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Method for producing pulverized organic compound particle

A technology of organic compounds and manufacturing methods, applied in the direction of active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of inability to manufacture suspended stable microparticles, and inability to obtain small particles , Difficulty removing solvents by finely pulverizing organic compound particles, etc.

Active Publication Date: 2010-01-27
活效制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] In the method of (12) above, since the compound dissolved in the solvent is lyophilized and spray-dried to pulverize, if the solvent is not sublimated by lyophilization, it is difficult to remove the solvent from the obtained finely pulverized organic compound particles. difficult
Therefore, even if this method is applied, it is not possible to produce finely pulverized organic compound particles, except for compounds such as proteins that are physiologically acceptable and can be dissolved in solvents that can be freeze-dried.
In addition, in the case of pulverization by this method, sufficiently small particles cannot be obtained, and fine particles with excellent suspension stability and 0.2 μm membrane permeability cannot be produced.

Method used

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  • Method for producing pulverized organic compound particle
  • Method for producing pulverized organic compound particle
  • Method for producing pulverized organic compound particle

Examples

Experimental program
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Effect test

Embodiment 1

[0183] In a 0.2L kneader (decomposable kneader, manufactured by YOSHIDA SEISAKUSHO CO., LTD), 9.3 g of indomethacin (melting point: 155-162° C.) with an average particle diameter of 3960 nm, pulverized chlorinated After 140.7 g of sodium (average particle diameter: 5 μm) was uniformly mixed, 35.5 g of glycerol was slowly injected, and the contents were kept in a kneaded powder state, and pulverized at 5° C. for 15 hours. Then, pour the content into 1L of 0.1mol / L aqueous acetic acid solution, and use a homogenizer to disperse evenly, then filter and wash with water, and dry the obtained wet filter cake under reduced pressure at 40°C. 8.7 g of indomethacin having an average particle diameter of 120 nm was obtained.

Embodiment 2

[0187] In a 0.2L kneader, 13.6 g of nifedipine (melting point: 172-175° C.) with an average particle diameter of 4310 nm and 136.4 g of pulverized sodium chloride (with an average particle diameter of 5 μm) were charged and uniformly mixed, 28 g of glycerol was slowly poured, and the content was kept in a kneaded powder form, and pulverized at 10°C for 8 hours. Then, pour the content into 1L of 0.1mol / L aqueous acetic acid solution, and use a homogenizer to disperse evenly, then filter and wash with water, and dry the obtained wet filter cake under reduced pressure at 50°C. 9.8 g of nifedipine with an average particle diameter of 260 nm was obtained.

Embodiment 3

[0191] In a 0.2L kneader, put 9.0 g of cortisone acetate (melting point: about 240° C.) with an average particle diameter of 1060 nm and 141 g of pulverized sodium chloride (average particle diameter of 5 μm) and mix them uniformly. 38 g of glycerin was poured in, and the content was kept in a kneaded powder form, and pulverized at 10° C. for 18 hours. Then, pour the content into 1L of 0.1mol / L aqueous acetic acid solution, and use a homogenizer to disperse evenly, then filter and wash with water, and dry the obtained wet filter cake under reduced pressure at 50°C. 7.4 g of cortisone acetate with an average particle diameter of 260 nm was obtained.

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Abstract

The invention provides a method for producing pulverized particles of a crystalline organic compound which is poorly water soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poorly water-soluble organic compound particle for medical use, which is characterized in that a poorly water-soluble organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poorly water-soluble organic compound particle for medical use, which is produced by such a production method.

Description

technical field [0001] The present invention relates to a method for producing finely pulverized organic compound particles, and more particularly, to a method for producing poorly water-soluble organic compound particles for medical use and organic compound particles for medical use. [0002] This application claims priority based on Patent Application No. 2007-100902 filed in Japan on April 6, 2007 and Patent Application No. 2007-210370 filed on August 10, 2007, and the contents described in these applications are incorporated herein by reference. In addition, the contents described in the patents, patent applications, and documents cited in this application are incorporated in this specification. Background technique [0003] In general, it is difficult to develop formulations containing poorly water-soluble organic compounds as active ingredients. For example, most oral preparations of poorly water-soluble or insoluble organic compounds have poor absorbability from the ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/015A61K31/192A61K31/216A61K31/404A61K31/41A61K31/4174A61K31/4422A61K31/4704A61K31/56A61K31/57A61K31/573A61K47/04A61K47/10A61K47/12A61K47/34
CPCA61K31/216A61K9/14A61K31/573A61K31/4174A61K9/0019A61K31/192A61K31/41A61K9/0073A61K31/57A61K31/404A61K31/015A61K31/4704A61K31/56A61K31/4422Y10T428/2982A61P1/02A61P1/04A61P1/10A61P1/12A61P1/14A61P11/00A61P11/06A61P11/08A61P11/10A61P11/14A61P13/02A61P19/00A61P19/06A61P19/10A61P21/02A61P25/02A61P25/08A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P27/02A61P27/16A61P29/00A61P3/02A61P31/04A61P31/10A61P31/12A61P35/00A61P3/06A61P37/06A61P37/08A61P43/00A61P5/00A61P5/38A61P7/00A61P7/04A61P9/00A61P9/04A61P9/06A61P9/10A61P9/12A61P3/10A61K47/10A61K9/16
Inventor 广川隆志多田贵广
Owner 活效制药股份有限公司
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