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Method for preparing myricetin/HP-beta-CD inclusion compound superfine granules through supercritical CO2 anti-solvent technique

An ultra-fine particle, anti-solvent technology, used in anti-toxic agents, anti-inflammatory agents, drug combinations, etc., to achieve green and efficient processes, reduce raw material losses, and overcome the effects of organic solvent residues

Inactive Publication Date: 2019-05-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no report on the preparation of myricetin / HP-β-CD inclusion compound ultrafine particles by supercritical antisolvent method

Method used

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  • Method for preparing myricetin/HP-beta-CD inclusion compound superfine granules through supercritical CO2 anti-solvent technique
  • Method for preparing myricetin/HP-beta-CD inclusion compound superfine granules through supercritical CO2 anti-solvent technique
  • Method for preparing myricetin/HP-beta-CD inclusion compound superfine granules through supercritical CO2 anti-solvent technique

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Single factor method to investigate the influence of various factors on the drug loading and recovery rate of myricetin / HP-β-CD inclusion complex ultrafine particles

[0041] Single factor experiment: CO 2 Effect of Flow Rate on the Recovery Rate and Morphology of Myricetin / HP-β-CD Inclusion Complex Ultrafine Particles

[0042] Under the conditions of crystallization pressure of 11MPa, crystallization temperature of 40°C, mass concentration of myricetin of 6.0g / L, molar ratio of myricetin raw material drug to HP-β-CD of 1:1, and solution volume flow rate of 1.0mL / min, the CO 2The effect on the morphology and recovery of myricetin inclusion compound when the flow rate is 2.0-2.5, 2.5-3.0, 3.0-3.5, 3.5-4.0, 4.0-4.5L / min respectively. Among them, when the flow rate is ≤2.5L / min, the product is similar to the rotary evaporation product under the same conditions, and it is a yellow transparent sticky solid attached to the bottom of the crystallization kettle; whe...

Embodiment 2

[0051] Example 2: Application of supercritical antisolvent method to prepare myricetin / HP-β-CD inclusion complex ultrafine particles

[0052] The method for preparing myricetin / HP-β-CD clathrate ultrafine particles by supercritical antisolvent method comprises the following steps:

[0053] Step S1, dissolving the myricetin raw material drug and the water-soluble carrier in an organic solvent to obtain a myricetin-carrier mixed solution;

[0054] Step S2, the CO 2 Pass into the crystallization kettle, adjust the temperature and pressure in the crystallization kettle;

[0055] Step S3, continue to feed CO 2 , maintaining the temperature and pressure in the crystallization kettle constant, while passing the myricetin-carrier mixed solution prepared in step S1 into the crystallization kettle;

[0056] Step S4, after the mixed solution is passed through, continue to pass through CO 2 40min, after exhausting the residual solvent, release the pressure; when the pressure in the cr...

Embodiment 3

[0066] Embodiment 3: In vitro dissolution test

[0067] Take a certain amount of myricetin raw material drug, myricetin / HP-β-CD solid mixture and myricetin / HP-β-CD inclusion compound ultrafine particles under the optimal process respectively, and measure their concentration in 0.1% Tween 80 The dissolution rate of the solution bell, compare its dissolution performance, the results are as follows Figure 9 As shown, the analysis shows that the dissolution rate of myricetin / HP-β-CD inclusion compound ultrafine particles can reach 85.69% in 5 minutes, and can reach more than 99% in 60 minutes, which proves that the dissolution of the drug has been significantly improved.

[0068] The in vitro dissolution results show that, compared with the raw material drug and solid mixture, the dissolution performance of myricetin / HP-β-CD inclusion complex ultrafine particles has been significantly improved, specifically, myricetin / HP-β-CD inclusion complex The cumulative dissolution rate of ...

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Abstract

The invention discloses a method for preparing myricetin / HP-beta-CD inclusion compound superfine granules through a supercritical CO2 anti-solvent technique. The method comprises the following steps of (1) compounding a myricetin-carrier mixed solution: weighing myricetin raw material medicines and a water-soluble carrier namely hydroxypropyl-beta-cyclodextrin, and enabling the weighed myricetin raw material medicines and the weighed water-soluble carrier namely hydroxypropyl-beta-cyclodextrin to dissolve in an organic solvent to obtain the myricetin-carrier mixed solution, wherein the organicsolvent is ethanol, and the molar ratio of the raw material medicines to the carrier is 1 to 1; (2) charging CO2 into a crystallization kettle at a certain flow rate, and regulating temperature and pressure in the crystallization kettle; (3) continuing charging the CO2, maintaining the temperature and the pressure in the crystallization kettle unchanged, and at the same time, spraying the myricetin-carrier mixed solution prepared in the step (1) into the crystallization kettle from the top of the crystallization kettle through a nozzle by a high-pressure liquid delivery pump; and (4) after completion of sample introduction, continuing charging the CO2 for some time, completely discharging remaining solvents, releasing pressure, opening the crystallization kettle, and collecting products.The myricetin / HP-beta-CD inclusion compound superfine granules obtained by the method can notably improve dissolving-out properties, and improvement of the biological availability of the myricetin isfacilitated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical engineering and relates to a supercritical CO 2 A method for preparing myricetin / HP-β-CD inclusion complex ultrafine particles by anti-solvent technology. Background technique [0002] Myricetin, also known as myricetin, is a polyhydroxy flavonoid widely present in plants of the genus Snakevine. Studies have shown that myricetin has a variety of pharmacological activities: antagonism of platelet activating factor, hypoglycemic effect, antioxidant effect, liver protection and liver protection, solution to light alcohol poisoning, anti-inflammatory and anti-tumor, elimination of free radicals in the body, etc. Today, myricetin has been widely used in the industries of medicine, food, health care products and cosmetics. The combination of myricetin and some drugs has become a research topic of many scholars. Some European countries have produced myricetin as a health food. However, studies have shown ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/352A61P7/02A61P3/10A61P39/06A61P1/16A61P39/02A61P29/00A61P35/00B01D9/02
Inventor 王志祥王聪聪陈昕航朱蜜蜜杨倩陈震
Owner CHINA PHARM UNIV
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