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Pharmaceutical composition containing esomeprazole

A technology of esomeprazole and composition, which is applied in the field of pharmaceutical composition containing esomeprazole, and can solve the problems such as the lack of stability of esomeprazole magnesium salt

Inactive Publication Date: 2010-08-18
CTC BIO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, esomeprazole magnesium salt also does not have good stability equally, therefore, in order to improve the stability of described salt, researchers have carried out a large amount of research work

Method used

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  • Pharmaceutical composition containing esomeprazole
  • Pharmaceutical composition containing esomeprazole
  • Pharmaceutical composition containing esomeprazole

Examples

Experimental program
Comparison scheme
Effect test

experiment Embodiment 1

[0028] Selection of Polymer

[0029]As shown in Table 1 below, each polymer was mixed with esomeprazole free base in a weight ratio of 1:3 or 1:6, and each mixture was compacted with a roller compactor, and become granular. All conditions were kept the same to maintain an equilibrium temperature during compaction. Stability testing was carried out by storing the prepared granules in brown plastic bottles under accelerated conditions (40° C., 75% RH) for one week, and the generated impurities were analyzed by HPLC. The results are shown in Tables 2 and 3 in full.

[0030] The impurity analysis process is as follows: crush each particle, weigh about 20 mg of esomeprazole and put it into a 100 mL flask. Add 10 mL of methanol to the flask and mix well. Then 20 mL of phosphate buffered saline (pH=11.0) was added and the flask was sonicated. Water was added to bring the volume of the solution to 100 mL, and the solution was subjected to membrane filtration to prepare a test sa...

experiment Embodiment 2

[0047] Production and Evaluation of Solid Dispersion

[0048] The solid dispersion was prepared according to the ingredients and contents in Table 4 below. Example 1 was prepared as follows: polyvinylpyrrolidone was dissolved in ethanol, an aqueous NaOH solution was added thereto, and mixed. Dissolve esomeprazole free base in the mixed solution. Lactose and colloidal silicon dioxide were then added to the solution and mixed. The solution was dried at 40°C and granulated to make solid dispersion particles. Example 2 was prepared as follows: polyvinylpyrrolidone was dissolved in ethanol, and esomeprazole free base was dissolved therein. Magnesia and colloidal silica were then added to the solution and mixed. The solution was dried at 40°C and granulated to make solid dispersion particles. Example 3 was prepared as follows: hydroxypropylmethylcellulose (5cP) was dissolved in ethanol, and an aqueous NaOH solution was added thereto. Esomeprazole free base was dissolved in th...

experiment Embodiment 3

[0055] Stability Detection of Simple Mixture

[0056] Test samples were prepared by simply mixing the ingredients and amounts according to Table 6, Simple Mix.

[0057] Table 6

[0058]

[0059] The stability of Examples 4-6 was evaluated according to the same method as Experimental Example 1. The results are shown in Table 7 below.

[0060] Table 7

[0061]

[0062] As shown in Table 7, simple mixing of ingredients was shown not to increase the stability of esomeprazole.

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Abstract

The present invention relates to esomeprazole free base or its alkali salt-containing composition which stability is improved and is easy to manufacture.

Description

technical field [0001] The present invention relates to pharmaceutical formulations containing esomeprazole free base or basic salts of esomeprazole, which pharmaceutical formulations have improved stability. Background technique [0002] Esomeprazole ((S)-5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)methylsulfinyl]-3H-benzo Imidazole) is a proton pump inhibitor used in the treatment of gastric ulcer, gastroesophageal reflux and the like. The free base of esomeprazole is not ideal in terms of storage stability and physical properties. Specifically, esomeprazole free base has a melting point of about 45°C, making it difficult to prepare; moreover, its stability is so poor that after two months of storage at 25°C / 60% RH, its total The impurity content increased to around 1%. In addition, esomeprazole is less stable under alkaline conditions than under acidic or neutral conditions. [0003] Commercially available products utilize esomeprazole magnesium salt to enhance the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/44A61K9/36A61P1/04
CPCA61K9/1611A61K9/2009A61K31/4439A61P1/04A61K9/14A61K31/44A61K47/30
Inventor 郭成信李凤相权度又全泓烈文志允李东榛
Owner CTC BIO INC
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