Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Pantoprazole sodium special ultrafine powder lyophilized preparation and preparation method thereof

A technology of pantoprazole sodium and ultrafine powder, which is applied in the field of medicine, can solve the problems of affecting the deposition effect of drug administration, low purity of pantoprazole sodium, affecting the exertion of drug effect, etc., and achieves good chemical reactivity, strong Surface activity and catalysis, the effect of improving bioavailability

Inactive Publication Date: 2014-10-08
杭州澳亚生物技术股份有限公司 +1
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Multiple methods for synthesizing Pantoprazole Sodium have been disclosed both at home and abroad at present, but the Pantoprazole Sodium that these methods make has low purity, many impurities, large particles, poor solubility, low activity and other shortcomings
These factors will affect the deposition effect of the drug, thereby affecting the efficacy of the drug.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pantoprazole sodium special ultrafine powder lyophilized preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Take 0.4mol of 2-bromo-3,4-lutidine as raw material and react with CuCN to produce 3,4-dimethoxy-2-cyanopyridine, which is then hydrolyzed in the presence of sodium hydroxide and reacted with diazonium Methane methylation produces methyl esters. The intermediate methyl ester is reduced and then chlorinated to form 2-chloromethyl-3,4-lutidine hydrochloride. Then it is condensed in ethanol solution to produce thioether, and finally oxidized by m-chloroperbenzoic acid in dichloromethane solution to produce crude pantoprazole sodium. The content of pantoprazole sodium is determined to be 86.78%.

[0027] Add anhydrous methanol to the crude product of pantoprazole sodium at a temperature of 10°C, stir and remove the methanol solution by suction filtration to obtain a filter cake of pantoprazole sodium. The amount of anhydrous methanol is pantoprazole sodium 75% of the volume, and then vigorously stirred to form a slurry, then suction filtered to remove the methanol solution to...

Embodiment 2

[0031] Dissolve pantoprazole sodium, calcium glutamate, and disodium edetate in water for injection containing 80 times the weight of pantoprazole sodium under constant speed stirring to obtain a composition solution; Activated carbon that removes heat source within hours is added to the composition solution, the ratio of the added weight of activated carbon to the volume of the drug solution is 0.15%; the combined drug solution is sterilized by moist heat at 121°C for 20 minutes. When the temperature of the drug solution is 70°C, it is filtered with two layers of superimposed membranes. Pass; when the sterilized and filtered combination drug solution is cooled to 10-15℃, adjust the pH value to 7.5-8.0 with 8% sodium hydroxide solution, and filter through the membrane; adjust the pH value to 6.5-7.5 with 8% hydrochloric acid solution , Determine the content of the combined drug components, aseptically dispense into pantoprazole sodium combined drug injection.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a pantoprazole sodium special ultrafine powder lyophilized preparation and a preparation method thereof. The method comprises the steps of: 1. taking 2-bromo-3, 4-dimethyl pyridine as the raw material to prepare a thioether compound, then employing sodium hypochlorite to undergo oxidation in an alkaline solution to obtain a pantoprazole sodium crude product; 2. at a temperature of 4DEG C, adding anhydrous methanol into the pantoprazole sodium crude product, carrying out stirring and suction filtration to remove the methanol solution, thus obtaining a filter cake of pantoprazole sodium; 3. dissolving the pantoprazole sodium-containing filter cake in water, heating the obtained aqueous solution to 70DEG C, maintaining the state for certain time and performing concentration, then adding ethanol, conducting gradient reduction of temperature, and performing re-crystallization to obtain purified pantoprazole sodium; 4. subjecting the crystallized pantoprazole sodium to centrifugal washing and drying; and 5. crushing the dried pantoprazole sodium into ultrafine powder by airflow, and carrying out recovery and packaging.

Description

Technical field [0001] The invention relates to a freeze-dried preparation of special ultrafine powder of pantoprazole sodium and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] Pantoprazole sodium, English name Pantoprazole Sodium, chemical name 5-difluoromethoxy-2-[(3,4-dimethoxy-2-pyridyl)methyl]sulfinyl-1H-benzene Bimidazole sodium salt, molecular formula C 16 H 14 F 2 N 3 NaO 4 S, molecular weight 405.36, structural formula: [0003] [0004] The main component of pantoprazole sodium is pantoprazole sodium, which is a proton pump inhibitor. + -K + The two sites of the ATPase system covalently bind to the left and the last step of gastric acid production; and H + -K + The combination of ATPase system can cause its anti-gastric acid secretion effect to last for more than 24 hours. Clinically, it is mainly used to treat memorable upper gastrointestinal bleeding caused by gastric ulcer, duodenal ulcer, acute gastric muco...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/19C07D401/12
Inventor 徐全华傅苗青李凤生陈宇东厉达中
Owner 杭州澳亚生物技术股份有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com