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Supercritical anti-solvent fluidized coating nanoparticle and preparation method thereof

A supercritical anti-solvent and nanoparticle technology, applied in anti-inflammatory agents, anti-toxic agents, pharmaceutical formulations, etc., can solve the problems of low oral bioavailability, poor solubility of breviscapine and short half-life, etc., to improve bioavailability , The effect of prolonging the onset time and stable product quality

Active Publication Date: 2018-06-15
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Scutellarin, 4’,5,6-trihydroxyflavone-7-O-β-D-gluconoside, molecular formula C 21 h 18 o 12 , the molecular weight is 462.37, because the neutral molecules of scutellarin can form intermolecular hydrogen bonds, so the solubility of scutellarin in water is poor
Currently, the problems of scutellarin preparations on the market are mainly low oral bioavailability, rapid elimination in the body by intravenous injection, and short half-life. According to reports, Beagle dogs randomly take scutellarin, and the absolute oral bioavailability is only (0.40±0.19)%.

Method used

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  • Supercritical anti-solvent fluidized coating nanoparticle and preparation method thereof
  • Supercritical anti-solvent fluidized coating nanoparticle and preparation method thereof
  • Supercritical anti-solvent fluidized coating nanoparticle and preparation method thereof

Examples

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preparation example Construction

[0016] A method for preparing supercritical antisolvent fluidized coating nanoparticles provided by the embodiments of the present invention; comprises the following steps:

[0017] The scutellarin solution is contacted with a supercritical fluid and then reacted with a coating agent to prepare nanoparticles.

[0018] Further, the scutellarin solution is a mixed solution obtained by mixing scutellarin raw materials with a solvent. That is, the scutellaria raw material is dissolved in a solvent to obtain a scutellaria solution, which is convenient for subsequent contact with a supercritical fluid, so that scutellarin is precipitated from the solvent, and scutellarin nanoparticles with a nanometer size are obtained.

[0019] Further, the solvent is an alcohol solvent, preferably a monohydric alcohol, more preferably methanol or ethanol. Methanol or ethanol can not only have a dissolving effect, but also can be mixed with a large amount of supercritical fluid, and then facilitat...

Embodiment 1

[0029] This example provides a method for preparing supercritical anti-solvent fluidized coating nanoparticles, which includes the following steps: dissolving 0.1 g scutellarin in 20 ml MeOH to obtain a scutellarin solution, which is filtered for later use. The scutellaria solution is continuously sprayed from the bottom of the fluidized bed at a flow rate of 1ml / min and pressed into the high-pressure fluidized kettle. The fluidized state also exists in the high-pressure fluidized kettle. The coating agent is 2g of microcrystalline cellulose, the supercritical pressure is 120bar, and the temperature is 40°C. After all the scutellarin solution is pumped into the high-pressure fluidized kettle, turn off the high-pressure liquid phase pump, continue to feed the supercritical fluid to maintain the original pressure of the system, and flush the medicine in the settling kettle to take out the residual organic solvent. Obtain the dry product, finally, close the supercritical fluid i...

Embodiment 2

[0032] This example provides a method for preparing supercritical antisolvent fluidized coating nanoparticles, which is consistent with the operation steps of the method for preparing supercritical antisolvent fluidized coated nanoparticles provided in Example 1. The difference is that this example The operating conditions are changed, the solvent is ethanol, the supercritical operating pressure is 80bar, and the temperature is 60°C. The carbon dioxide flow rate is 30g / min, and the solution flow rate is 0.5ml / min.

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Abstract

The invention relates to the field of pharmaceuticals, and particularly relates to a supercritical anti-solvent fluidized coating nanoparticle and a preparation method of the supercritical anti-solvent fluidized coating nanoparticle. The preparation method of the supercritical anti-solvent fluidized coating nanoparticle comprises the following steps: enabling a breviscapine solution and a supercritical carbon dioxide fluid to contact, and then reacting with a coating agent to prepare the nanoparticle. The coating nanoparticle has the advantages of stable quality, even distribution of particlesize and good stability, can be directly packaged into a capsule, is high in dissolving-out speed, and obviously improves the bioavailability of the medicine.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a supercritical antisolvent fluidized coating nanoparticle and a preparation method thereof. Background technique [0002] Erigeronbreviscapus (Vant.) Hand-Mazz is the dry whole herb of the Compositae plant, also known as Erigeronbreviscapus (Vant.) Hand-Mazz, also known as Erigeronbreviscapus (Vant.) Hand-Mazz. Dehumidification, promoting blood circulation and removing blood stasis, dredging channels and collaterals, reducing inflammation and relieving pain. Breviscapine (breviscapine) is a class of total flavonoids extracted and refined from Breviscapine, mainly composed of scutellarin (also known as scutellarin), containing a small amount of breviscapine (apigenin-7-O-glucuronide ). Scutellarin, 4’,5,6-trihydroxyflavone-7-O-β-D-gluconoside, molecular formula C 21 h 18 o 12 , with a molecular weight of 462.37. Since the neutral molecules of scutellarin can form intermolecular hydro...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/7048A61K47/38A61P29/00A61P39/02A61P15/00
CPCA61K9/5078A61K9/5089A61K31/7048A61K47/38
Inventor 李庆国刘莺燕卢铁军刘柳毅叶学经
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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