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Lipid-lowering drug ezetimibe compound

The technology of a hypolipidemic drug and ezetimibe, which is applied in the field of medicine, can solve the problems of difficult patient acceptance, large preparation volume, and easy aging of solid dispersions after long-term storage.

Inactive Publication Date: 2015-11-04
QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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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
Solid dispersion technology can improve the dissolution rate and bioavailability of ezetimibe, but the preparation method is not very satisfactory, because the solid dispersion is easy to age after a long time, and it needs to use a large amount of carriers and some other pharmaceutical excipients , resulting in too large a volume of the preparation, which is not easily accepted by patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of ezetimibe compound

[0033] (1) Grind the crude ezetimibe, pass it through a 60-mesh sieve, and then add it to a mixed solution of methylnitrile, ethanol, and acetone whose volume is 8 times the weight of ezetimibe. The volume ratio is 3:3:1, 65 rev / min stirring for 20 minutes;

[0034] (2) Add acetonitrile with a volume 5 times the weight of ezetimibe under stirring at 110 rpm, and raise the temperature to 30°C at the same time;

[0035] (3) After adding the solution, let it stand for 2 hours, and add deionized water at 0°C dropwise under the condition of stirring at 80 rpm. The volume of deionized water is 10 times the weight of ezetimibe, and drop it at a constant speed within 2 hours complete;

[0036] (4) After the dropwise addition was completed, the temperature was lowered to -10°C, and stirring was continued at a stirring rate of 40 rpm for 2 h, and the crystals were precipitated after standing for 1 h, filtered, and vacuum-dried to...

Embodiment 2

[0038] Example 2: Preparation of ezetimibe compound

[0039] (1) Grind the crude product of ezetimibe, pass it through a 75-mesh sieve, and then add it to a mixed solution of methylnitrile, ethanol, and acetone whose volume is 9 times the weight of ezetimibe. The volume ratio is 3:3:1, stirred at 70 rpm for 20 minutes;

[0040] (2) Add acetonitrile with a volume 6 times the weight of ezetimibe under stirring at 115 rpm, and raise the temperature to 32.5°C at the same time;

[0041] (3) After adding the solution, let it stand still for 2.5 hours, and add deionized water at 2.5°C dropwise under the condition of stirring at 85 rpm. added;

[0042] (4) After the dropwise addition was completed, the temperature was lowered to -7.5°C, and stirring was continued for 2.5 hours at a stirring rate of 45 rpm, and crystals were precipitated after standing for 1.5 hours, filtered, and vacuum-dried to obtain ezetimibe crystals.

[0043] The X-ray powder diffraction spectrum obtained by...

Embodiment 3

[0044] Example 3: Preparation of ezetimibe compound

[0045] (1) Grind the crude ezetimibe, pass it through a 90-mesh sieve, and then add it to a mixed solution of methylnitrile, ethanol, and acetone whose volume is 10 times the weight of ezetimibe. The volume ratio is 3:3:1, stirred at 75 rpm for 20 minutes;

[0046] (2) Add acetonitrile with a volume 7 times the weight of ezetimibe under stirring at 120 rpm, and raise the temperature to 35°C at the same time;

[0047] (3) After adding the solution, let it stand still for 3 hours, and add deionized water at 5°C dropwise under the condition of stirring at 90 rpm. complete;

[0048] (4) After the dropwise addition was completed, the temperature was lowered to -5°C, and the stirring was continued for 3 hours at a stirring rate of 50 rpm, and the crystals were precipitated after standing for 2 hours, filtered, and vacuum-dried to obtain ezetimibe crystals.

[0049] The X-ray powder diffraction spectrum obtained by measuring th...

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Abstract

The present invention belongs to the technical field of drugs, and relates to a lipid-lowering drug ezetimibe compound. The lipid-lowering drug ezetimibe compound is measured by Cu-K alpha ray to obtain an X- ray powder diffraction pattern shown in Figure 1, the lipid-lowering drug ezetimibe compound has good liquidity, and a tablet prepared from the lipid-lowering drug ezetimibe compound has high dissolution, low impurity content, and good stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a blood lipid-lowering drug ezetimibe compound. Background technique [0002] 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 lipid-lowering treatments (such as LDL-C apheresis), can also be used in other It is used to reduce TC and LDL-C levels in HoFH patients when lipid-lowering therapy is ineffective. [0003] Ezetimibe is insoluble in water. When th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D205/08A61K31/397A61K9/20A61P3/06
CPCC07D205/08A61K9/0056A61K9/20C07B2200/13
Inventor 吕冠男
Owner QINGDAO LANSHENGYANG PHARMA & BIOTECH CO LTD
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