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Oral tablet containing 2-[(4-methoxy-3-methyl)-2-pyridyl]ethylsulfonyl-5-(1-H-pyrrole-1-yl)-1H-benzimidazole

A technology of methylsulfinyl, oral tablet, applied in the 2-[(4-methoxy-3-methyl)-2-pyridyl]methylsulfinyl-5-(1H-pyrrole -1-yl)-1H-benzimidazole in the field of oral tablets, which can solve problems such as difficulty in stabilizing the effect

Inactive Publication Date: 2005-01-19
IL YANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the present inventors have found that it is difficult to obtain the desired stabilizing effect by simply mixing the acid-labile active ingredient of the present invention with a base compound

Method used

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Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach

[0017] Mg(OH) that will be particularly suitable for stabilizing the active ingredient IY-81149 of the present invention 2 , Na 2 HPO 4 , NaHCO 3 , arginine and the like are mixed with the active ingredient at a molar ratio of 1:2, microcrystalline cellulose as an excipient and magnesium stearate as a lubricant are added to the mixture, and the resulting mixture is compressed into tablets . Using a conventional pan coater, the obtained bare tablets are coated with a film-forming material for the first time and then with an enteric coating material for a second time.

[0018] A control was also prepared in the same manner as the above method, which control did not contain the stabilizer used in the stability test of the enteric-coated tablet containing IY-81149.

Embodiment 1

[0020] IY-81149 10.0mg

[0021] Magnesium Hydroxide 3.2mg

[0022] Microcrystalline Cellulose 135.3mg

[0023] Magnesium Stearate 1.5mg

[0024] Hydroxypropyl methylcellulose 2910 5.0mg

[0025] Macrogol 6000 1.0mg

[0026] Hydroxypropyl Methylcellulose Phthalate 20.0mg

[0027] Cetyl Alcohol 2.0mg

[0028] Myvacet TM 2.0mg

[0029] Appropriate amount of purified water

[0030] Proper amount of ethanol

[0031] Proper amount of acetone

[0032] IY-81149 is mixed with magnesium hydroxide, microcrystalline cellulose, and magnesium stearate. The mixture was compressed into tablets and the resulting tablets were first coated with a solution consisting of hydroxypropylmethylcellulose 2910 and polyethylene glycol 6000 dissolved in purified water and ethanol Tablets prepared in a mixed solvent and coated a second time with a solution consisting of hydroxypropylmethylcellulose phthalate, cetyl alcohol and Myvacet TM Dissolved in a mixed solvent of...

Embodiment 2

[0034] IY-81149 10.0mg

[0035] Magnesium Hydroxide 3.2mg

[0036]Microcrystalline Cellulose 135.3mg

[0037] Magnesium Stearate 1.5mg

[0038] Hydroxypropyl methylcellulose 2910 5.0mg

[0039] Macrogol 6000 1.0mg

[0040] Kollicoat TM MAE30DP 36mL

[0041] (12.0 mg, solid)

[0042] Propylene glycol 1.0mg

[0043] Appropriate amount of purified water

[0044] Proper amount of ethanol

[0045] IY-81149 is mixed with magnesium hydroxide, microcrystalline cellulose, and magnesium stearate. The mixture was compressed into tablets and the resulting tablets were first coated with a solution consisting of hydroxypropylmethylcellulose 2910 and polyethylene glycol 6000 dissolved in purified water and ethanol prepared in a mixed solvent and coated a second time with a solution made by mixing purified water and propylene glycol and then mixing with Kollicoat TM Made by mixing MAE30DP.

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PUM

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Abstract

The preparation method of an oral tablet includes the following steps: mixing the active component 2-[(4-methoxy-3-methyl)-2-pyridyl] methyl sulfinyl-5-(1H-pyrrolyl-1-gruop)-1H-benzimidazole, alkaline compound as stabilizing agent and proper medicinal additive, tableting the obtained the above-mentioned mixture to obtain naked tablet, using film-forming material to make first coating and using enteric soluble coating material to make secondary coating so as to obtain the invented tablet.

Description

technical field [0001] The present invention relates to tablets containing 2-[(4-methoxy-3-methyl)-2-pyridyl]methylsulfinyl-5-(1H-pyrrol-1-yl)-1H-benzimidazole agent (hereinafter referred to as IY-81149). More specifically, the present invention relates to IY-81149 as an active ingredient, which has potent inhibitory activity on gastric acid secretion by irreversibly inhibiting proton pumps involved in gastric acid secretion. The object of the present invention is to provide a stable oral tablet containing IY-81149. Background technique [0002] The active ingredient 2-[(4-methoxy-3-methyl)-2-pyridyl]methylsulfinyl-5-(1H-pyrrol-1-yl)-1H-benzimidazole is the present invention A new type of compound developed by the author, and its application as a product patent is currently pending or authorized in 27 countries including South Korea, Japan, and the United States. This compound has an excellent antiulcer effect by irreversibly inhibiting proton pumps, and although it is st...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4439A61P1/04
Inventor 金东渊朴东雨金熙埈
Owner IL YANG PHARMA CO LTD
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