Lansoprazole or dextral lansoprazole crystal type compound and preparation method thereof

A technology of dexlansoprazole trihydrate and racemic lansoprazole trihydrate is applied in the field of medicine, which can solve problems such as unsatisfactory results and influence on drug quality, achieve small content changes, improve dissolution rate, The effect of good fluidity

Active Publication Date: 2015-08-19
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] However, according to the chemical structure characteristics of lansoprazole, lansoprazole or dexlansoprazole are prone to produce 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 or dex-lansoprazole have improved their hygroscopicity, solubility or stability to a certain extent, after the inventors have investigated the impurities of the above-mentioned certain crystal forms, The result is not ideal

Method used

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  • Lansoprazole or dextral lansoprazole crystal type compound and preparation method thereof
  • Lansoprazole or dextral lansoprazole crystal type compound and preparation method thereof
  • Lansoprazole or dextral lansoprazole crystal type compound and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] [embodiment 1] the preparation of lansoprazole crystal form compound

[0050] (1) Get lansoprazole crude product 100g, add mixed solution A2000ml at 45 DEG C, stir until all dissolvings, get lansoprazole solution, wherein said mixed solution A is N-methylpyrrolidone and methyl alcohol with 4: Prepared with a volume ratio of 1;

[0051] (2) The lansoprazole solution obtained in step 1) is naturally cooled to room temperature, and the mixed solution B is added under stirring at a stirring speed of 1480r / min. After the addition is completed, the temperature is lowered to 2° C., and crystals are precipitated, wherein the The volume ratio of mixed solution B and lansoprazole solution is 20:1, and described mixed solution B is that acetone and water are prepared with the volume ratio of 1:3.5;

[0052] (3) Stand still in an environment with a temperature of 2° C. for 3 hours, filter, wash the filter cake with methanol, and dry in vacuum to obtain the lansoprazole crystal com...

Embodiment 2-8

[0059]

[0060] The lansoprazole crystal form compound that embodiment 2-8 makes adopts U.S. Perkin-Elmer company PE 2400 II elemental analyzer, elemental analysis (%) measured value is close to embodiment 1; Use Cu-Kα ray measurement to obtain The X-ray powder diffraction spectrogram is similar to Example 1; Cassette type moisture determination is similar to Example 1;

Embodiment 9

[0061] [embodiment 9] preparation of dexlansoprazole crystal form compound

[0062] (1) Get dexlansoprazole crude product 100g, add mixed solution A2000ml at 45 ℃, stir until all dissolving, get dexlansoprazole solution, wherein said mixed solution A is N-methylpyrrolidone and Methanol is prepared at a volume ratio of 4:1;

[0063] (2) The dexlansoprazole solution obtained in step 1) is naturally cooled to room temperature, and the mixed solution B is added under stirring at a stirring speed of 1480r / min. The volume ratio of described mixed solution B and dexlansoprazole solution is 20:1, and described mixed solution B is that acetone and water are prepared with the volume ratio of 1:3.5;

[0064] (3) Stand still in an environment with a temperature of 2°C for 3 hours, filter, wash the filter cake with methanol, and dry in vacuo to obtain the crystalline compound of D-lansoprazole with an optical purity of 99.9%.

[0065] Using the PE 2400 II elemental analyzer of Perkin-Elm...

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Abstract

The invention belongs to the medical technical field and particularly relates to a lansoprazole or dextral lansoprazole crystal type compound and a preparation method thereof. The lansoprazole or dextral lansoprazole crystal type compound is trihydrate crystal, the molecular formula of the lansoprazole or dextral lansoprazole crystal type compound is as follows, the strutral formula of the lansoprazole or dextral lansoprazole crystal type compound is as follows, and an X-ray powder diffraction spectrum which is obtained through the formula ray measurement is as follows. The lansoprazole or dextral lansoprazole crystal type compound is free of impurity E, and the content of impurities A and impurities B is significantly reduced, the change of the content of the impurities A and the impurities B is small along with the extension of the storage time, the liquidity is excellent, and the dissolution rate is significantly improved.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a lansoprazole or dex-lansoprazole crystal form compound and a preparation method thereof. Background technique [0002] Lansoprazole (Lansoprazole) chemical name: (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]ylidene Sulfonyl]-1H-benzimidazole, its chemical structural formula is: [0003] [0004] Lansoprazole is a benzimidazole derivative with anti-acid effect developed by Takeda Corporation of Japan in December 1991. It acts on the H of gastric parietal cells. + -K + -ATPase, which makes parietal cell H + It cannot be transported to the stomach, so that the amount of gastric acid in the gastric juice is greatly reduced. It is used to treat gastric ulcer, duodenal ulcer and reflux esophagitis, and to eradicate Helicobacter pylori. [0005] Lansoprazole is a new type of proton pump inhibitor, which is an upgraded product of omeprazole. Lansoprazole has in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04A61P31/04
CPCC07D401/12
Inventor 何雅官韩云龙王广明徐太平
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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