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Vonoprazan fumarate solid dispersions and preparation method thereof

A technology for vonoprazan fumarate and solid dispersion, which is applied in the field of vonoprazan fumarate solid dispersion and tablets thereof, can solve the problems of poor water solubility, low bioavailability and the like, and achieves reduction in dosage, The preparation process is simple and the effect of improving the dissolution rate in vitro

Inactive Publication Date: 2017-12-22
SUZHOU XINEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The currently commercially available vonoprazan fumarate only has ordinary tablets, because the water solubility of fumaric acid vonoprazan is poor and the bioavailability is low, so the raw materials of the commercially available ordinary tablets for oral administration need to be crushed into smaller granules. to increase the solubility

Method used

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  • Vonoprazan fumarate solid dispersions and preparation method thereof
  • Vonoprazan fumarate solid dispersions and preparation method thereof
  • Vonoprazan fumarate solid dispersions and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: 1000 pieces of specifications

[0034] prescription:

[0035] Ingredients Dosage per tablet (mg)

[0036] Vonoprazan Fumarate 13

[0037] Polyvinylpyrrolidone K30 30

[0038] Mannitol 170

[0039] Sodium starch glycolate 7

[0040] Magnesium stearate 3

[0041] Preparation method:

[0042] (1) Take 1300mg of vonoprazan fumarate, add it to 100ml of organic solvent, dissolve it by ultrasonic, weigh PVP K30, add 30000mg to the above organic solvent, and dissolve it by ultrasonic. Place the organic solution on a rotary evaporator at 55-60°C to evaporate the organic solvent under reduced pressure, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of vonoprazan fumarate.

[0043] (2) Weigh the prescribed amount of mannitol, sodium carboxymethyl starch, and magnesium stearate, mix them evenly, and then compress into tablets.

Embodiment 2

[0044] Embodiment 2: 1000 pieces of specifications

[0045] prescription:

[0046] Ingredients Dosage per tablet (mg)

[0047] Vonoprazan Fumarate 13

[0048] Polyvinylpyrrolidone K30 33

[0049] Lactose 170

[0050] Croscarmellose Sodium 7

[0051] Magnesium stearate 3

[0052] Preparation method:

[0053] (1) Take 13000mg of vonoprazan fumarate, add it to 200ml of organic solvent, dissolve it by ultrasonic, weigh PVP K30, add 33000mg to the above organic solvent, and dissolve it by ultrasonic. Place the organic solution on a rotary evaporator at 55-60°C to evaporate the organic solvent under reduced pressure, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of vonoprazan fumarate.

[0054] (2) Weigh the prescribed amount of mannitol, lactose, croscarmellose sodium, and magnesium stearate, mix well, and then compress into tablets.

Embodiment 3

[0055] Embodiment 3: 1000 pieces of specifications

[0056] prescription:

[0057] Ingredients Dosage per tablet (mg)

[0058] Vonoprazan Fumarate 13

[0059] Poloxamer 30

[0060] Microcrystalline Cellulose 170

[0061] Povidone 7

[0062] Talc powder 3

[0063] Preparation method:

[0064] (1) Take 13,000 mg of vonorazan fumarate, add it to 100 ml of organic solvent, and dissolve it by ultrasonication, weigh 30,000 mg of poloxamer, add it to the above organic solvent, and dissolve it by ultrasonication. Place the organic solution on a rotary evaporator at 55-60°C to evaporate the organic solvent under reduced pressure, dry the product in a vacuum oven for 24 hours, pulverize, grind and sieve to obtain a solid dispersion of vonoprazan fumarate.

[0065] (2) Weigh the prescribed amount of mannitol, microcrystalline cellulose, povidone, talcum powder, mix well, and then press

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Abstract

The invention discloses a preparation method of vonoprazan fumaric acid solid dispersion: dissolve vonoprazan fumaric acid and a carrier material in an organic solvent (acetone:methane=3:1), and reduce the temperature at 50 to 90°C. Pressure rotary evaporation, to obtain; the mass ratio of the fumaric acid vonoprazan to the carrier material is 1:1.5~1:10; the carrier material is selected from one of polyvinylpyrrolidone K30 and poloxamer or two. The present invention also provides a solid dispersion tablet of vonoprazan fumarate: made of solid dispersion of vonoprazan fumarate, filler, disintegrant, lubricant, wherein, the amount of filler accounts for 35%-65% of the total weight of the tablet; the dosage of the disintegrating agent is 1%-5% of the total weight of the tablet; the dosage of the lubricant is 0.5%-3% of the total weight of the tablet. The vonoprazan fumarate solid dispersion and tablet of the present invention improve the dissolution rate of vonoprazan fumarate in vitro, and improve the disadvantages of poor oral absorption and low bioavailability.

Description

technical field [0001] The invention relates to a solid dispersion of vonoprazan fumarate, a tablet thereof, and a preparation method. The medicine of the invention is used for treating and maintaining non-erosive gastroesophageal reflux disease, duodenal ulcer, gastric ulcer, erosive esophagitis and other acid-related diseases. Background technique [0002] Vonoprazan fumarate (formula below), the chemical name is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N - Methylmethylamine fumarate, which belongs to a new type of PPI-potassium ion competitive acid blocker [0003] (Potassium-competitive acid blockers, P-CAB), by competitively inhibiting hydrogen ion / potassium ion-ATP [0004] It acts on potassium ions in the enzyme and is a reversible potassium ion antagonist. Compared with traditional PPIs, the acid suppression effect of vonoprazan fumarate has nothing to do with the activation of proton pumps, and it can significantly reduce the occurrence of n...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/32A61K47/10A61K31/4439A61K9/20A61P1/04
CPCA61K31/4439A61K9/146A61K9/2027A61K9/2054A61K9/2059
Inventor 居丽娜
Owner SUZHOU XINEN PHARMA
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