorophenyl)-1-(pyridine-3-sulfonyl)-1H-pyrrol-3-yl]-N-methyl Methylamine fumarate, molecular formula: C 17 h 16 FN 3 o 2 S·C 4 h 4 o 4 , molecular weight: 461.4. The chemical formula is shown in formula I. [0003] Formula I [0004] Vonoprazan fumarate belongs to a new class of inhibitors of potassium ion (K) competitive acid blockers (P-CAB), which has a strong and long-lasting inhibitory effect on gastric acid secretion. In one step, it also has an early termination effect on gastric acid secretion by inhibiting the binding effect of K on H,K-ATPase (proton pump). For erosive esophagitis, gastric ulc...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/16A61K31/4439A61P1/04A61P31/04
Inventor 祁伟力白莉高飞邹韬博
Owner DISHA PHARMA GRP
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