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Special ultrafine omeprazole sodium powder freeze-dried preparation and preparation method thereof

A technology of omeprazole sodium and ultrafine powder, applied in the field of medicine, can solve the problems of large toxic and side effects, small specific surface area, low clarity, etc., and achieve the effect of improving utilization rate, large specific surface area and good clarity

Inactive Publication Date: 2014-11-05
杭州长典老一元健康管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Existing omeprazole 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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  • Special ultrafine omeprazole sodium powder freeze-dried preparation and preparation method thereof

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Experimental program
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Embodiment 1

[0029] 222 grams (1mol) of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 180 grams (1mol) of 2-mercapto-5-methoxy-1H-benzimidazole Add to 5 liters of ethanol and acetone mixed solvent, the volume ratio of ethanol and acetone is 3:1, the mixed solvent contains 80 grams (2mol) of sodium hydroxide, while adding 4.5 grams (0.03mol) of sodium iodide catalyst, this reaction The mixture was heated to reflux for 1.5 hours, cooled to room temperature, filtered to remove insoluble matter, the filtrate was distilled off under reduced pressure to remove most of the solvent, the residue was dissolved by adding 3 liters of ethyl acetate, washed twice with 1 liter of water, washed with anhydrous sodium sulfate Dry the organic phase, filter, concentrate, add 400ml of acetone to the residue, freeze the organic phase to 0°C, precipitate a solid overnight, and filter to obtain 315.8 g of off-white solid 5-methoxy-2-[(4-methoxy-3 , 5-dimethylpyridin-2-yl)methylthio]-1H-benzimida...

Embodiment 2

[0035] 222 grams (1mol) of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 180 grams (1mol) of 2-mercapto-5-methoxy-1H-benzimidazole Add to 5 liters of ethanol and acetone mixed solvent, the volume ratio of ethanol and acetone is 3:1, the mixed solvent contains 80 grams (2mol) of sodium hydroxide, while adding 3.7 grams (0.025mol) of sodium iodide catalyst, this reaction The mixture was heated to reflux for 2 hours, cooled to room temperature, filtered to remove insoluble matter, the filtrate was distilled under reduced pressure to remove most of the solvent, the residue was dissolved in 3 liters of ethyl acetate, washed twice with 1 liter of water, washed with anhydrous sodium sulfate Dry the organic phase, filter, concentrate, add 400ml of acetone to the residue, freeze the organic phase to 0°C, precipitate a solid overnight, and filter to obtain 315.8 g of off-white solid 5-methoxy-2-[(4-methoxy-3 , 5-dimethylpyridin-2-yl)methylthio]-1H-benzimidazole.

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Embodiment 3

[0041] 222 grams (1mol) of 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 180 grams (1mol) of 2-mercapto-5-methoxy-1H-benzimidazole Add to 5 liters of ethanol and acetone mixed solvent, the volume ratio of ethanol and acetone is 3:1, the mixed solvent contains 80 grams (2mol) of sodium hydroxide, while adding 3 grams (0.02mol) of sodium iodide catalyst, this reaction The mixture was heated to reflux for 2.5 hours, cooled to room temperature, filtered to remove insoluble matter, the filtrate was distilled under reduced pressure to remove most of the solvent, and 3 liters of ethyl acetate was added to the residue to dissolve, washed twice with 1 liter of water, washed with anhydrous sodium sulfate Dry the organic phase, filter, concentrate, add 400ml of acetone to the residue, freeze the organic phase to 0°C, precipitate a solid overnight, and filter to obtain 315.8 g of off-white solid 5-methoxy-2-[(4-methoxy-3 , 5-dimethylpyridin-2-yl)methylthio]-1H-benzimidaz...

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Abstract

The invention discloses a special ultrafine omeprazole sodium powder freeze-dried preparation and a preparation method thereof. The method comprises the following steps: step 1, adding 2-chloromethyl-3,5-dimethyl-4-methoxypyridine hydrochloride and 2-mercapto-5-methoxy-1H-benzimidazole into a sodium hydroxide-containing mixed solvent of ethanol and acetone, adding sodium iodide and carrying out a reaction so as to prepare 5-methoxy-2-[(4-methoxy-3,5-dimethylpyridine-2-yl)methylthio]-1H-benzimidazole; step 2, oxidizing 5-methoxy-2-[(4-methoxy-3,5-dimethylpyridine-2-yl)methylthio]-1H-benzimidazole with an oxidizing agent so as to produce omeprazole; step 3, dissolving omeprazole in isopropanol, reacting omeprazole with sodium hydroxide so as to produce omeprazole sodium and carrying out filtering, washing and drying so as to obtain high-purity omeprazole sodium; and step 4, carrying out air jet pulverization on dried meprazole sodium so as to obtain ultrafine powder and subjecting the ultrafine powder to freeze-drying.

Description

technical field [0001] The invention relates to a special ultrafine powder freeze-dried preparation of omeprazole sodium and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Omeprazole sodium, its chemical name is: 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)-methyl]-sulfinyl] -1H-benzimidazole sodium monohydrate, the English name is Omeprazole Sodium, molecular formula: C 17 h 18 N 3 NaO 3 S·H 2 O, molecular weight: 385.41, structural formula as follows: [0003] [0004] In the prior art, the auxiliary materials of this product are: mannitol and water for injection. This product is white or off-white loose lump or powder. As an alternative therapy for the following conditions when oral therapy is not appropriate: duodenal ulcer, gastric ulcer, reflux esophagitis, and Zollinger-Ellison syndrome. [0005] In December 1999, "Special Ultrafine Powder Preparation Technology" won the first prize of the Natio...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4439C07D401/12A61P1/04
Inventor 傅苗青李凤生陈宇东傅根元
Owner 杭州长典老一元健康管理有限公司
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