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Preparation method of ezetimibe medicine composition

A technology of ezetimibe and composition, which is applied in the field of preparation of ezetimibe pharmaceutical composition, can solve the problems of easy aging, large preparation volume, and difficult acceptance by patients, and achieve the effect of large-scale production and simple operation

Inactive Publication Date: 2014-03-26
CHINA RESOURCES SAIKE PHARMA
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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: micronized products are very easy to agglomerate, often making it unable to fully demonstrate the advantages of micronization. The co-grinding method used in the patent can reduce this aggregation phenomenon
Solid dispersion technology can improve the dissolution rate and bioavailability of ezetimibe, but this preparation method is not very satisfactory, because the solid dispersion body is easy to age after a long time; and it needs to use a large number of carriers and some other medicinal products. Excipients, resulting in too large a volume of the preparation, which is not easily accepted by patients

Method used

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  • Preparation method of ezetimibe medicine composition
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  • Preparation method of ezetimibe medicine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 One-step granulation of micronized ezetimibe

[0031] According to conventional methods, the ezetimibe API is first micronized, and the equipment used for the micronization treatment may be a jet mill, a ball mill or a fluid energy mill, or other equipment conventionally used in the art may be used. The particle size of ezetimibe should be controlled to be less than 10 μm by pre-crushing.

[0032] Formula (4000 tablets / batch)

[0033] No. Component Composition per tablet (mg) per batch (g) 1 Ezetimibe 10 40 2 lactose monohydrate 55 220 3 Microcrystalline Cellulose (Extra) 25 100 4 Croscarmellose sodium (additional) 3 12 5 Croscarmellose sodium (extra) 2 8 6 Povidone K30 3 12 7 Sodium dodecyl sulfate 1 4 8 Magnesium stearate 1 4

[0034] Preparation Process:

[0035] A. Dissolve the components of No. 6 and No. 7 in an appropriate amount of water to prepare adhesive solution I;...

Embodiment 2

[0041] Example 2 One-step granulation of micronized ezetimibe suspended in sodium lauryl sulfate solution

[0042] Prescription is with embodiment 1

[0043] Preparation Process:

[0044] A. Dissolve the component No. 7 in an appropriate amount of water to prepare binder solution I;

[0045] B. Suspend the micronized ezetimibe API (1) in the binder solution I, grind and mix evenly with a colloid mill to obtain the suspension solution II.

[0046] C. Add the components of serial numbers 2 and 4 into the fluidized bed and mix thoroughly to obtain mixture III;

[0047] D. Add the suspension solution Ⅱ to the mixture Ⅲ by spraying, granulate and dry to prepare granules Ⅳ; the fluidized bed parameters are set at 60°C for the inlet air temperature and 55M for the inlet air volume 2 / h, spray speed 4±2g / min.

[0048] E. Add the components of serial numbers 3, 5, 6, and 8 to Granule IV and mix evenly to prepare Granule V;

[0049] F. Compress granule V into tablets, the theoretic...

Embodiment 3

[0051] Example 3 One-step granulation of micronized ezetimibe suspended in sodium lauryl sulfate and HPMC E5 solution

[0052] Formula (4000 tablets / batch)

[0053] No. Component Composition per tablet (mg) per batch (g) 1 Ezetimibe 10 40 2 lactose monohydrate 55 220 3 Microcrystalline Cellulose (Extra) 25 100 4 Croscarmellose sodium (additional) 3 12 5 Croscarmellose sodium (extra) 2 8 6 HPMC E5 3 12 7 Sodium dodecyl sulfate 1 4 8 Magnesium stearate 1 4

[0054] Preparation Process:

[0055] A. Dissolve the components of No. 6 and No. 7 in an appropriate amount of water to prepare adhesive solution I;

[0056] B. Suspend the micronized ezetimibe API (1) in the binder solution I, grind and mix evenly with a colloid mill to obtain the suspension solution II.

[0057]C. Add the components of serial numbers 2 and 4 into the fluidized bed and mix thoroughly to obtain mixture III;

[0058] D. Add...

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Abstract

The invention relates to a preparation method of an ezetimibe medicine composition. The preparation method comprises the following steps: 1, suspending ezetimibe in a proper solvent to prepare an uniform ezetimibe micron-sized suspension; 2, adding the suspension into a diluent of the medicine composition in a spraying manner and drying to prepare particles and powder of the ezetimibe medicine composition; and 3, preparing the particles and the powder into the ezetimibe medicinal minimum dose unit. Firstly, the medicine is prepared into the micron-sized suspension, granulation is carried out in a one-step granulation manner, the medicine is added into the diluent and finally, the medicinal minimum dose unit is prepared. The preparation method has the benefits that the effect of the preparation method is superior to that of a method in which micronization is carried out after the slightly soluble medicament is separately micronized; and the operation is simple and the large scale production is easy.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a preparation method of an ezetimibe pharmaceutical composition. Background technique [0002] Ezetimibe (Ezetimibe), the chemical name is 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S )-(4-hydroxyphenyl)-2-azetidin (azetidin) ketone, its structural formula is: [0003] [0004] Ezetimibe is an oral, potent lipid-lowering drug that works differently from other lipid-lowering drugs, such as statins or bile acid sequestrants. Its mechanism of action is to attach to the brush border of small intestinal villi, inhibit the absorption of cholesterol, thereby reducing the transfer of cholesterol from the small intestine to the liver, reducing the storage of cholesterol in the liver and increasing the clearance of cholesterol in the blood. But it does not increase bile secretion (eg, bile acid sequestrants) and does not inhibit cholesterol synthes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/397A61P3/06
Inventor 高妍蒋玲敏张蕾杨琰王文峰
Owner CHINA RESOURCES SAIKE PHARMA
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