Manufacturing method of organic compound particulate

A technology of organic compounds and manufacturing methods, applied in the direction of mixing methods, chemical instruments and methods, medical preparations of non-active ingredients, etc., can solve the problems of drug pollution, yield reduction, noise generation, etc.

Inactive Publication Date: 2006-12-13
MITSUBISHI CHEM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] However, the micronization method of the drug by the above-mentioned mechanical pulverization has disadvantages such as a decrease in yield, generation of noise, and generation of dust. In addition, there is also a problem of contamination of the drug by a pulverization medium such as a steel ball for impact pulverization.

Method used

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  • Manufacturing method of organic compound particulate
  • Manufacturing method of organic compound particulate
  • Manufacturing method of organic compound particulate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～5

[0077] In the mixing and precipitation step (A), use figure 2 The coaxial mixer with the structure shown in (a) continuously mixes the poor solvent and the organic compound solution to generate a particle suspension. The coaxial mixer is composed of a stainless steel cylindrical tube (7mm inner diameter) that constitutes the main flow path (1), and a stainless steel cylindrical tube (1.6mm outer diameter, inner diameter 0.8mm) that constitutes the introduction flow inside the main flow path (1). (2), and an ultrasonic vibrator (4a) (ultrasonic radiator with a diameter of 20mm ) is inserted into the large-diameter mixing chamber (3) so that it is located 5 mm directly above the overflow port of the introduction flow path (2), so that the poor solvent supplied to the main flow path (1) and the poor solvent supplied to the introduction flow path ( 2) The organic compound solution is contacted and mixed in the mixing chamber (3) under ultrasonic irradiation, thereby generating f...

Embodiment 6

[0089] Indomethacin (water solubility of 1 mg / mL or less) which is a poorly water-soluble organic compound was dissolved in ethanol (purity: 99.5%) as a good solvent to obtain a drug concentration of 10 mg / mL drug solution. Desalted water was used as a poor solvent, and sodium lauryl sulfate as a dispersion stabilizer was dissolved in desalted water (0.625 mg / mL). Using a coaxial mixer with the same double tube structure as in Examples 1 to 5, the poor solvent was supplied to the main flow path (1) at 76mL / min, and the drug solution was supplied to the introduction flow path (2) at 2mL / min. Ultrasonic waves (20kHz, 150W) are irradiated to the contact area of ​​the two liquids to generate a particle suspension at room temperature (about 25°C). Immediately measure the generated particle suspension with a dynamic light scattering particle size distribution meter ("HPP5001" (trade name) manufactured by Malvern Co., Ltd.), and the volume average particle diameter is 0.81 μm. In ad...

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Abstract

The present invention provided the manufacturing method of an organic compound particulate which utilizes a poor solvent depositing method of a continuous system and can quickly and uniformly disperse an organic compound solution in quantities of a poor solvent and which can more easily manufacture the organic compound particulate of <=1 [mu]m volume average grain size. In the manufacturing method of the organic compound particulate, an organic compound solution obtained by dissolving the organic compound in a good solvent which is miscible with the poor solvent and easily dissolves the organic compound is continuously mixed with the poor solvent which hardly dissolves the organic compound to manufacture the organic compound particulate. The organic compound solution is mixed with the poor solvent under ultrasonic irradiation.

Description

technical field [0001] The present invention relates to a method for producing organic compound microparticles, in particular, to an organic method for obtaining submicron particles of organic compounds that are poorly soluble in water with a particle size of 1 μm or less by using a continuous poor solvent precipitation method. Method for producing compound microparticles. Background technique [0002] Organic compounds that are poorly soluble in water, that is, particles of organic compounds with a solubility of less than about 10 mg / mL, are used in a wide range of products such as pharmaceuticals, inks, dyes, lubricants, insecticides, pesticides, fertilizers, and cosmetics. In most cases, the quality of the product can be improved by controlling the particle size. [0003] For example, in pharmaceuticals, in particular, poorly water-soluble drugs are slow to dissolve and elute, and sometimes cannot be sufficiently dissolved and eluting even though they pass through the ab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): B01D9/02B01J19/10A61K31/192A61K47/10A61K9/14B01D9/00B01F3/12B01F5/04B01F11/02B01J19/00
CPCA61K9/145B01D9/0054B01D11/0265A61K31/192B01F3/1242B01F11/0241B01D11/0407B01F11/025B01J19/10B01D9/0081B01F5/0451B01D11/0203B01J2219/089B01F23/551B01F25/3131B01F31/84B01F31/841
Inventor 关宏也浅谷治生
Owner MITSUBISHI CHEM CORP
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