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Ezetimibe oral solid pharmaceutical composition

A technology for ezetimibe and composition, which is applied in the field of ezetimibe oral solid pharmaceutical composition and its preparation field, and can solve the problems of ineffective ezetimibe dissolution rate and the like

Inactive Publication Date: 2019-06-11
董贵雨
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Increasing the solubility of poorly soluble drugs by reducing the particle size is one of the commonly used methods in the field of preparations. Experiments have shown that reducing the particle size of ezetimibe raw materials in various ways to improve solubility does not effectively improve the solubility of ezetimibe. Dissolution rate increased to a satisfactory level

Method used

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  • Ezetimibe oral solid pharmaceutical composition
  • Ezetimibe oral solid pharmaceutical composition
  • Ezetimibe oral solid pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Example 1: Preparation of ezetimibe tablets with 5 mg specifications (unit: g)

[0108] prescription:

[0109] Raw materials

Dosage

Ezetimibe

5.0g

Soy Lecithin

5.0g

Polyvinylpyrrolidone

20.0g

microcrystalline cellulose

62.0g

Crospovidone

5.0g

colloidal silica

2.0g

Magnesium stearate

1.0g

Opadry

5% weight gain for plain tablets

Unit preparation weight (mg)

100mg

Co-made

1000 pieces

[0110] .

[0111] Preparation Process:

[0112] 1) Take the ezetimibe raw material, pulverize it, pass through a 100-mesh sieve, and set aside;

[0113] 2) Take the ezetimibe raw material drug obtained in step 1), the hydrophilic polymer polyvinylpyrrolidone, and the surfactant soybean lecithin are sequentially added to ethanol, stirred, and dissolved to obtain the ezetimibe lipid solution, which is drug adhesive;

[0114] 3) Take the filler microcrystalline cellulose ...

Embodiment 2

[0118] Example 2: Preparation of 10 mg ezetimibe tablet (unit: g)

[0119] prescription:

[0120] Raw materials

Dosage

Ezetimibe

10.0g

Soy Lecithin

10.0g

Polyvinylpyrrolidone

40.0g

microcrystalline cellulose

124.0g

Crospovidone

10.0g

colloidal silica

4.0g

Magnesium stearate

2.0g

Opadry

5% weight gain for plain tablets

Unit preparation weight (mg)

200mg

Co-made

1000 pieces

[0121] .

[0122] Preparation Process:

[0123] 1) Take the ezetimibe raw material, pulverize it, pass through a 100-mesh sieve, and set aside;

[0124] 2) Take the ezetimibe raw material drug obtained in step 1), the hydrophilic polymer polyvinylpyrrolidone, and the surfactant soybean lecithin are sequentially added to ethanol, stirred, and dissolved to obtain the ezetimibe lipid solution, which is drug adhesive;

[0125] 3) Take the filler microcrystalline cellulose and the disinteg...

Embodiment 3

[0129] Example 3: Preparation of 5 mg ezetimibe hard capsules (unit: g)

[0130] prescription:

[0131]

[0132]

[0133] Preparation Process:

[0134] 1) Take the ezetimibe raw material, pulverize it, pass through a 100-mesh sieve, and set aside;

[0135] 2) Take the ezetimibe raw material drug obtained in step 1), the hydrophilic polymer polyvinylpyrrolidone, and the surfactant soybean lecithin are sequentially added to ethanol, stirred, and dissolved to obtain the ezetimibe lipid solution, which is drug adhesive;

[0136] 3) Take the filler microcrystalline cellulose and the disintegrating agent crospovidone, mix them evenly, and add the drug-loaded adhesive obtained in step 2) into a soft material;

[0137] 4) Take the soft material obtained in step 3), granulate it with a 24-mesh sieve, vacuum-dry it, and granulate it with a 40-mesh sieve to obtain dry granules loaded with ezetimibe;

[0138] 5) Take the drug-loaded dry granules obtained in step 4), add a glidan...

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Abstract

The invention relates to an ezetimibe oral solid pharmaceutical composition, an inventor finds that an ezetimibe raw material medicine is poor in water solubility and relatively low in bioavailabilityin the research process of an ezetimibe preparation, and meanwhile, after an existing preparation is stored for a long time, an azacyclobutanone structure can be hydrolyzed to generate an open-loop impurity A; the inventor applies a surfactant solubilizing technology to the ezetimibe preparation. Bulk drug, the surfactant and the hydrophilic polymer are jointly dissolved in the solvent; when theezetimibe oral solid preparation is used for preparing a soft material, the raw material medicine and the surfactant are separated out, tightly combined and dispersed in the hydrophilic polymer at thesame time, the solubility of the medicine in water is effectively improved, and test results prove that the dissolution behavior of the ezetimibe oral solid preparation prepared through the technology is obviously improved, so that the bioavailability of the ezetimibe oral solid preparation is also improved. Meanwhile, the hydrolysis impurity A is inhibited, the stability is improved, and the preparation is simple in process, controllable in quality and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an oral solid pharmaceutical composition of ezetimibe, a preparation method and application thereof. Background technique [0002] With the continuous development of social economy, people's diet level is constantly improving, and the blood lipid level of the people is also increasing thereupon. Many domestic epidemiological studies on blood lipids have confirmed that the incidence rate of hyperlipidemia in China is conservatively estimated at 7% to 8%, while the actual average incidence rate may reach more than 10%. There are more than 100 million people in the country who need to accept Lipid-lowering treatment. With the coming aging society, more people in the country will need to receive blood lipid-lowering treatment. [0003] Cardiovascular and cerebrovascular diseases caused by atherosclerosis are one of the main causes of death in developed countries. The d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/36A61K31/397A61K47/32A61K47/24A61P3/06
Inventor 不公告发明人
Owner 董贵雨
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