Esomeprazole drug-containing pellet composition and preparation method thereof

A technology of esomeprazole and esomeprazole magnesium, which is applied in the field of esomeprazole drug-containing pellet composition and its preparation, can solve the problem of stabilizers increasing the complexity of the formula, easily causing allergies, and slow dissolution and other problems, to achieve significant gastric acid inhibition, ensure safety and effectiveness, and high dissolution rate

Active Publication Date: 2014-05-28
SINOPHARM ZHIJUN (SHENZHEN) PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the addition of stabilizers increases the complexity of the formula, which can easily cause adverse reactions such as allergies
In addition, the preparation of drug-containing pellets by extrusion

Method used

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  • Esomeprazole drug-containing pellet composition and preparation method thereof
  • Esomeprazole drug-containing pellet composition and preparation method thereof
  • Esomeprazole drug-containing pellet composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: esomeprazole drug-containing pellet composition of the present invention

[0040] A drug-containing pellet composition of esomeprazole consists of 2g of esomeprazole magnesium dihydrate, 12g of mannitol and 6g of sodium chloride.

[0041] Preparation method: pass the esomeprazole magnesium dihydrate, mannitol, and sodium chloride of the above prescription amount through a 60-mesh sieve, mix evenly, add water to make a soft material, put it into an extrusion spheronizer, and use a 0.3mm-1.0 mm sieve plate extrusion, spheronization in the extrusion spheronizer, drying until the drying weight loss is less than 3.0%, namely to obtain esomeprazole drug-containing pellets.

Embodiment 2

[0043] A drug-containing pellet composition of esomeprazole is composed of 4 g of esomeprazole magnesium trihydrate, 10.2 g of sucrose, 4 g of potassium chloride, 1 g of sodium carbonate, and 0.8 g of magnesium stearate.

[0044] Preparation method: pass the esomeprazole magnesium trihydrate, sucrose, potassium chloride, sodium carbonate, and magnesium stearate of the above prescription amount through a 60-mesh sieve, mix well, add water to make a soft material, and put it into an extrusion spheronizer In the process, extrude with a sieve plate of 0.3 mm to 1.0 mm, spheronize in an extrusion spheronizer, and dry until the loss on drying is less than 3.0%, to obtain esomeprazole drug-containing pellets.

Embodiment 3

[0046] A kind of esomeprazole drug-containing pellet composition, is made up of 3g esomeprazole magnesium dihydrate, 6g lactose, 5g microcrystalline cellulose, 2g arginine, 2g sodium bicarbonate, 2g stearic acid .

[0047] Preparation method: pass the esomeprazole magnesium dihydrate, lactose, microcrystalline cellulose, arginine, and stearic acid in the above-mentioned prescription amount through a 60-mesh sieve, mix well, add water to make a soft material, and then put it into an extrusion ball In the machine, extrude with a sieve plate of 0.3 mm to 1.0 mm, spheronize in an extrusion spheronizer, and dry until the drying weight loss is less than 3.0%, to obtain esomeprazole drug-containing pellets.

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Abstract

The invention belongs to the field of medicines, and discloses an esomeprazole drug-containing pellet composition and a preparation method thereof. The esomeprazole drug-containing pellet composition provided by the invention comprises esomeprazole magnesium and hydrate thereof, a filling agent and a pore-forming agent. The filling agent and the pore-forming agent are mixed with esomeprazole according to a certain proportion, so that the stability of an esomeprazole medicament can be effectively improved, and adverse reactions such as allergy and the like caused by the use of a stabilizing agent are avoided. Moreover, the pore-forming agent can be quickly dissolved in water and can form pore passages in pellets to accelerate dissolution of the medicament. Experiments show that the esomeprazole drug-containing pellet composition disclosed by the invention is good in stability, high in dissolution degree and significant in gastric acid inhibition, so that the composition can be widely applied to treatment of gastroesophageal reflux diseases and peptic ulcers with positive helicobacter pylori. The preparation method disclosed by the invention is simple in operation, low in production cost and high in efficiency, and is suitable for industrial large-scale production of the esomeprazole drug-containing pellet composition.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a composition of esomeprazole drug-containing pellets and a preparation method thereof. Background technique [0002] Esomeprazole, namely esomeprazole, trade name Nexiumò (Chinese translation "Nexium"), is the world's first isomer proton pump inhibitor (I-PPI) isolated and synthesized by the Swedish company AstraZeneca (Astra). ), by inhibiting the H+ / K+-ATPase of gastric parietal cells to reduce gastric acid secretion and prevent the formation of gastric acid. Since it was launched in foreign countries in 2000 and in my country in 2003, it has been widely used in the treatment of gastroesophageal reflux disease and Helicobacter pylori-positive peptic ulcer because of its outstanding acid-suppressing effect and small side effects. [0003] Esomeprazole, Chinese name esomeprazole, chemical name 5-methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridine Base) methyl) sulfinyl) -1H-...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/4439A61K47/38A61K47/36A61K47/34A61K47/26A61K47/18A61K47/10A61K47/04A61P1/04
Inventor 陈芳晓黄怀龙仕贵曾环想王磊李娟廖婉莹丁梅
Owner SINOPHARM ZHIJUN (SHENZHEN) PHARMA CO LTD
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