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Pharmaceutical lansoprazole compound for treating gastric ulcer

A lansoprazole and compound technology, applied in the directions of drug combination, digestive system, organic chemistry, etc., can solve problems such as unsatisfactory results and influence drug quality, and achieve the effects of small content change, improved dissolution rate, and good fluidity

Inactive Publication Date: 2015-08-12
苗怡文
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, according to the chemical structure characteristics of lansoprazole, lansoprazole easily produces the following impurity A, impurity B and impurity E during production and storage, and these trace impurities will affect the quality of the drug
Although some crystal forms of the above-mentioned lansoprazole have improved its hygroscopicity, solubility or stability to a certain extent, the inventors' results are not ideal after investigating the impurities of the above-mentioned certain crystal forms

Method used

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  • Pharmaceutical lansoprazole compound for treating gastric ulcer
  • Pharmaceutical lansoprazole compound for treating gastric ulcer
  • Pharmaceutical lansoprazole compound for treating gastric ulcer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of lansoprazole crystal compound

[0035] (1) The crude product of lansoprazole is ground, passed through a 80 mesh sieve, and then added to a mixed solution of methanol, isopropanol and methyl furan whose volume is 5 times the weight of lansoprazole, methanol, isopropanol and formaldehyde The volume ratio of base furan is 5:3.5:2, stirs 15 minutes with the speed of 120 revs / min;

[0036] (2) Add a mixed solution of tetrahydrofuran and water whose volume is 8 times the weight of lansoprazole under stirring at a speed of 50 rpm, and the volume ratio of tetrahydrofuran:water is 1:1, and the temperature is raised to 20°C at the same time;

[0037] (3) After the solution has been added, leave it to stand for 2 hours, add dropwise the mixed solution of dichloromethane and acetone whose volume is 8 times of the weight of lansoprazole under the condition of 80 rev / min speed stirring, the mixture of dichloromethane and acetone The volume ratio is 1:1.5...

Embodiment 2

[0040] Example 2: Preparation of lansoprazole crystal compound

[0041] (1) The crude product of lansoprazole is ground, passed through a 100-mesh sieve, and then added to a mixed solution of methanol, isopropanol and methyl furan whose volume is 6 times the weight of lansoprazole, methanol, isopropanol and formaldehyde The volume ratio of base furan is 5:3.5:2, stirs 20 minutes with the speed of 150 rev / mins;

[0042] (2) Add a mixed solution of tetrahydrofuran and water whose volume is 10 times the weight of lansoprazole under stirring at a speed of 60 rpm, and the volume ratio of tetrahydrofuran:water is 1:1, and the temperature is raised to 27.5°C at the same time;

[0043] (3) After the solution has been added, leave it to stand for 2.5 hours, add dropwise the mixed solution of dichloromethane and acetone whose volume is 9 times of the weight of lansoprazole under the condition of 90 rev / min speed stirring, the mixture of dichloromethane and acetone The volume ratio is 1...

Embodiment 3

[0046] Example 3: Preparation of lansoprazole crystal compound

[0047] (1) The crude product of lansoprazole is ground, passed through a 120 mesh sieve, and then added to a mixed solution of methanol, isopropanol and methyl furan whose volume is 7 times the weight of lansoprazole, methanol, isopropanol and formaldehyde The volume ratio of base furan is 5:3.5:2, stirs 25 minutes with the speed of 180 rev / mins;

[0048] (2) Add a mixed solution of tetrahydrofuran and water whose volume is 12 times the weight of lansoprazole under stirring at a speed of 70 rpm, and the volume ratio of tetrahydrofuran:water is 1:1, and the temperature is raised to 35°C at the same time;

[0049] (3) After the solution has been added, leave it to stand for 2-3 hours, add dropwise the mixed solution of dichloromethane and acetone whose volume is 10 times the weight of lansoprazole with 100 rev / min speed stirring, dichloromethane and The volume ratio of acetone is 1:1.5, and the uniform dropwise ...

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Abstract

The invention discloses a pharmaceutical lansoprazole compound for treating gastric ulcer, belongs to the field of medicines and particularly relates to a lansoprazole compound and a preparation method thereof. The lansoprazole compound is measured with a Cu-K alpha ray to obtain an X-ray powder diffraction diagram shown in Figure 1. The crystal lansoprazole compound provided by the invention contains no impurity E, the contents of impurities A and B are remarkably reduced and change a little as the storage time increases, and the lansoprazole compound has superior fluidity and is remarkably improved in dissolution rate.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a drug lansoprazole compound for treating gastric ulcer, in particular to a lansoprazole compound and a preparation method thereof. Background technique [0002] Lansoprazole is a benzimidazole derivative with anti-acid effect developed by Takeda Corporation of Japan in December 1991. It acts on the H+-K+-ATPase of gastric parietal cells, so that the H+ of parietal cells cannot be transported into the stomach It is used to treat gastric ulcer, duodenal ulcer and reflux esophagitis, and to eradicate Helicobacter pylori. [0003] Lansoprazole is a new type of proton pump inhibitor, which is an upgraded product of omeprazole. Lansoprazole has introduced fluorine into the side chain at the 4-position of the pyridine ring and has a trifluoroethoxy substituent, so that its bioavailability is relatively low. Omeprazole is increased by more than 30%, and its lipophilicity is stronger than that of o...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04A61P31/04
CPCC07D401/12
Inventor 于相芬
Owner 苗怡文
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