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Lansoprazole compound

A technology of lansoprazole and compounds, applied in the field of lansoprazole compounds, can solve the problems of fluid crystal form change, unfavorable operation, time-consuming, etc., and achieve the effects of low hygroscopicity, good water solubility, and quality assurance

Active Publication Date: 2014-03-26
北京科创鼎诚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The preparation method of lansoprazole anhydrous crystal form (type I) described in CN1355798A has been recrystallized four times successively, and the preparation process is complicated and time-consuming; the lansoprazole B crystal form described in US2009 / 0018339A1 is a metastable crystal Type, under certain conditions will undergo a solid-solid phase transition to form A crystal
[0009] However, lansoprazole also has strong hygroscopicity, which will cause changes in physical and chemical properties such as agglomeration, decreased fluidity, deliquescence, and crystal form changes after moisture absorption, thereby affecting product stability, effectiveness, safety, and efficacy. Intrinsic quality, not conducive to the operation of the preparation process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] [embodiment 1] the preparation of lansoprazole compound

[0037] 1) Take 10kg of crude lansoprazole and dissolve it in 12L of acetone at 50°C to obtain acetone solution of lansoprazole;

[0038] 2) Add 0.01 g of activated carbon to the lansoprazole acetone solution obtained in step 1), stir for 15 minutes, filter with suction, and take the filtrate;

[0039] 3) Cool the filtrate to room temperature naturally, and then add 24L of organic solvent A to the filtrate at a speed of 13L / min under stirring at a speed of 50r / min to form a cloudy solution, wherein the organic solvent A is methanol and A mixed solvent composed of methyl chloride at a volume ratio of 2:1;

[0040] 4) Adjust the stirring speed to 25r / min, then add 36L of organic solvent B to the turbid solution in step 3) at a speed of 12L / min, after the addition is completed, cool down to 0°C, and crystals are precipitated. Solvent B is a mixed solvent composed of ethyl acetate and dimethylformamide at a volume r...

Embodiment 2

[0043] [embodiment 2] the preparation of lansoprazole compound

[0044] 1) Take 10kg of crude lansoprazole and dissolve it in 26L of acetone at 60°C to obtain acetone solution of lansoprazole;

[0045] 2) Add 0.01 g of activated carbon to the lansoprazole acetone solution obtained in step 1), stir for 15 minutes, filter with suction, and take the filtrate;

[0046] 3) Cool the filtrate to room temperature naturally, then add 130L of organic solvent A to the filtrate at a speed of 20L / min under stirring at a speed of 60r / min to form a cloudy solution, wherein the organic solvent A is methanol and A mixed solvent composed of methyl chloride at a volume ratio of 5:1;

[0047] 4) Adjust the stirring speed to 25r / min, then add 78L of organic solvent B to the turbid solution in step 3) at a rate of 6L / min, after the addition is completed, cool down to 5°C, and crystals are precipitated. Solvent B is a mixed solvent composed of ethyl acetate and dimethylformamide at a volume ratio of...

Embodiment 3

[0050] [embodiment 3] the preparation of lansoprazole compound

[0051] 1) Take 10kg of crude lansoprazole and dissolve it in 20L of acetone at 55°C to obtain acetone solution of lansoprazole;

[0052] 2) Add 0.01 g of activated carbon to the lansoprazole acetone solution obtained in step 1), stir for 15 minutes, filter with suction, and take the filtrate;

[0053] 3) Cool the filtrate to room temperature naturally, and then add 60L of organic solvent A to the filtrate at a speed of 18L / min under stirring at a speed of 55r / min to form a cloudy solution, wherein the organic solvent A is methanol and A mixed solvent composed of methyl chloride at a volume ratio of 4:1;

[0054] 4) Adjust the stirring speed to 20r / min, then add 160L of organic solvent B to the turbid solution in step 3) at a speed of 8L / min, after the addition is completed, cool down to 3°C, and crystals are precipitated. Solvent B is a mixed solvent composed of ethyl acetate and dimethylformamide in a volume r...

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Abstract

The invention belongs to the technical field of medicines and in particular relates to a lansoprazole compound. The lansoprazole compound has a chemical structural formula and is measured by a powder X-ray diffraction measurement method, and an X-ray diffraction pattern represented by a diffraction angle of 2theta 0.2 degrees is as shown in a figure 1. The lansoprazole compound provided by the invention is a novel lansoprazole crystal form different from that in the prior art, and the crystal form is lower in moisture absorptivity and better in solubility.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a lansoprazole compound. 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 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. [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 omeprazole. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 李琦杨磊
Owner 北京科创鼎诚医药科技有限公司
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