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Method for preparing stable esomeprazole enteric-coated pills

A technology for esomeprazole enteric and esomeprazole magnesium is applied in the field of preparation of esomeprazole enteric-coated pellets, and can solve the problems of enteric-coated drugs disintegration and poor drug dissolution, influence and complicated preparation process and other problems to achieve the effect of saving time, overcoming the complexity of the preparation process and simplifying the process

Inactive Publication Date: 2012-04-11
SHANGHAI SUNTECH PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method also has the following defects: firstly, the preparation process is complicated; secondly, most of the isolation layer materials are water-insoluble materials, which have good waterproof performance, but may have adverse effects on the disintegration and drug dissolution of enteric-coated drugs. influences

Method used

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  • Method for preparing stable esomeprazole enteric-coated pills
  • Method for preparing stable esomeprazole enteric-coated pills
  • Method for preparing stable esomeprazole enteric-coated pills

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Compatibility experiment between embodiment 1 bulk drug and auxiliary material

[0030] 1. Mix 50mg of esomeprazole magnesium and 50mg of enteric-coated materials together, put them in a sample box at 60°C under the condition of sealing and avoiding light, and take samples at one week and two weeks for Esso Meprazole magnesium content detection. The proportioning ratio between raw materials and auxiliary materials is shown in Table 1.

[0031] Under table 1 anhydrous condition, the proportioning between bulk drug and auxiliary material

[0032]

[0033] Result: The content of esomeprazole magnesium in samples determined at one week and two weeks is shown in Table 2.

[0034] Under table 2 anhydrous condition, the compatibility test result between bulk drug and auxiliary material

[0035]

[0036]According to the content detection results in Table 2, the content of the active ingredient did not change significantly in the two-week reserved sample experiment, and...

Embodiment 2

[0045] 1. Preparation of pill core:

[0046] The ratio of each substance is as follows:

[0047]

[0048] The preparation steps are as follows:

[0049] 1) Dissolve hypromellose in 1000g of water, add esomeprazole magnesium into the above solution, stir and disperse evenly;

[0050] 2) Calcium carbonate and talcum powder are evenly dispersed in the water of 500g;

[0051] 3) Add the dispersion in step 2) to the dispersion in step 1), stir evenly, and set aside;

[0052] 4) Wrap the mixed solution in step 3) on the surface of the blank sugar core with a fluidized bed to prepare a pill-containing core. During the whole process, the temperature of the product is controlled at 25-30°C, and the ventilation volume is 1.0-1.4m 3 / min / kg, the spraying speed is 10-15g / min / kg, and the free moisture (detection value: 1.54%) of control containing pill core.

[0053] 2. Coating of enteric coating:

[0054] The ratio of each substance is as follows:

[0055]

[0056] The prepar...

Embodiment 3

[0065] 1. Preparation of drug-containing pill core:

[0066] The ratio of each substance is as follows:

[0067]

[0068] The preparation steps are as follows:

[0069] 1) Dissolve hypromellose in 1000g of water, add esomeprazole magnesium into the above solution, stir and disperse evenly;

[0070] 2) Calcium carbonate and talcum powder are evenly dispersed in 500g of water;

[0071] 3) Add the dispersion in step 2) to the dispersion in step 1), stir evenly, and set aside;

[0072] 4) Wrap the mixed solution in step 3) on the surface of the blank sugar core with a fluidized bed to prepare a pill-containing core. During the whole process, the temperature of the product is controlled at 30-40°C, and the ventilation volume is 0.7-1.0m 3 / min / kg, the spraying speed is 5-8g / min / kg, and the free moisture (detection value: 1.81%) of control containing pill core.

[0073] 2. Coating of enteric coating:

[0074] The ratio of each substance is as follows:

[0075]

[0076] ...

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Abstract

The invention provides a method for preparing stable esomeprazole enteric-coated pills, which comprises: (1) preparing pill cores containing a medicine and controlling the free water in the pill cores containing the medicine to be less than 2.5 weight percent; and (2) performing enteric coating under a condition that the free water content in the pill cores containing the medicine is controlled to be less than 2.5 weight percent. The invention provides a new feasible process method for replacing an isolating layer, thereby overcoming the complexity of a preparation process and adverse effect on enteric-coated medicine disintegration, exsolution or the like in the prior art.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to the preparation of enteric-coated pellets, more specifically to the preparation of esomeprazole enteric-coated pellets. Background technique [0002] Esomeprazole magnesium is the S-isomer of omeprazole, which reduces gastric acid secretion through a specific targeting mechanism and is a specific inhibitor of the proton pump in gastric parietal cells. For the treatment of gastroesophageal reflux disease, erosive reflux esophagitis, long-term maintenance therapy to prevent recurrence of cured patients with esophagitis, symptom control of gastroesophageal reflux disease, and for appropriate antimicrobial therapy combination It is used to eradicate Helicobacter pylori, and is used to heal duodenal ulcers associated with Helicobacter pylori infection and prevent recurrence of peptic ulcers associated with Helicobacter pylori. [0003] Esomeprazole magnesium is a weak base that co...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/32A61K9/36A61K31/4439A61P1/04
Inventor 何平钱晓明
Owner SHANGHAI SUNTECH PHARMA
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