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Preparation method of ezetimibe tablet

A technology of ezetimibe and hydroxypropyl cellulose, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Problems such as the production process of wheat cloth flakes and the inability to fully demonstrate the superiority of micronization

Inactive Publication Date: 2014-06-25
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, direct micronization of drugs has a common disadvantage: micronization is very easy to agglomerate, often making it unable to fully demonstrate the advantages of micronization
[0010] In the prior art, none of them can provide a production process that can quickly dissolve ezetimibe tablets

Method used

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  • Preparation method of ezetimibe tablet
  • Preparation method of ezetimibe tablet
  • Preparation method of ezetimibe tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028] Preparation Process:

[0029] (1) Hydroxypropyl cellulose and ezetimibe were weighed for the prescription amount, dissolved in ethanol, and mannitol was weighed for the prescription amount and dissolved in water;

[0030] (2) Set the pressure of the supercritical carbon dioxide fluid to 10MPa and the temperature to 35°C, pass the supercritical carbon dioxide fluid and the above two solutions into a coaxial three-channel nozzle respectively, and use the anti-solvent effect of the supercritical carbon dioxide fluid to obtain Superfine powder blend of ezetimibe, hydroxypropyl cellulose and mannitol;

[0031] (3) Mix the superfine particle mixed powder with microcrystalline cellulose, crospovidone and magnesium stearate evenly, and directly compress it into tablets.

Embodiment 2

[0033]

[0034]

[0035] Preparation Process:

[0036] (1) Hydroxypropyl cellulose and ezetimibe were weighed for the prescription amount, dissolved in ethanol, and mannitol was weighed for the prescription amount and dissolved in water;

[0037] (2) Set the pressure of the supercritical carbon dioxide fluid to 50MPa and the temperature to 60°C, pass the supercritical carbon dioxide fluid and the above two solutions into a coaxial three-channel nozzle respectively, and use the anti-solvent effect of the supercritical carbon dioxide fluid to obtain Superfine powder blend of ezetimibe, hydroxypropyl cellulose and mannitol;

[0038] (3) Mix ultrafine granule mixed powder with microcrystalline cellulose, starch, crospovidone, sodium carboxymethyl starch, and zinc stearate, and directly compress into tablets.

Embodiment 3

[0040]

[0041] Preparation Process:

[0042] (1) Hydroxypropyl cellulose and ezetimibe were weighed for the prescription amount, dissolved in ethanol, and mannitol was weighed for the prescription amount and dissolved in water;

[0043] (2) Set the pressure of the supercritical carbon dioxide fluid to 30MPa and the temperature to 50°C, pass the supercritical carbon dioxide fluid and the above two solutions into a coaxial three-channel nozzle respectively, and use the anti-solvent effect of the supercritical carbon dioxide fluid to obtain Superfine powder blend of ezetimibe, hydroxypropyl cellulose and mannitol;

[0044] (3) Mix the superfine particle mixed powder with microcrystalline cellulose, crospovidone and magnesium stearate evenly, and directly compress it into tablets.

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Abstract

The invention discloses a preparation method of an ezetimibe tablet. The preparation method comprises the following steps of (1) dissolving hydroxypropyl cellulose and ezetimibe into ethanol, and dissolving a carrier material mannitol into a water solution; (2) respectively introducing a supercritical carbon dioxide fluid and the two solutions into a coaxial three-channel nozzle by setting the pressure and temperature of the supercritical carbon dioxide fluid to 10-50 MPa and 35-60 DEG C, and acquiring ultrafine granule mixed powder which contains the ezetimibe, the hydroxypropyl cellulose and the mannitol by utilizing the anti-solvent effect of the supercritical carbon dioxide fluid; (3) directly tabletting the ultrafine granule mixed powder and pharmaceutically acceptable auxiliary materials. The method disclosed by the invention can be used for fast dissolving the ezetimibe, can achieve the dissolution rate of the ezetimibe tablet by 95% for 5 minutes and does not contain the surface active agent.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a preparation method of ezetimibe tablets. Background technique [0002] The chemical name of ezetimibe is 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4 -Hydroxyphenyl)-2-azetidinone, which has the following chemical structure: [0003] [0004] Ezetimibe is a white crystalline powder, easily soluble in ethanol, methanol and acetone, but almost insoluble in water. The melting point of ezetimibe is about 163°C, and it is stable at room temperature. Ezetimibe is mainly used clinically for primary hypercholesterolemia. As an adjuvant therapy other than diet control, this product can be used alone or in combination with HMG-CoA reductase inhibitors such as statins to treat hypercholesterolemia. Lowering total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (ApoB), or as an adjunct to other ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/397A61K47/10A61K47/38A61P3/06
Inventor 胡德栋叶卫华王琦张守忠段淑娜
Owner QINGDAO UNIV OF SCI & TECH
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