A 20(R)-ginsenoside Rg3 sustained-release nanosphere combination and its preparation method

A technology of ginsenosides and nano-microspheres, which can be used in drug combinations, microcapsules, and pharmaceutical formulations. It can solve the problems of unstudied slow-release nanoparticles, achieve enhanced tissue and plasma protein affinity, and high encapsulation efficiency. , good physical stability effect

Active Publication Date: 2020-07-28
富力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, dosage forms such as capsules, sustained-release tablets, emulsions, and dripping pills have all appeared in ginsenoside patents, but polylactic-co-glycolic acid (PLGA) is used as a capsule material to coat Rg3 to prepare sustained-release nanoparticles.

Method used

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  • A 20(R)-ginsenoside Rg3 sustained-release nanosphere combination and its preparation method
  • A 20(R)-ginsenoside Rg3 sustained-release nanosphere combination and its preparation method
  • A 20(R)-ginsenoside Rg3 sustained-release nanosphere combination and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] 1. Preparation of polyvinyl alcohol aqueous solution

[0073] Add 1.25g of PVA (polyvinyl alcohol) to 50ml of three-distilled water (water collected after three distillations), heat at 95°C for 2 hours to fully dissolve, filter, and prepare polyvinyl alcohol with a mass-volume concentration of 2.5%. Aqueous solution (50ml), stored at room temperature, for later use;

[0074] 2. Preparation of polylactic acid-glycolic acid copolymer solution (i.e. PLGA oil phase)

[0075] The accurately weighed poly(lactic-co-glycolic acid) copolymer (i.e. PLGA, 0.09g) was dissolved in 2ml of chloroform, stirred evenly, and made into a poly(lactic-co-glycolic acid) solution (i.e. PLGA) with a concentration of 45mg / ml. Oil phase, 2ml) for subsequent use, wherein, the mass percent of lactic acid and glycolic acid in polylactic acid-glycolic acid copolymer is 50:50; Its molecular weight is 6 * 10 3 ;

[0076] 3. Preparation of Rg3-PLGA mixture

[0077] 20(R)-ginsenoside Rg3 (content is ...

Embodiment 2

[0105] 1. Preparation of polyvinyl alcohol aqueous solution

[0106] Add 2.5g of PVA (polyvinyl alcohol) to 50ml of triple-distilled water, heat at 95°C for 2 hours to fully dissolve, filter, and prepare a polyvinyl alcohol aqueous solution (50ml) with a mass volume concentration of 5%, store at room temperature, and set aside;

[0107] 2. Preparation of polylactic acid-glycolic acid copolymer solution (i.e. PLGA oil phase)

[0108] Accurately weighed poly(lactic-co-glycolic acid) (i.e. PLGA, 0.1g) was dissolved in 2ml of chloroform, stirred evenly to make a concentration of 50mg / ml poly(lactic-co-glycolic acid) solution (i.e. PLGA Oil phase, 2ml) for subsequent use, wherein the percentage of lactic acid and glycolic acid in the polylactic acid-glycolic acid copolymer is 60:40, and the molecular weight of the copolymer is 7×10 3 ;

[0109] 3. Preparation of Rg3-PLGA mixture

[0110] 20 (R)-ginsenoside Rg3 (content is 64%, 0.025g) is added to the PLGA oily phase of 2ml, stir...

Embodiment 3

[0126] 1. Preparation of polyvinyl alcohol aqueous solution

[0127] Add 1.5g of PVA (polyvinyl alcohol) to 50ml of triple-distilled water, heat at 95°C for 2 hours to fully dissolve, filter, and prepare a polyvinyl alcohol aqueous solution (50ml) with a mass volume concentration of 3%, store at room temperature, and set aside;

[0128] 2. Preparation of polylactic acid-glycolic acid copolymer solution (i.e. PLGA oil phase)

[0129] Accurately weighed poly(lactic-co-glycolic acid) (i.e. PLGA, 0.12g) was dissolved in 2.5ml of chloroform, stirred evenly, and made into a solution of poly(lactic-co-glycolic acid) with a concentration of 48mg / ml (i.e. PLGA Oil phase, 2.5ml) for subsequent use, wherein the percentage of lactic acid and glycolic acid in the polylactic acid-glycolic acid copolymer is 80:20, and its molecular weight is 8×10 3 ;

[0130] 3. Preparation of Rg3-PLGA mixture

[0131] 20(R)-ginsenoside Rg3 (content is 79%, 0.02g) is added to the PLGA oil phase of 2.5ml, ...

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Abstract

The invention discloses a ginsenoside Rg3 slow release nanometer microsphere composition, and a preparation method and a use thereof. The method is characterized in that a medicine coating matrix is a polylactic acid-glycolic acid copolymer (PLGA), polyvinyl alcohol (PVA) is adopted as an emulsifier, and Rg3-PLGA nanoparticles with good re-dispersibility are prepared through purifying and drying by adopting a solvent volatility technology; and the Rg3-PLGA nanoparticles are dried to form white powder which can be preserved for a long term. The particles have the advantages of smooth and round surfaces, no adhesion among the particles, good dispersiveness and uniform size, and the average particle size of the particles is 97.5 nm. The composition has high endophilicity to the PLGA material, has a high entrapment rate (of 94.3%), and has a good slow release performance, and the slow release period is 4 d or more. The nanoparticles can be used in antitumor therapy in an intravenous injection and local administration mode, and has wide application prospect.

Description

technical field [0001] The invention belongs to the field of biotechnology and pharmacy, and relates to a slow-release medicine wrapping method for ginsenoside Rg3. Rg3 is wrapped with PLGA as a carrier, and Rg3-PLGA slow-release drug with good redispersibility is prepared by using solvent evaporation method, separation, purification and drying. released nanoparticles. The preparation technology obviously improves the water solubility of the drug, makes the drug release slowly, and achieves the purpose of prolonging the half-life of the drug. Background technique [0002] Ginsenosides are the main active ingredients of ginseng. 20(R)-ginsenoside Rg3 (Rg3 for short) is a traditional Chinese medicine monomer extracted from red ginseng in a small amount. It can enhance the immunity and other functions of tumor patients, and is currently used in the clinical adjuvant therapy of tumors. [0003] The low water solubility of Rg3 limits the research and application of Rg3 to some...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/704A61P35/00
CPCA61K9/0002A61K9/5031A61K31/704
Inventor 燕秋付元山刘基巍张绍智王凯乾富力
Owner 富力
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