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Breviscapine nano particles and preparation method thereof

A technology of breviscapine and nanoparticles, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of short half-life, low oral bioavailability, and poor solubility of scutellarin and other problems, to achieve the effect of improving dissolution rate, stable product quality and good reproducibility

Active Publication Date: 2018-06-19
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Abstract
  • Description
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AI Technical Summary

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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  • Breviscapine nano particles and preparation method thereof
  • Breviscapine nano particles and preparation method thereof
  • Breviscapine nano particles and preparation method thereof

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preparation example Construction

[0028] The embodiment of the present invention also provides a preparation method of scutellarin nanoparticles, comprising the following steps:

[0029] Mix breviscapine and stabilizer according to the corresponding ratio to obtain a suspension, then pour the suspension into a media grinder, and then add grinding media for grinding.

[0030] The grinding media is a zirconium compound, preferably zirconium oxide. Zirconia has high hardness and strong wear resistance. It is suitable for ultra-fine grinding and dispersion of "zero pollution" and high-viscosity samples. The suspension is a sample with high viscosity. Zirconia can be used for samples. Grind finely.

[0031] Further, the particle size of the grinding medium is 0.4-0.6 mm. The smaller the diameter of the grinding beads, the larger the surface area, the more points of contact with the drug, and the greater the frequency of collisions between the drug and the grinding beads, but the grinding beads with small diameter...

Embodiment 1

[0040] This embodiment provides a scutellarin nanoparticle, which is mainly made of scutellarin and a stabilizer, and the mass of scutellarin accounts for 25% of the total suspension of scutellarin and the stabilizer; wherein, The stabilizer is Tween 80; the mass of the stabilizer accounts for 15% of the mass of breviscapine.

[0041] This embodiment also provides a preparation method of scutellarin nanoparticles, comprising the following steps:

[0042] Weigh 7.5g of breviscapine medicine, place it in 22.5ml of aqueous solution containing 1.125g of Tween 80, stir and suspend to obtain a suspension. Then pour the suspension into the grinding chamber of the media mill, add 450g of zirconia beads with a diameter of 0.6mm, install the machine, turn on the circulating cooling water, and run at a speed of 1400r / min for 1h. Finally, freeze-dry, take the suspension and divide it into 25ml vials, place it at -40°C for 5 hours, and heat it up to -20°C in the first step of the sublimat...

Embodiment 2

[0044] This embodiment provides a scutellarin nanoparticle, which is mainly made of scutellarin and a stabilizer, and the mass of scutellarin accounts for 22% of the total suspension of scutellarin and the stabilizer; wherein, The stabilizer is sodium lauryl sulfate; the mass of the stabilizer accounts for 18% of the mass of breviscapine.

[0045] This embodiment also provides a preparation method of scutellarin nanoparticles, comprising the following steps:

[0046] Weigh 7g of scutellarin, place it in 31.9ml of aqueous solution containing 1.26g of sodium lauryl sulfate, stir and suspend to obtain a suspension. Then pour the suspension into the grinding chamber of the media mill, add 445g of zirconia beads with a diameter of 0.4mm, install the machine, turn on the circulating cooling water, and run at a speed of 1300r / min for 1.5h. Finally, freeze-dry, take the suspension and divide it into 25ml vials, place it at -50°C for 5.5 hours, and heat it up to -17°C in the first ste...

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Abstract

The invention relates to the field of pharmacy, and concretely relates to breviscapine nano particles and a preparation method thereof. The breviscapine nano particles are mainly prepared by breviscapine and a stabilizing agent, and mass of breviscapine accounts for 22-27% of a total amount of a suspension of breviscapine and the stabilizing agent. The nano particles have the advantages of small particle size and stable mass, can obviously increase the dissolution speed, and prolong the effect time of a drug in body.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a scutellarin 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 hydrogen bonds, the solubility of scu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/7048A61K47/26
CPCA61K9/19A61K31/7048A61K47/26
Inventor 李庆国刘柳毅高巍叶学经罗海燕
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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