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Ampelopsin grossedentata total flavonoid solid lipid nanoparticle and preparation method

A technology of solid lipid nanometer and total flavonoids, which is applied in the directions of liquid delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of large particle size and low drug load, etc. The effect of good capacitance and high physical stability

Inactive Publication Date: 2019-04-09
FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has been reported that the long-circulation nanoliposomes, liposomes, microcapsules, self-emulsifying systems, and clathrates of dihydromyricetin, the main component of the total flavonoids of vine tea, have larger particle size and encapsulation efficiency to varying degrees. , The problem of low drug loading needs to be improved

Method used

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  • Ampelopsin grossedentata total flavonoid solid lipid nanoparticle and preparation method
  • Ampelopsin grossedentata total flavonoid solid lipid nanoparticle and preparation method
  • Ampelopsin grossedentata total flavonoid solid lipid nanoparticle and preparation method

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preparation example Construction

[0034] (2) Preparation of mixed reference substances: Accurately weigh a certain amount of dihydromyricetin, myricetin, and myricetin in 10mL volumetric flasks, dissolve in methanol to constant volume, and the concentrations are 505.68 μg / mL, 6.29 μg / mL, and 13.42 μg / mL, respectively. μg / mL, store at 4°C for future use. According to the above-mentioned chromatographic conditions, the sample was injected and analyzed, and the standard curve was drawn by the external standard method.

[0035] (2) Determination of free flavonoids content: Precisely draw 500 μL of solid lipid nanoparticle suspension of total flavonoids of vine tea into an ultrafiltration centrifuge tube, centrifuge at 8000r / min for 10min, take 100μL of the centrifuged liquid, dilute to 1mL with methanol, and follow the above chromatographic Condition determination.

[0036] (3) Determination of the total flavonoid content: Another precise absorption of 500 μL of the solid lipid nanoparticle suspension of the tota...

Embodiment 1

[0049] Weigh 0.6g of poloxamer 188, and take an appropriate amount of ultrapure water to dissolve it by ultrasonic, and heat it to a constant temperature of 75-80°C as the water phase. In addition, 0.06 g of total flavonoid raw materials of vine tea and 0.6 g of glyceryl monostearate were weighed, and a small amount of ethanol was added. Stir and melt with the water phase at the same temperature to form the oil phase. When the two phases are completely dissolved and the temperature is the same, pour the water phase into the oil phase and stir quickly to mix well. After the mixed solution was evaporated until it had no alcohol smell, the probe was ultrasonicated for 5 minutes with an ultrasonic cell pulverizer to obtain a solid lipid nanoparticle suspension of total flavonoids of vine tea. After cooling at room temperature, store in a refrigerator at 4°C.

Embodiment 2

[0051] Weigh 0.8 g of poloxamer 188, and measure an appropriate amount of ultrapure water to dissolve it ultrasonically, and heat it to a constant temperature of 75-80°C as the water phase. In addition, 0.05 g of the total flavonoid raw materials of vine tea and 0.17 g of glyceryl monostearate were weighed, and a small amount of ethanol was added. Stir and melt with the water phase at the same temperature to form the oil phase. When the two phases are completely dissolved and the temperature is the same, pour the water phase into the oil phase and stir quickly to mix well. After the mixed solution was evaporated until it had no alcohol smell, the probe was ultrasonicated for 5 minutes with an ultrasonic cell pulverizer to obtain a solid lipid nanoparticle suspension of total flavonoids of vine tea. After cooling at room temperature, store in a refrigerator at 4°C.

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Abstract

The invention belongs to the field of pharmaceutical preparations and relates to an ampelopsin grossedentata total flavonoid solid lipid nanoparticle and a preparation method. The solid lipid nanoparticle takes solid natural or synthetical lipoid as a carrier and comprises the following raw materials in percentage by weight: 0.3-0.7% of ampelopsin grossedentata total flavonoids, 4-12% of a surfactant and the balance of water, wherein a drug-lipid ratio is 1:3-1:12. The preparation method employs a fusion-ultrasound method or a high-pressure homogenization method. Encapsulation efficiency and drug loading capacity of the ampelopsin grossedentata total flavonoids can be improved by selecting the appropriate solid lipid and an emolsifier and optimizing a raw material proportion; a particle size is reduced; and stability, bioavailability and targeting ability of the nanoparticle are improved. The ampelopsin grossedentata total flavonoid solid lipid nanoparticle with the small particle sizeand the higher encapsulation efficiency is prepared by the simple, convenient and operation controllable fusion-ultrasound method and shows a slow release characteristic; and a novel dosage form is provided for development and clinical application of the ampelopsin grossedentata total flavonoids.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to solid lipid nanoparticles of vine tea total flavonoids and a preparation method thereof. Background technique [0002] Vine tea is the stem and leaf of Ampelopsis grossedentata (Hand.-Mazz.) W.T.Wang. in the family Vitis genus. It is a tea-like plant resource for both medicine and food. A gem of a county Hakka. It has the effects of clearing away heat and detoxification, promoting dampness and reducing swelling, and is mainly used to treat jaundice hepatitis, cold and wind-heat, throat, conjunctival congestion, swelling and pain. Recent studies have shown that vine tea is a natural plant rich in flavonoids, the total flavonoid content is as high as 40%, and it is the king of flavonoids. Among them, dihydromyricetin (also known as Fujian tea) is its characteristic component. Modern pharmacological studies have shown that the total flavonoids of vine tea have good anti-tu...

Claims

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Application Information

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IPC IPC(8): A61K36/87A61K9/10A61K9/19A61K9/51A61K47/14A61K47/12A61K47/10A61P35/00A61P1/16A61P3/10A61P3/06A61P39/06A61P29/00A61P31/04A61P31/10A61P37/02
CPCA61K9/10A61K9/19A61K9/5123A61K9/5146A61K36/87A61K47/10A61K47/12A61K47/14A61P1/16A61P3/06A61P3/10A61P29/00A61P31/04A61P31/10A61P35/00A61P37/02A61P39/06
Inventor 林珠灿杨毛毛罗花彩宋煜沙玫徐伟郭素华
Owner FUJIAN UNIV OF TRADITIONAL CHINESE MEDICINE
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