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Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media

A technology for esomeprazole magnesium and enteric-coated preparations, which is applied in the field of pharmaceutical preparation analysis and detection, can solve the problem of accurate calculation of unfavorable dissolution results, and difficulty in accurately evaluating the dissolution process of esomeprazole magnesium enteric-coated preparations. Discover research reports and other issues to achieve the effect of strong practicability, high sensitivity and good reproducibility

Active Publication Date: 2016-10-12
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is a sulfoxide group in the structure of esomeprazole magnesium, which makes it extremely sensitive to acidic media and easy to degrade, which also leads to its ineffectiveness in media such as pH 6.0 phosphate buffer, pH 6.8 phosphate buffer, and water. Degradation occurs during the dissolution process, which is not conducive to the accurate calculation of dissolution results
However, searching the literature and patents on the dissolution control method of esomeprazole magnesium preparations did not find any relevant research reports
This is also difficult to accurately evaluate the dissolution process of esomeprazole magnesium enteric-coated preparations

Method used

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  • Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media
  • Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media
  • Method for measuring dissolution rates of esomeprazole magnesium enteric-coated preparation in different media

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Degradation Law of Esomeprazole Magnesium Enteric-coated Tablets or Enteric-coated Pellet Capsules in Phosphate Buffered Saline at pH 6.0

[0042] Take the specification of 20mg Esomeprazole magnesium enteric-coated tablets or enteric-coated micropill capsules (remove the capsule shell, take the contents, the same below), put in a mortar, grind finely, weigh 100mg into a 20ml volumetric flask, add 0.0125mol / L Sonicate 12mL of sodium hydroxide solution for 5min, add 7.5ml of ethanol to continue sonicating for 3min, and dilute to volume with 0.0125mol / L sodium hydroxide solution. Filtrate, take 2ml of the filtrate into a 100ml volumetric flask, make up to volume with pH6.0 phosphate buffer, put it in a water bath at 37°C±0.5°C, and set at 0, 15, 30, 45, 60, 90, 120, 180, 240min respectively Take a sample, filter. Take 5ml of the continued filtrate into a vial, add 600μl of 0.5mol / L sodium hydroxide respectively, mix well, accurately draw 20μl into the liquid ...

Embodiment 2

[0051] Example 2. Degradation Law of Esomeprazole Magnesium Enteric-coated Tablets or Enteric-coated Pellet Capsules in Water

[0052] Take the specification of 20mg Esomeprazole magnesium enteric-coated tablets or enteric-coated micropill capsules (remove the capsule shell, take the contents) in a mortar, grind finely, weigh 100mg into a 20ml volumetric flask, and add 0.0125mol / L sodium hydroxide Solution 12mL, ultrasonic 5min, add 7.5ml ethanol and continue ultrasonication for 3min, 0.0125mol / L sodium hydroxide solution to volume, filter, take 2ml of filtrate to 100ml volumetric flask, adjust pH to 7.0±0.05 with 0.1mol / L hydrochloric acid , then dilute to volume with water, place in a water bath at 37°C±0.5°C, sample and filter at 0, 30, 60, 90, 120, 180, 240, 300, and 360 minutes respectively, take 5ml of the filtrate, add 0.25mol / L hydrogen respectively Add 600 μl of sodium oxide, mix well, accurately pipette 20 μl into the liquid chromatograph, and record the chromatogr...

Embodiment 3

[0061] Example 3. Accuracy (sample recovery) verification of the dissolution rate determination of esomeprazole magnesium enteric-coated tablets

[0062] (1) The recovery rate of sample addition in the phosphate buffer medium of pH 6.0

[0063] Reference substance solution preparation: Weigh about 20 mg of omeprazole, put it in a 100ml measuring bottle, dissolve it with ethanol and dilute to the mark, and use it as the reference substance solution.

[0064] The preparation of need testing solution: get the blank auxiliary material in the esomeprazole magnesium enteric-coated tablet prescription of specification 20mg, grind finely, take by weighing 100mg powder in 100ml volumetric flask, add 0.0125mol / L sodium hydroxide solution, Sonicate for 5min, add 37.5ml of ethanol, sonicate for 3min, and dilute to the mark with 0.0125mol / L sodium hydroxide solution. Filter, take 5ml of continued filtrate and put it in a 100ml volumetric flask, take 9 parts in total, add three parts of re...

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Abstract

The invention discloses a method for measuring the dissolution rates of an esomeprazole magnesium enteric-coated preparation in different media. The method is characterized in that a step of establishing a linear regression equation is added, that is, a sodium hydroxide solution and ethyl alcohol are added into the content of an esomeprazole magnesium enteric-coated tablet or capsule to perform ultrasonic dissolution, then filtration is conducted, the filtrate is taken out, subjected to constant-volume treatment and then placed in a water bath of 37+ / -0.5 DEG C, a sample is taken at each dissolution time and is injected into a high performance liquid chromatograph, chromatograms are recorded, and the linear relationship between a main peak and a relative retention time 2.7 impurity peak is found out from the area change relationship between the main peak and the relative retention time 2.7 impurity peak to obtain the linear regression equation which is applied to calculation of the dissolution quantity of esomeprazole magnesium. The method solves the problem that the dissolution rate of the esomeprazole magnesium enteric-coated preparation cannot be accurately measured in the prior art, and has the advantages of being convenient, quick, accurate, excellent in repeatability, high in sensitivity and strong in practicability during operation.

Description

technical field [0001] The invention relates to the field of analysis and detection of pharmaceutical preparations, in particular to a method for measuring the dissolution rate of esomeprazole magnesium enteric-coated preparations in different media. Background technique [0002] Esomeprazole Magnesium (Bis-S-5-methoxy-2-{[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]sulfin Acyl-1H-benzimidazole magnesium trihydrate) a new proton pump inhibitor with the molecular formula C 34 h 36 MgN 6 o 6 S 2 ·3H 2 O, molecular weight 767.17, chemical structure formula is as follows: [0003] [0004] Esomeprazole magnesium, also known as esomeprazole magnesium, is the S-configuration optical isomer of omeprazole, which is weakly alkaline and can be found in the high acid environment of the acid-secreting microtubules of parietal cells Concentrated in and converted into the active substance sulfenic acid amide, and then combined with H on parietal cells + -K + -The sulfhydryl group...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02G01N30/06
CPCG01N30/02G01N30/06G01N2030/027
Inventor 谭银合余思琴钟露露颜楚红赵明馨杨新明蒋林波
Owner SUN YAT SEN UNIV
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