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Ezetimibe tablet composition

The technology of Maibu tablet and ezetimibe is applied in the field of medicine, which can solve the problems of easy clogging of nozzles, poor material dispersibility, influence on curative effect, etc., and achieve the effects of improving drug release rate, improving utilization rate and improving drug efficacy.

Inactive Publication Date: 2014-12-03
SICHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of taking tablets, their bioavailability is often limited by the dissolution rate, which affects the curative effect.
[0005] The patent application number is 201410158848.7, and the application name is a preparation method of ezetimibe tablets. A preparation method of ezetimibe tablets is disclosed. It uses supercritical carbon dioxide fluid to preliminarily process ezetimibe tablets, and then directly Adding auxiliary materials for tableting treatment, the applicant found that although the method can make the particle size distribution uniform, the particle agglomeration phenomenon is also obvious, the material dispersibility is poor, and the nozzle is easy to block during the preparation process, which is very Not suitable for large-scale industrial applications

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Ezetimibe tablet composition, comprising the following weight components:

[0033] ezetimibe 280

[0034] Lactose 2100

[0035] Croscarmellose sodium 270

[0036] Sodium Lauryl Sulfate 50

[0037] Povidone K30 80

[0038] Magnesium Stearate 28

[0039] 30% ethanol 720.

[0040] The dissolution rate of Example 1 is 85.1%, and the content of related substances is less than or equal to 0.3%.

Embodiment 2

[0042] Ezetimibe tablet composition, comprising the following weight components:

[0043] Ezemabu 300

[0044] Lactose 2400

[0045] Croscarmellose sodium 270

[0046] Sodium Lauryl Sulfate 60

[0047] Povidone K30 80

[0048] Magnesium Stearate 30

[0049] 30% ethanol 720.

[0050] The dissolution rate of Example 2 is 86.2%, and the content of related substances is less than or equal to 0.28%.

Embodiment 3

[0052] Ezetimibe tablet composition, comprising the following weight components:

[0053] ezetimibe 320

[0054] Lactose 2400

[0055] Croscarmellose sodium 300

[0056] Sodium Lauryl Sulfate 80

[0057] Povidone K30 80

[0058] Magnesium Stearate 30

[0059] 30% ethanol 720.

[0060] The dissolution rate of Example 3 is 86.8%, and the content of related substances is less than or equal to 0.25%.

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Abstract

The invention discloses an ezetimibe tablet and a preparation method thereof. Ezetimibe with a certain angle of repose is selected as a raw material, a technology comprising the steps of firstly mixing an ezetimibe main material with lauryl sodium sulphate and crosslinked sodium carboxymethylcellulose, then mixing and wrapping with part of lactose and controlling the mixing time is adopted, particles of the obtained mixed powder are uniformly wrapped, then a binding agent and a lubricating agent are used for continuously preparing the ezetimibe tablet, wherein focus of the whole process is as follows: various factors are matched and controlled moderately, the finally obtained tablet is good in stability, particles are uniform, the dispersity is good, and no agglomeration phenomenon is caused, so that the ezetimibe tablet is applicable to mass production.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an ezetimibe tablet composition. Background technique [0002] Ezetimibe is a white crystalline powder. It is a drug used to regulate blood lipids jointly developed by Schering-Plough and Merck. It is the first cholesterol regulation inhibitor with a single-ring β-lactam functional group successfully synthesized. Ezetimibe is easily soluble in ethanol, methanol and acetone, insoluble in water, and relatively stable at room temperature. [0003] Ezetimibe has a unique mode of action. It mainly acts on the small intestine to inhibit the absorption of cholesterol without affecting the absorption of other nutrients. It has less adverse reactions to the human body and is better tolerated by patients than other lipid-lowering drugs. [0004] Clinically, ezetimibe can be used alone or in combination with statins. Currently, ezetimibe is often taken in the form of tablets. However, in the proc...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/397A61K47/26A61P3/06
Inventor 包莹刘萍陈继源
Owner SICHUAN PHARMA