Method for preparing irbesartan ultrafine particles by applying supercritical anti-solvent technology

A supercritical anti-solvent, ultra-fine particle technology, used in medical preparations containing active ingredients, pharmaceutical formulations, metabolic diseases, etc., can solve the problems of difficult filtration and drying, large density and flow index, poor flowability, etc.

Active Publication Date: 2016-05-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The "needle-shaped" crystal form A presents a stable state without hygroscopicity, but it is difficult to filter and dry, and has poor fluidity; while the "brick-shaped" crystal form A has a relatively large bulk density and flow index, and is easy to dry and operate

Method used

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  • Method for preparing irbesartan ultrafine particles by applying supercritical anti-solvent technology
  • Method for preparing irbesartan ultrafine particles by applying supercritical anti-solvent technology
  • Method for preparing irbesartan ultrafine particles by applying supercritical anti-solvent technology

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Accurately weigh 240 mg of irbesartan raw material, add it to a mixed solvent of ethanol: dimethyl sulfoxide = 13 mL: 2 mL, dissolve at 25 ° C, and ultrasonicate at 70 Hz for 5 min to ensure that the solute is completely dissolved; set a supercritical antisolvent The crystallization pressure in the equipment system is 13.5MPa, and the crystallization temperature is 48°C; the drug solution is sprayed into the crystallization kettle at a sampling rate of 0.8mL / min through the HPLC pump, and the supercritical CO 2 The inlet and outlet of the control system is 13.5MPa, in which the supercritical CO 2 The flow rate of the sample is controlled between 5.0-6.0L / min; after the injection volume reaches 10mL, stop the injection and maintain the supercritical CO 2 After 80 minutes of the on and off state, stop the CO 2After the pressure in the system dropped to atmospheric pressure, the sample was taken out from the crystallization kettle for testing and analysis; the obtained ir...

Embodiment 2

[0035] Accurately weigh 225 mg of irbesartan raw material, add it to a mixed solvent of dichloromethane: dimethyl sulfoxide = 13.5 mL: 1.5 mL, dissolve at 25 ° C, and ultrasonicate at 70 Hz for 5 min to ensure that the solute is completely dissolved; set The crystallization pressure in the supercritical antisolvent equipment system is 15MPa, and the crystallization temperature is 45°C; the drug solution is sprayed into the crystallization kettle at a sampling rate of 0.8mL / min through the HPLC pump, and the supercritical CO 2 The inlet and outlet of the control system is 15MPa, in which the supercritical CO 2 The flow rate of the sample is controlled between 5.0-6.0L / min; after the injection volume reaches 10mL, stop the injection and maintain the supercritical CO 2 After 70 minutes of on-off and off-state, stop the CO 2 After the pressure in the system dropped to atmospheric pressure, the sample was taken out from the crystallization kettle for testing and analysis; the obta...

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Abstract

The invention discloses a process for preparing irbesartan ultrafine particles by applying a supercritical anti-solvent technology, and belongs to the technical field of medicinal dosage forms and supercritical technologies. The method is characterized in that an irbesartan solution is sprayed into a crystallization kettle through a supercritical fluid anti-solvent equipment system, and brick-shaped and amorphous-state irbesartan ultrafine particles are crystalized and precipitated in the crystallization kettle. According to the process, the shape and particle size of a medicament are controlled by changing parameters such as a solvent type, solution concentration, a solution sample introduction rate, a crystallization pressure and crystallization temperature. The irbesartan ultrafine particles prepared by the process have the advantages small particle sizes and narrow grain size distribution, and the dissolution rate and equilibrium solubility of the medicinal fine particles are improved remarkably.

Description

technical field [0001] What the present invention relates to is the process for preparing irbesartan ultrafine particles, specifically, the present invention relates to the application of supercritical CO 2 The invention discloses a process for preparing irbesartan ultrafine particles by compression anti-solvent precipitation method (PCA), which belongs to the field of pharmaceutical dosage form and supercritical technology. technical background [0002] In recent years, the development of ultrafine drug particles, especially nanoparticles, has become a hot spot in the field of drug delivery systems (DDS). The particle size of drugs for intravenous injection is usually between 0.1-0.3 μm, for inhalation administration is 1-5 μm, and for oral administration is 0.1-100 μm. For the traditional drug micronization technology, including grinding method, spray drying method, anti-solvent method, freeze-drying method, etc., the particle size distribution of the particles obtained i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4184A61P9/12A61P3/10A61P13/12
CPCA61K9/16A61K31/4184
Inventor 王志祥张依王倩刘尚德周进莉宋雅琴王为彦高赵华
Owner CHINA PHARM UNIV
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