Supercritical anti-solvent breviscapine nanoparticle, preparation method of supercritical anti-solvent breviscapine nanoparticle, and breviscapine capsule and tablet

A technology of supercritical anti-solvent and breviscapine, which is applied in the delivery of capsules, anti-inflammatory agents, and pills, can solve the problems of short half-life, low oral bioavailability, and poor solubility of breviscapine, and achieve large free energy , stable product quality, good reproducibility

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 main problem of scutellarin on the market is 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 breviscapine nanoparticle, preparation method of supercritical anti-solvent breviscapine nanoparticle, and breviscapine capsule and tablet
  • Supercritical anti-solvent breviscapine nanoparticle, preparation method of supercritical anti-solvent breviscapine nanoparticle, and breviscapine capsule and tablet
  • Supercritical anti-solvent breviscapine nanoparticle, preparation method of supercritical anti-solvent breviscapine nanoparticle, and breviscapine capsule and tablet

Examples

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preparation example Construction

[0023] A method for preparing supercritical anti-solvent scutellarin nanoparticles provided in an embodiment of the present invention; comprises the following steps:

[0024] The obtained nanoparticles are precipitated after the scutellarin solution is contacted with a supercritical carbon dioxide fluid.

[0025] 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 supercritical carbon dioxide fluid, so that scutellarin is precipitated from the solvent, and scutellarin nanoparticles with nanometer particle size are obtained.

[0026] 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 supercritical carbon dioxide fluid in larg...

Embodiment 1

[0036] This example provides a method for preparing supercritical anti-solvent scutellarin 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, and at the same time, carbon dioxide is pumped into the high-pressure fluidized kettle at a flow rate of 25g / min for inversion. The supercritical pressure is 120 bar and the temperature is 40°C. After all the breviscapine solution is pumped into the high-pressure fluidized kettle, turn off the high-pressure liquid phase pump, continue to feed the supercritical carbon dioxide fluid to maintain the original pressure of the system, and flush the medicine in the settling kettle to take out the residual organic solvent. , to obtain a dry product, and finally, close the sup...

Embodiment 2

[0041] This example provides a method for preparing supercritical anti-solvent scutellarin nanoparticles, which has the same operation steps as the method for preparing supercritical anti-solvent scutellarin nanoparticles provided in Example 1. The difference is that the operation of this example The conditions were changed, the solvent was ethanol, the supercritical operating pressure was 800 bar, and the temperature was 35°C. The carbon dioxide flow rate is 10g / 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 breviscapine nanoparticle, a preparation method of the supercritical anti-solvent breviscapine nanoparticle, a breviscapine capsule and a breviscapine tablet. The preparation method of the supercritical anti-solvent breviscapine nanoparticle comprises the following steps: enabling a breviscapine solution and a supercritical carbon dioxide fluid to contact, and precipitating to obtain the nanoparticle. The nanoparticle has the advantages of small particle size and even distribution ofparticles, the dissolving-out speed of the medicine is obviously improved, and the bioavailability of the medicine in vivo is improved.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to supercritical antisolvent scutellarin nanoparticles, a preparation method thereof, and scutellarin capsules and tablets. 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 c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K9/14A61K9/48A61K9/20A61P29/00
CPCA61K9/14A61K9/20A61K9/48A61K31/7048
Inventor 李庆国丘振文王春怡刘柳毅张振宇
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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