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Specific L-pantoprazole sodium superfine powder lyophilized preparation and preparation method thereof

A technology of levopantoprazole sodium and ultrafine powder, which is applied in the field of medicine, can solve the problems of large toxic and side effects, small specific surface area, poor solubility, etc., and achieve the effect of improving utilization rate, large specific surface area and easy absorption

Inactive Publication Date: 2014-11-12
浙江磐谷药源有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing L-pantoprazole sodium has the disadvantages of low clarity, poor stability, low purity, many impurities, large particles, small specific surface area, poor solubility, large toxic and side effects, and easy allergies

Method used

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  • Specific L-pantoprazole sodium superfine powder lyophilized preparation and preparation method thereof
  • Specific L-pantoprazole sodium superfine powder lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 367 grams (1mol) of 5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfur]-1H-benzimidazole, Ethyl acetate 2.4L (2.20 kg), purified water 5ml (0.28mol), D-(-)-diethyl tartrate 165g (0.8mol) and titanium tetraisopropoxide 57g (0.2mol), stirred and heated to 60°C to form a transparent solution, keep stirring and react for 1 hour, then cool the reaction solution to 20°C, add 42ml (0.3mol) of triethylamine, stir for 15 minutes, then slowly add 80% hydroxycumene peroxide 172ml (1.2 mol), the reaction was carried out at 20°C, followed by HPLC until the residual raw material was reduced to less than 1%, the reaction was terminated, 12% ammonia solution was added for extraction, the aqueous phase was combined, the pH was adjusted to 7.5 with concentrated acetic acid, and then ethyl acetate Extract, combine the organic phases, dry over anhydrous sodium sulfate, filter, and concentrate under reduced pressure to obtain crude L-pantoprazole as a pink solid. Recrystallize wi...

Embodiment 2

[0028]367 grams (1mol) of 5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfur]-1H-benzimidazole, Ethyl acetate 3.3L (2.94 kg), purified water 7ml (0.4mol), D-(-)-diethyl tartrate 206g (1mol) and titanium tetraisopropoxide 94g (0.33mol), stirred and heated to 62 ℃ into a transparent solution, keep stirring and react for 1 hour, the temperature of the reaction solution is lowered to 22 ℃, add 63ml (0.45mol) of triethylamine, stir for 15 minutes, then slowly add 230ml (1.6mol) of 80% hydroxycumene peroxide dropwise ), the reaction was carried out at 22°C, followed by HPLC until the residual raw material was reduced to less than 1%, the reaction was terminated, and 12% ammonia solution was added for extraction, the aqueous phase was combined, adjusted to pH = 7 with concentrated acetic acid, and then extracted with ethyl acetate , combined organic phases, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain crude L-pantoprazole ...

Embodiment 3

[0035] 367 grams (1mol) of 5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)methyl]sulfur]-1H-benzimidazole, 4.1 L (3.67 kg) of ethyl acetate, 11 ml (0.6 mol) of purified water, 247 g (1.2 mol) of D-(-)-diethyl tartrate and 171 g (0.6 mol) of titanium tetraisopropoxide, stirred and heated to Form a transparent solution at 65°C, heat and stir for 1 hour, cool the reaction solution to 25°C, add 84ml (0.6mol) of triethylamine, stir for 15 minutes, then slowly add 287ml (2mol) of 80% hydroxycumene peroxide dropwise , carry out the reaction at 25°C, follow up with HPLC until the residual raw material is reduced to less than 1%, stop the reaction, add 12% ammonia solution for extraction, combine the water phases, adjust the pH=7 with concentrated acetic acid, and then extract with ethyl acetate, The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure to obtain crude L-pantoprazole as a pink solid. Recrystallize with ace...

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Abstract

The invention discloses a specific L-pantoprazole sodium superfine powder lyophilized preparation and a preparation method thereof. The preparation method uses 5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)methyl] sulfur]-1H-benzimidazole and cumene hydroperoxide as raw materials, and comprises the following steps: preparing a L-pantoprazole crude product by catalysis of tetraisopropyl orthotitanate, D-(-)diethyl tartrate and triethylamine system; recrystallizing with acetone to obtain a L-pantoprazole refined product; reacting with NaOH to obtain L-pantoprazole sodium; performing air-jet superfine crushing, and lyophilizing. The specific L-pantoprazole sodium superfine powder lyophilized preparation has the advantages of good clarity, high stability, high purity, few impurities, small particles, large specific surface area, good solubility, small toxic and side effect, allergy prevention and the like.

Description

technical field [0001] The invention relates to a special ultrafine powder freeze-dried preparation of L-pantoprazole sodium and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Levpantoprazole Sodium (Levpantoprazole Sodium), chemical name: S-(-)-5-difluoromethoxy-2-[[(3,4-dimethoxy-2-pyridyl)methyl ]sulfinyl]-1H-benzimidazole sodium is the third-generation proton pump inhibitor after omeprazole and lansoprazole, and is the single enantiomer of pantoprazole that has been applied clinically. Sodium salt of S-(-)-pantoprazole. The drug is mainly used for the treatment of: ① peptic ulcer bleeding. ② Acute gastric mucosal injury caused by non-steroidal anti-inflammatory drugs and the occurrence of ulcer bleeding under stress; ③ Prevention of gastric acid reflux combined with aspiration pneumonia after general anesthesia or major surgery and in debilitated comatose patients. The drug is stable under weak acid conditions...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4439A61P1/04
Inventor 傅苗青李凤生
Owner 浙江磐谷药源有限公司
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