Method for improving dissolution rate of ezetimibe tablet

A technology of ezetimibe and dissolution rate, which is applied in pill delivery, metabolic diseases, drug combination, etc., can solve problems such as difficult process requirements, unsuitable for industrial production, high price, etc., and achieves high safety, easy process scale-up, The effect of request reduction

Inactive Publication Date: 2017-11-28
CHONGQING HUAPONT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method requires the use of supercritical equipment, which is expensive and operated at high pressure, and is not suitable for industrial production
[0012] The current production process is difficult to achieve low process requirements, and the dissolution behavior of the prepared ezetimibe tablets is consistent with that of Yishichun and has high safety standards

Method used

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  • Method for improving dissolution rate of ezetimibe tablet
  • Method for improving dissolution rate of ezetimibe tablet
  • Method for improving dissolution rate of ezetimibe tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] 1. Preparation prescription:

[0060] The bulk drug obtained by common jet milling.

[0061] serial number

Element

mg / tablet

1

Ezetimibe

10.0

2

lactose monohydrate

55.0

3

Sodium dodecyl sulfate

2.00

4

Povidone K30

4.00

5

Croscarmellose Sodium

8.00

6

microcrystalline cellulose

20.0

7

Magnesium stearate

1.00

total

100

[0062] 2. Preparation process

[0063] The bulk drug obtained by common jet milling. In wet granulation, ingredients 1, 2, 3, 4 and part No. 5 are mixed, purified water and ethanol are prepared into a 50% ethanol solution as a wetting agent, and the weight ratio of the wetting agent to ezetimibe is 0.7:1, that is 7mg. The wetting agent is sprayed into the mixture and granulated and dried. The dry granules are sieved and mixed with the remaining ingredients No. 5 and No. 6. Add ingredient No. 7 and mix. The mixture is compressed...

Embodiment 2

[0065] 1. Preparation prescription: same as Example 1.

[0066] The bulk drug obtained by common jet milling.

[0067] 2. Preparation process:

[0068] The bulk drug obtained by common jet milling. Mix No. 1, 2, 3 and part No. 5 components in a fluidized bed, mix No. 4 component with 50% ethanol solution to prepare an adhesive, and the weight of ethanol aqueous solution is 10 times that of No. 4 component, ie 40mg. The binder is sprayed into the mixture and granulated and dried. The dry granules are sieved and mixed with the remaining ingredients No. 5 and No. 6. Add ingredient No. 7 and mix. The mixture is compressed to the appropriate size and weight on a suitable tablet machine.

Embodiment 3

[0070] 1. Preparation prescription:

[0071] The bulk drug obtained by common jet milling.

[0072] serial number

Element

mg / tablet

1

Ezetimibe

10.0

2

lactose monohydrate

40.0

3

Sodium dodecyl sulfate

1.00

4

Povidone K30

8.00

5

Croscarmellose Sodium

15.00

6

microcrystalline cellulose

25.0

7

Magnesium stearate

1.00

total

100

[0073] 2. Preparation process:

[0074] The bulk drug obtained by common jet milling. Mix No. 1, 2, 3 and part No. 5 components in a fluidized bed, mix No. 4 component with 50% ethanol solution to prepare an adhesive, and the weight of the ethanol aqueous solution is 10 times that of No. 4 component, ie 80mg. The binder is sprayed into the mixture and granulated and dried. The dry granules are sieved and mixed with the remaining ingredients No. 5 and No. 6. Add ingredient No. 7 and mix. The mixture is compressed to the appropri...

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PUM

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Abstract

Belonging to the field of pharmaceutical preparations, the invention in particular relates to a method for improving the dissolution rate of an ezetimibe tablet. The method uses ordinary air jet comminution to acquire bulk drugs, and employs ethanol of appropriate concentration to replace purified water for granulation, thus obtaining a product with a dissolution behavior consistent with ezetimibe tablet. The preparation technology has lowered requirement for bulk drugs, can acquire bulk drugs meeting the preparation requirements only by means of ordinary air jet comminution, is easy for process scale-up, and guarantees smooth preparation production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a method for improving the dissolution rate of ezetimibe tablets. Background technique [0002] The chemical name of ezetimibe: 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-( 4-hydroxyphenyl)-2-azetidin(azetidin)one, has the following chemical structure: [0003] [0004] Its molecular formula is: C24H21F2NO, molecular weight: 409.4. [0005] 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-dens...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/397A61K47/10A61P3/06
CPCA61K9/2013A61K31/397
Inventor 胡渝慧陈博程刚
Owner CHONGQING HUAPONT PHARMA
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