Ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere and preparation method thereof

A technology of polylactic acid glycolic acid and ginsenoside, which is applied in the field of medicine, can solve the problems of low blood drug concentration, limited clinical drug efficacy, and reduced drug utilization rate, and achieve the effects of reducing side effects, good therapeutic effect, and reducing the number of medications

Inactive Publication Date: 2015-01-21
BEIJING JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, 20(R)-ginsenoside Rg3 is not easily soluble in water. Through pharmacokinetic studies on ginsenoside Rg3, it has been found that after oral administration, Rg3 absorbs quickly, metabolizes quickly, and has low blood drug concentration, which reduces its drug utilization. Greatly limit its clinical efficacy, but also limit the application of its parenteral route of administration

Method used

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  • Ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere and preparation method thereof
  • Ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere and preparation method thereof
  • Ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere and preparation method thereof

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preparation example Construction

[0030] like figure 1 As shown, the preparation method of ginsenoside Rg3 polylactic-glycolic acid nano-microspheres according to an embodiment of the present invention comprises the following steps:

[0031] S1: Dissolve ginsenoside Rg3 in dimethyl sulfoxide (DMSO) to obtain the first solution of the first predetermined concentration, and dissolve polylactic acid-glycolic acid copolymer in dichloromethane (DCM) to obtain the second predetermined concentration. concentration of the second solution.

[0032] S2: adding a predetermined ratio of the first solution to the second solution, and ultrasonicating to form a suspension.

[0033] S3: Add the suspension into an aqueous solution containing polyvinyl alcohol (PVA), and perform ultrasonic emulsification to obtain an emulsion.

[0034] S4: drying the emulsion, and after the microspheres of the emulsion are solidified, centrifuge, wash, and freeze-dry to obtain ginsenoside Rg3 polylactic-glycolic acid nanospheres.

[0035] Ac...

Embodiment 1

[0044] Example 1: Firstly, ginsenoside Rg3 was dissolved in DMSO with a drug concentration of 40 mg / ml, and PLGA was dissolved in DCM with a concentration of 30 mg / ml. Precisely measure 1ml of PLGA solution, add 80μl of ginsenoside Rg3 solution to it, ultrasonic power 210w, supersonic for 5 seconds, pause for 5 seconds, and ultrasonic for 1 minute.

[0045] The suspension was quickly added to 10 ml of aqueous solution containing 1% PVA, and the aforementioned ultrasonic conditions were repeated, and the resulting emulsion was poured into 30 ml of aqueous solution containing 1% PVA, and after 3 hours of magnetic stirring at 1000 r, the microspheres were separated by high-speed freezing and centrifugation. Washed three times with deionized water, freeze-dried and stored at -20°C. Microsphere scanning electron microscope photo as figure 2 As shown in A.

Embodiment 2

[0046] Example 2: Firstly, ginsenoside Rg3 was dissolved in DMSO with a drug concentration of 40 mg / ml, and PLGA was dissolved in DCM with a concentration of 30 mg / ml. Precisely measure 1ml of PLGA solution, add 60μl of ginsenoside Rg3 solution to it, ultrasonic power 210w, supersonic for 5 seconds, stop for 5 seconds, and ultrasonic for 1 minute.

[0047] The suspension was quickly added to 10 ml of aqueous solution containing 1% PVA, and the aforementioned ultrasonic conditions were repeated, and the resulting emulsion was poured into 30 ml of aqueous solution containing 1% PVA, and after 3 hours of magnetic stirring at 1000 r, the microspheres were separated by high-speed freezing and centrifugation. Washed three times with deionized water, freeze-dried and stored at -20°C. Microsphere scanning electron microscope photo as figure 2 Shown in B.

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Abstract

The invention discloses a ginsenoside Rg3 poly(lactic-co-glycolic acid) (PLGA) nano microsphere and a preparation method thereof. The preparation method of the ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere comprises the following steps: S1, dissolving ginsenoside Rg3 in dimethyl sulfoxide to obtain a first liquid with a first predetermined concentration, and dissolving poly(lactic-co-glycolic acid) copolymer into dichloromethane to obtain a second liquid with a second predetermined concentration; S2, adding the first liquid in a predetermined proportion into the second liquid to perform ultrasonic treatment to form a turbid liquid; S3, adding the turbid liquid into an aqueous liquid containing polyvinyl alcohol to perform ultrasonic emulsion to obtain emulsion; and S4, drying the emulsion, centrifugally separating and washing, and freeze-drying the emulsion after curing the microspheres of the microsphere of the emulsion to obtain the ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere. According to the preparation method of the ginsenoside Rg3 poly(lactic-co-glycolic acid) nano microsphere of the embodiment of the invention, the prepared ginsenoside PLGA microsphere is good in pesticide effect.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically, relates to a ginsenoside Rg3 polylactic-glycolic acid nano-microsphere and a preparation method thereof. Background technique [0002] Ginsenoside Rg3 is a tetracyclic triterpenoid saponin compound present in ginseng, with a molecular weight of 784.13 and two optical isomer forms of 20(R)-ginsenoside Rg3 and 20(s)-ginsenoside Rg3, of which 20(R)-ginsenoside Rg3 is chemically stable, and its structural formula is as follows: [0003] [0004] Ginsenoside Rg3 has multiple pharmacological effects, which can significantly improve the immune function of tumor-bearing mice; inhibit the formation of new blood vessels in tumors; prevent the implantation of exfoliated cancer cells in the vessel wall; inhibit the infiltration of tumor cells into the basement membrane of the vessel wall, It has significant anti-infiltration and anti-transfer effects. Clinical experiments have co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/704A61K47/34A61P37/04A61P35/00
Inventor 孙维敏金玺园
Owner BEIJING JIAOTONG UNIV
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