Novel benzimidazole isomer preparation and preparation method thereof

A benzimidazole and isomerization technology is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., and can solve the problems of low bioavailability, poor water solubility, unstable aqueous solution and the like, To achieve the effect of improving curative effect, promoting emulsification and improving water solubility

Inactive Publication Date: 2015-01-21
DASHENGXIANG (WUHAN) TRADITIONAL CHINESE MEDICINE INVESTMENT MANAGEMENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, omeprazole has special properties and poor water solubility, so it is difficult to be effectively transported to the lesion or cells. Its aqueous solution is unstable and decomposes quickly under acidic conditions, and its bioavailability is low.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A freeze-dried powder injection containing omeprazole, which is made of the following raw materials:

[0027] Omeprazole 10g, berberine hydrochloride 10g, sodium bicarbonate 500g, magnesium hydroxide 450g, hydroxypropyl-β cyclodextrin (degree of substitution 4-5) 20g, oleic acid 200g, water for injection 950g.

[0028] The preparation method of above-mentioned freeze-dried powder injection containing omeprazole, comprises the following steps:

[0029] (1) Grind and mix the prescribed amount of omeprazole, berberine hydrochloride, and magnesium hydroxide, and set aside;

[0030] (2) Weigh the prescribed amount of sodium bicarbonate, dissolve it in water for injection, and stir to dissolve it;

[0031] (3) Add the powder of step (1) to the clarified liquid of step (2), and stir for 30 minutes to form a suspension;

[0032] (4) Add hydroxypropyl-β-cyclodextrin (substitution degree is 4-5), and slowly drop oleic acid, after the dropwise addition, stir for 20 minutes;

[...

Embodiment 2

[0036] A freeze-dried powder injection containing omeprazole, which is made of the following raw materials:

[0037] Omeprazole 15g, berberine hydrochloride 15g, sodium bicarbonate 600g, magnesium hydroxide 500g, hydroxypropyl-β cyclodextrin (substitution degree 4-5) 30g, oleic acid 300g, water for injection 950g.

[0038] The preparation method of above-mentioned freeze-dried powder injection containing omeprazole, comprises the following steps:

[0039] (1) Grind and mix the prescribed amount of omeprazole, berberine hydrochloride, and magnesium hydroxide, and set aside;

[0040] (2) Weigh the prescribed amount of sodium bicarbonate, dissolve it in water for injection, and stir to dissolve it;

[0041] (3) Add the powder of step (1) to the clarified liquid of step (2), and stir for 40 minutes to form a suspension;

[0042] (4) Add hydroxypropyl-β-cyclodextrin (substitution degree is 4-5), and slowly drop oleic acid, after the dropwise addition, stir for 30 minutes;

[004...

Embodiment 3

[0046] A freeze-dried powder injection containing omeprazole, which is made of the following raw materials:

[0047] Omeprazole 13g, berberine hydrochloride 12g, sodium bicarbonate 550g, magnesium hydroxide 480g, low polyester β-cyclodextrin 25g, oleic acid 210g, water for injection 950g.

[0048] The preparation method of above-mentioned freeze-dried powder injection containing omeprazole, comprises the following steps:

[0049] (1) Grind and mix the prescribed amount of omeprazole, berberine hydrochloride, and magnesium hydroxide, and set aside;

[0050] (2) Weigh the prescribed amount of sodium bicarbonate, dissolve it in water for injection, and stir to dissolve it;

[0051] (3) Add the powder of step (1) to the clarified liquid of step (2), and stir for 35 minutes to form a suspension;

[0052] (4) Add hydroxypropyl-β-cyclodextrin (substitution degree is 4-5), and slowly drop oleic acid, after the dropwise addition, stir for 25 minutes;

[0053] (5) Add 0.1mol / L sodium...

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PUM

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Abstract

The invention discloses a novel benzimidazole isomer preparation. The novel benzimidazole isomer preparation is prepared from the following components in parts by weight: 1-1.5 parts of omeprazole, 1-1.5 parts of berberine hydrochloride, 50-60 parts of sodium bicarbonate, 45-50 parts of magnesium hydrate, 2-3 parts of oligoester beta-cyclodextrin, 20-30 parts of oleic acid and 80-95 parts of injection water. The invention also discloses a preparation method of the novel benzimidazole isomer preparation. Omeprazole and berberine hydrochloride disclosed by the invention have synergistic effects; and the berberine hydrochloride not only can prompt the omeprazole to restrain gastric acid secretion and increase effect, but also effectively reduces the adverse effects rate. The oligoester beta-cyclodextrin is also introduced into the novel benzimidazole isomer preparation, so that the effective ingredients omeprazole and berberine hydrochloride are coated by the oligoester beta-cyclodextrin; the water solubility is effectively improved; the oligoester beta-cyclodextrin is mixed into oleinic acid, so that emulsification of the oligoester beta-cyclodextrin is also further prompted; the conditions of uneven distribution such as suspension or sedimentation are prevented; and the curative effect is greatly improved.

Description

[0001] technical field [0002] The invention relates to a new benzimidazole isomer preparation, in particular to a new preparation containing omeprazole. It belongs to the field of medical technology. Background technique [0003] Omeprazole, chemical name is 5-methoxy-2-{[(4-methoxy-3,5-dimethyl-2-pyridyl)-methyl]-sulfinyl}-1H- Benzimidazole is a proton pump inhibitor that can effectively inhibit gastric acid secretion. It selectively acts on gastric parietal cells and inhibits H+ on the secretory microtubules formed by the apical membrane of gastric parietal cells and tubular vesicles in the cytoplasm. The activity of -K+-ATPase can effectively inhibit the secretion of gastric acid, and the effect is rapid. It is suitable for gastric and duodenal ulcers, reflux esophagitis and gastrinoma. due to H + 、K + -ATPase is the last process of parietal cell acid secretion, so this product has a strong ability to suppress acid, and has a strong and long-lasting effect of inhibit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/06A61K31/4439A61K47/48A61K9/19A61P1/04A61K31/4375A61K33/00
CPCA61K31/4375A61K9/19A61K31/4439A61K33/00A61K33/06A61K47/6951A61K2300/00
Inventor 傅苗青克隆斯特伦马特松
Owner DASHENGXIANG (WUHAN) TRADITIONAL CHINESE MEDICINE INVESTMENT MANAGEMENT CO LTD
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