Ezetimibe tablet and preparation method thereof

A technology of ezetimibe and microcrystalline cellulose, applied in the field of ezetimibe tablets and their preparation, can solve the problems of unsustainable and stable release of drug effect, damage to human organs and tissues, large fluctuation of absorption in the body, and the like, Achieve the effect of adapting to large-scale industrial production, simplifying the production process and improving safety

Inactive Publication Date: 2016-01-06
WUXI FORTUNE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the release of ezetimibe tablets in the prior art varies greatly in gastric juice, and the absorption fluctuations in the body are relatively large. The drug effect of ezetimibe tablets in the human body cannot be released continuously and stably. If the dissolution of ezetimibe tablets is too fast, it will cause damage to human organs and tissues, and has certain side effects in pharmacology

Method used

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  • Ezetimibe tablet and preparation method thereof
  • Ezetimibe tablet and preparation method thereof
  • Ezetimibe tablet and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0030] Prescription quantity: 1000 tablets

[0031]

[0032] Among them, the particle diameter D of microcrystalline cellulose 102 15 48±2.4μm, D 85 65±1.5μm, porosity (5.0±0.4)×10 -5 cm 3 / g.

[0033] Pass lactose, sodium carboxymethyl cellulose and sodium lauryl sulfate through a 80-mesh sieve (sodium lauryl sulfate should be crushed if necessary), and microcrystalline cellulose 102 and magnesium stearate through a 60-mesh sieve respectively Add the sodium lauryl sulfate, sodium carboxymethyl cellulose and ezetimibe of the prescribed amount into the mixer successively, mix for 5 minutes to mix evenly to obtain a mixed powder, and pass the mixed powder through a 40-mesh sieve; then Add lactose in equal increments; transfer the mixed powder to the wet granulator, set the stirring and chopping speed, and mix for 10 minutes; set the stirring and chopping speed, start the wet mixing granulator, and start spraying the poly Vitone K30 aqueous solution, the spray time is con...

Embodiment 2

[0035] Prescription quantity: 1000 tablets

[0036]

[0037] Among them, the particle diameter D of microcrystalline cellulose 102 15 48±2.4μm, D 85 65±1.5μm, porosity (5.0±0.4)×10 -5 cm 3 / g.

[0038] Pass lactose, sodium carboxymethyl cellulose and sodium lauryl sulfate through a 80-mesh sieve (sodium lauryl sulfate should be crushed if necessary), and microcrystalline cellulose 102 and magnesium stearate through a 60-mesh sieve respectively net; the sodium lauryl sulfate, sodium carboxymethyl cellulose and ezetimibe of prescription quantity are added in the mixer successively, mix 5min and mix evenly to obtain mixed powder, then the mixed powder is passed through 40 mesh sieves; then Add lactose in equal increments; transfer the mixed powder to the wet granulator, set the stirring and chopping speed, and mix for 10 minutes; set the stirring and chopping speed, start the wet mixing granulator, and start spraying the poly Vitone K30 aqueous solution, the spray time is...

Embodiment 3

[0040] Prescription quantity: 1000 tablets

[0041]

[0042] Among them, the particle diameter D of microcrystalline cellulose 102 15 48±2.4μm, D 85 65±1.5μm, porosity (5.0±0.4)×10 -5 cm 3 / g.

[0043] Pass lactose, sodium carboxymethyl cellulose and sodium lauryl sulfate through a 80-mesh sieve (sodium lauryl sulfate should be crushed if necessary), and microcrystalline cellulose 102 and magnesium stearate through a 60-mesh sieve respectively Net; Add sodium lauryl sulfate, sodium carboxymethyl cellulose and ezetimibe in the mixer in turn in the prescribed amount, mix for 5 minutes to mix evenly to obtain a mixed powder, and pass the mixed powder through a 40-mesh sieve; then pass Add lactose in equal increments; transfer the mixed powder to the wet granulator, set the stirring and chopping speed, and mix for 10 minutes; set the stirring and chopping speed, start the wet mixing granulator, and start spraying polydimensional Ketone K30 aqueous solution, the spray time is...

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Abstract

The invention provides an ezetimibe tablet and a preparation method thereof. The ezetimibe tablet is prepared from the following components in parts by weight: 10 parts of ezetimibe, 10 parts of a disintegrating agent, 2 parts of a solubilizing agent, 55 to 70 parts of a filling agent, 5 to 15 parts of microcrystalline cellulose, 5 parts of an adhesive and 0.5 parts of a lubricant. According to the ezetimibe tablet disclosed by the invention, the fluctuation of the dissolution of the ezetimibe tablet can be effectively reduced, the dissolution difference is reduced, the safety of the ezetimibe tablet in a medicine using process is improved, and the fluctuation of in-vivo absorption of the ezetimibe tablet is reduced; meanwhile, according to the preparation method of the ezetimibe tablet, a production process is simplified, and the method can adapt to large-scale industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an ezetimibe tablet and a preparation method thereof. Background technique [0002] Ezetimibe Tablets is a powerful blood lipid-lowering drug, jointly developed by Schering-Plough and Merck & Co., Ltd., and is the only selective cholesterol absorption inhibitor currently on the market. Ezetimibe is white crystalline powder, very soluble in ethanol, methanol, acetone and dimethylformamide, slightly soluble in acetonitrile, insoluble in water. The melting point of ezetimibe is about 163°C, and it is relatively stable at room temperature. Ezetimibe is mainly used clinically to treat primary hypercholesterolemia, and can be used alone or in combination with HMG-CoA reductase inhibitors. Ezetimibe inhibits the absorption of cholesterol mainly by acting on the small intestine, and will not affect the absorption of other nutrients. Patients tolerate it better than other lipid-lowerin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/397A61P3/06
Inventor 米靖宇陈跃坚葛亮卢欣徐建国李晓明
Owner WUXI FORTUNE PHARMA
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