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New crystal form of lansoprazole and preparation method and application thereof

A technology of lansoprazole and its crystal form, which is applied in the field of new lansoprazole crystal form and its preparation, can solve the problems of complex preparation process and time-consuming, and achieve simple operation, less solvent amount and good reproducibility Effect

Inactive Publication Date: 2011-09-14
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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

Method used

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  • New crystal form of lansoprazole and preparation method and application thereof
  • New crystal form of lansoprazole and preparation method and application thereof
  • New crystal form of lansoprazole and preparation method and application thereof

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preparation example Construction

[0037] The preparation method of Lansoprazole M crystal form, comprises the following steps:

[0038] 1) Lansoprazole is dissolved in methanol: in the mixed solvent of water=5:3 (volume ratio), filter;

[0039]2) Cool the filtrate to -20~-15°C to precipitate crystals;

[0040] 3) The crystals are filtered and dried to obtain the M crystal form of lansoprazole.

[0041] Lansoprazole N crystal form, its X-ray powder diffraction at diffraction angle 2 θ For: 5.438, 7.062, 8.230, 9.216, 11.022, 11.789, 12.610, 13.541, 20.603, 21.862, 26.242 have characteristic peaks; 1 H-NMR (CDCl 3 ) data are: 8.34 (d, 1H), 7.65 (br., 2H), 7.30 (d, 1H), 6.67 (d, 1H), 4.74 (q, 2H), 4.40 (d, 1H), 4.32 (d , 1H), 2.21 (s, 3H); Its IR (KBr, cm -1 ) data are: 3628, 3382, 3133, 3071, 2974, 2896, 2818, 1645, 1582, 1475, 1441, 1315, 1265, 1198, 1168, 1111, 1036, 972, 916, 857, 744, 661.

[0042] The preparation method of Lansoprazole N crystal form, comprises the following steps:

[0043] 1) Lansop...

Embodiment 1

[0049] 1) 50mg lansoprazole was dissolved in 0.1mL methanol solution;

[0050] 2) Add 0.06 mL of water dropwise to the resulting solution, and filter;

[0051] 3) Cool down the clear solution to -15°C to make it fully crystallized, filter and dry.

[0052] Obtained 43.1 mg of off-white crystalline powder with a yield of 86.2%.

Embodiment 2

[0054] 1) 100mg lansoprazole was dissolved in 0.5mL methanol solution;

[0055] 2) Add 0.3 mL of water dropwise to the resulting solution, and filter;

[0056] 3) Cool down the clear solution to -15°C to make it fully crystallized, filter and dry.

[0057] 87.5 mg of off-white crystalline powder was obtained, with a yield of 87.5%.

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Abstract

The invention discloses a new crystal form of lansoprazole and a preparation method and application thereof. The new crystal form of the lansoprazole is easy to prepare. The crystal form of the lansoprazole prepared by the method has high purity and low impurity content; the required amount of a solvent is small, and production cost is low; the preparation method is easy to operate and high in repeatability; reaction conditions are mild, and easy to control; and the target product crystal form can be stably obtained.

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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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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