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Method of preparing formononetin ultrafine particles by supercritical antisolvent crystallization

A supercritical anti-solvent and formononetin technology, which is applied in the direction of anti-toxic agents, anti-inflammatory agents, and medical preparations containing active ingredients, can solve problems such as formononetin ultrafine particles that have not yet been seen, and achieve the improvement of biological Effects of utilization, enhanced adsorption, and increased specific surface area

Active Publication Date: 2019-09-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no report on the preparation of superfine formononetin particles by supercritical anti-solvent crystallization technology

Method used

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  • Method of preparing formononetin ultrafine particles by supercritical antisolvent crystallization
  • Method of preparing formononetin ultrafine particles by supercritical antisolvent crystallization
  • Method of preparing formononetin ultrafine particles by supercritical antisolvent crystallization

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: single factor experiment

[0043] Single factor experiment: the effect of injection flow rate on the particle size of formononetin

[0044] At crystallization temperature 42°C, crystallization pressure 10MPa, CO 2 Under the condition that the flow rate is 4~4.5L / min and the mass concentration of formononetin is 5mg / mL, the effect of the injection flow rate of 1.0, 1.4, 1.8, 2.2, 2.6mL / min on the volume average of formononetin particles was investigated. Influenced by the particle size, the volume average particle sizes were 9.185, 7.860, 6.146, 6.910, and 7.785 μm, so the injection flow rate of the optimal group was determined to be 1.8 mL / min.

[0045] Single Factor Experiment: Effect of Crystallization Pressure on Formononetin Particle Size

[0046] At a crystallization temperature of 42°C, an injection flow rate of 1.8mL / min, CO 2 Under the conditions of flow rate of 4-4.5L / min and formononetin mass concentration of 5mg / mL, the effects of crystalliza...

Embodiment 2

[0051] Example 2: Application of supercritical anti-solvent crystallization technology to prepare formononetin ultrafine particles under optimal process parameters

[0052] The method for preparing formononetin ultrafine particles by using supercritical anti-solvent crystallization technology comprises the following steps:

[0053] Step S1, dissolving the formononetin raw material drug in a mixed organic solvent to obtain a formononetin solution;

[0054] Step S2, adjust the temperature in the crystallization kettle to be constant, and CO 2 Pass into the crystallization kettle at a certain flow rate, and adjust the pressure of the crystallization kettle to be constant;

[0055] Step S3, continue to feed CO 2 , keep the temperature and pressure in the crystallization kettle constant, and at the same time, spray the above-mentioned formononetin solution into the kettle through the high-pressure infusion pump through the nozzle on the top of the crystallization kettle;

[0056...

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Abstract

The invention discloses a method of preparing formononetin ultrafine particles by supercritical antisolvent crystallization. The method comprises the steps of (1) preparing formononetin solution; (2)adjusting interior temperature of a crystallizer to a constant value, introducing CO2 into the crystallizer at a certain speed, and adjusting pressure of the crystallizer to a constant level; (3) spraying the prepared formononetin solution into the crystallizer through a top nozzle of the crystallizer via an efficient infusion pump; and (4) after sample injection, continuing to introduce CO2 intothe crystallizer, relieving the pressure over a certain time, opening the crystallizer, and collecting the formononetin ultrafine particles. The formononetin ultrafine particles with small particle size and narrow particle size distribution are prepared successfully by supercritical antisolvent crystallization; drug dissolution rate is increased; the specific surface area of the particles herein is enlarged; the drug, the particles, can adsorb better to the gastrointestinal mucosa and has higher bioavailability; operating conditions are mild, the method is green, good in safety and high in efficiency, and no residue of organic solvents occurs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical engineering, and in particular relates to a method for preparing formononetin ultrafine particles by applying supercritical antisolvent crystallization technology. Background technique [0002] Formononetin (Formononetin), also known as formononetin, formononetin, molecular formula C 16 h 12 o 4 , the chemical name is 7-hydroxy-3-(4-methoxyphenyl)-4H-1-benzopyran-4-one, which is widely found in plants such as astragalus, licorice, milletus, and red clover , is a naturally occurring isoflavone and phytoestrogen. Studies have shown that formononetin has a variety of pharmacological effects, such as anti-inflammation, anti-tumor, anti-oxidation, anti-arrhythmia, anti-atherosclerosis, etc. However, formononetin is almost insoluble in water, hard to dissolve, and has low bioavailability, which greatly limits the clinical application of formononetin. [0003] Theoretically, the goal of improving drug ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/352A61P29/00A61P35/00A61P39/06A61P9/06A61P9/10
CPCA61K9/1682A61K31/352A61P9/06A61P9/10A61P29/00A61P35/00A61P39/06
Inventor 王志祥占晶晶陶钰婷王聪聪朱蜜蜜杨倩陈昕航陈震
Owner CHINA PHARM UNIV
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