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Lansoprazole N crystal form and preparation method and application thereof

A technology of lansoprazole and crystal form, applied in the field of new crystal form of lansoprazole and its preparation, can solve the problems of complicated preparation process, time-consuming and the like, and achieves simple operation, less solvent and good reproducibility Effect

Inactive Publication Date: 2013-04-03
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] CN1355798A describes the preparation method of lansoprazole anhydrous crystal type (I type), successively undergoes four times of recrystallization, the preparation process is complicated and time-consuming; US 2009 / The crystal form B of lansoprazole described in 0018339A1 is a metastable crystal form, which will undergo a solid-solid phase transition under certain conditions to form a crystal form A

Method used

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  • Lansoprazole N crystal form and preparation method and application thereof
  • Lansoprazole N crystal form and preparation method and application thereof
  • Lansoprazole N crystal form and preparation method and application thereof

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preparation example Construction

[0028] The preparation method of Lansoprazole N crystal form, comprises the following steps:

[0029] 1) Lansoprazole is dissolved in ethyl acetate, or n-butanol and water volume ratio are in the mixed solvent of 10:1;

[0030] 2) Cool the above solution to -20~-10°C to precipitate crystals;

[0031] 3) The crystals are filtered and dried to obtain the N crystal form of lansoprazole.

Embodiment 1

[0035] 1) 50mg lansoprazole was dissolved in 0.1mL ethyl acetate, filtered;

[0036] 2) Cool down the clear solution to -10°C to make it fully crystallized, filter and dry.

[0037] Obtained 42.7 mg of off-white crystalline powder with a yield of 85.4%.

Embodiment 2

[0039] 1) 100mg lansoprazole was dissolved in 0.5mL ethyl acetate, filtered;

[0040] 2) Cool down the clear solution to -10°C to make it fully crystallized, filter and dry.

[0041] 79.6 mg of off-white crystalline powder was obtained, with a yield of 79.6%.

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Abstract

The invention discloses a lansoprazole N crystal form and a preparation method and application thereof. The X-ray powder diffraction of the lansoprazole N crystal form has characteristic peaks when the diffraction angle 2(theta) is 5.438, 7.062, 8.230, 9.216, 11.022, 11.789, 12.610, 13.541, 20.603, 21.862 and 26.242. The preparation method comprises the following steps of: dissolving lansoprazole in ethyl acetate or a mixed solvent of n-butyl alcohol and water; cooling to separate out crystals; and filtering and drying to obtain the lansoprazole N crystal form. The new lansoprazole crystal form disclosed by the invention is easy to prepare; the preparation method requires little solvent and is simple to operate, and the production cost is low; the reaction conditions are mild, and the control is easy; and the reproducibility is good, and a target product crystal form can be stably obtained. Through the method disclosed by the invention, the prepared lansoprazole crystal form has high purity and low impurity content, maintains all pharmacologic characteristics of lansoprazole, and can be used for treating gastric ulcer, duodenal ulcer and reflux esophagitis and eradicating helicobacter pylori.

Description

technical field [0001] The invention relates to a new crystal form of lansoprazole 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 introduced fluorine into the side chain at the 4-position of the pyridine r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04A61P31/04
Inventor 闫岩鲁统部陈嘉媚梁仁兴王晓玲高建陈果唐雪枫
Owner SUN YAT SEN UNIV
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