Ezetimibe solid orally-taken preparation for degrading cholesterol and preparing method of ezetimibe solid orally-taken preparation for degrading cholesterol

A technology for ezetimibe and oral preparations, applied in the field of pharmaceutical preparations, can solve problems such as poor water solubility of ezetimibe and general solubilizer effect, and achieve the effects of easy industrialized large-scale production, rapid drug dissolution, and simple preparation method

Inactive Publication Date: 2015-10-21
严白双
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the problem of poor water solubility of ezetimibe, the inventor tried to disperse ezetimibe in water, and then added a solubilizer to promote its dissolution, but the effects of various solubilizers were average.

Method used

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  • Ezetimibe solid orally-taken preparation for degrading cholesterol and preparing method of ezetimibe solid orally-taken preparation for degrading cholesterol
  • Ezetimibe solid orally-taken preparation for degrading cholesterol and preparing method of ezetimibe solid orally-taken preparation for degrading cholesterol
  • Ezetimibe solid orally-taken preparation for degrading cholesterol and preparing method of ezetimibe solid orally-taken preparation for degrading cholesterol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023]

[0024]

[0025] Preparation Process:

[0026] Dissolve trometamol in prescription quantity in ethanol, add prescription quantity of ezetimibe, stir to dissolve, dry at 50°C to remove ethanol to obtain mixture, pass this mixture through 60 mesh sieve, and then mix with prescription quantity of microcrystalline Cellulose, sodium carboxymethyl starch, and magnesium stearate are mixed evenly, and compressed into tablets.

Embodiment 2

[0028]

[0029] Preparation Process:

[0030] Dissolve trometamol in prescription quantity in ethanol, add prescription quantity of ezetimibe, stir to dissolve, dry at 55°C to remove ethanol to obtain mixture, pass this mixture through 80 mesh sieve, and then mix with prescription quantity of microcrystalline Cellulose, lactose, crospovidone, and magnesium stearate are mixed evenly and compressed into tablets.

Embodiment 3

[0032]

[0033] Preparation Process:

[0034] Dissolve tromethamine in prescription quantity in ethanol, add prescription quantity of ezetimibe, stir to dissolve, dry at 50°C to remove ethanol to obtain mixture, pass this mixture through 65 mesh sieve, and then mix with prescription quantity of microcrystalline Cellulose, sodium carboxymethyl starch, and magnesium stearate are mixed evenly, and compressed into tablets.

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PUM

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Abstract

The invention discloses an ezetimibe solid orally-taken preparation for degrading cholesterol and a preparing method of the ezetimibe solid orally-taken preparation for degrading cholesterol. The preparation is prepared through a medicine-contained compound and acceptable auxiliary materials on pharmacy; preferentially, the direct compression method is adopted for making a tablet; and the medicine-contained compound is an ezetimibe-tromethamine compound. The preparation is rapid in medicine dissolution and simple in preparing method, raw materials do not need to be specially smashed, complex preparation devices are not needed, and industrialization large-scale production of the ezetimibe solid orally-taken preparation is easy to achieve.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a solid oral preparation, in particular to a cholesterol-lowering ezetimibe solid oral preparation and a preparation method thereof. Background technique [0002] Ezetimibe is a white crystalline powder, easily soluble in ethanol, methanol and acetone, but almost insoluble in water. Ezetimibe has a melting point of about 163°C and is stable at room temperature. Its structural formula is as follows: [0003] [0004] 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 lipid-lowering treatments (such as LDL-C apheresis), can als...

Claims

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Application Information

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IPC IPC(8): A61K31/397A61K9/20A61K47/18A61P3/06
Inventor 严白双
Owner 严白双
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