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Glycyrrhizin triple composition nano micro particle and its preparing method

A ternary complex and nanoparticle technology, which is applied in the field of nanomaterials, can solve the problems that there is no preparation method for ternary complex nanoparticles, cannot inhibit the replication of hepatitis virus, and the curative effect is yet to be further confirmed, etc., so as to improve oral bioavailability. , Uniform size, strong practicability

Inactive Publication Date: 2005-03-02
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, adverse reactions such as fever, myalgia, even myelosuppression, autoantibody production, and high treatment costs often limit the use of alpha interferon
The efficacy of the new generation of oral active nucleoside drugs, such as lamivudine (Lumivudine) in the treatment of chronic hepatitis B has yet to be further confirmed
Although schisandra, milk thistle, and weeping grass have non-specific transaminase-lowering effects, glutamyl transpeptidase (ALT) tends to rebound after drug withdrawal, and these drugs cannot inhibit the replication of hepatitis virus
[0009] There is no report on the above-mentioned ternary composite nanoparticle and its preparation method at present

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: in 250ml round bottom flask, 25ml (1mg / ml) monoammonium glycyrrhizinate is added in 100ml chitosan (molecular weight is 360000, 1mg / ml) in acetic acid solution, under stirring at room temperature, 5ml ( 4mg / ml) sodium tripolyphosphate solution is added dropwise in the chitosan solution containing monoammonium glycyrrhizinate, after the dropwise addition, continue to stir for 4 hours to obtain monoammonium glycyrrhizinate-chitosan-trimeric Sodium phosphate ternary complex nanoparticles. The particle size is 248nm and the dispersion index is 0.15 as measured by dynamic light scattering; the zeta potential is 39.21±1.39 (mV) as measured by a zeta potential analyzer; the particle is a regular spherical shape as observed by a transmission electron microscope.

Embodiment 2

[0039] Embodiment 2: in 250ml round bottom flask, 60ml (1mg / ml) diammonium glycyrrhizinate is added in 15ml chitosan (molecular weight is 18000, 8mg / ml) acetic acid solution, at room temperature stirring speed, 36ml ( 1 mg / ml) sodium tripolyphosphate solution is added dropwise in the chitosan solution containing diammonium glycyrrhizinate, after the dropwise addition, continue stirring for 1 hour to obtain diammonium glycyrrhizinate-chitosan-tripolyphosphoric acid Sodium ternary complex nanoparticles. The particle size was 145nm and the dispersion index was 0.14 as determined by dynamic light scattering; the zeta potential was 37.93±2.46 (mV) as measured by a zeta potential analyzer; the particle was a regular spherical shape as observed by a transmission electron microscope.

Embodiment 3

[0040] Embodiment 3: in 250ml round bottom flask, 5ml (4mg / ml) monoammonium glycyrrhizinate is added in 100ml chitosan (molecular weight is 24000, 2mg / ml) in acetic acid solution, under stirring at room temperature, 30ml ( 2 mg / ml) sodium tripolyphosphate dilute solution is added dropwise in the chitosan solution containing monoammonium glycyrrhizinate, after the addition is completed, continue stirring for 2 hours to obtain monoammonium glycyrrhizinate-chitosan- Sodium tripolyphosphate ternary complex nanoparticles. The particle size is 110nm and the dispersion index is 0.14 as determined by dynamic light scattering; the zeta potential is 33.60±3.34 (mV) as measured by a zeta potential analyzer. The particles observed by the transmission electron microscope are regular spherical.

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Abstract

The nano ternary composite glycyrrhizin particle of the present invention results in raised orally taken absorption rate and bioavailability of glycyrrhizin. The present invention prepares nano ternary composite glycyrrhizin particle through ion gelifying process of sodium tripolyphosphate, sodium carboxymethyl cellulose as anion polymer and chitosan or quaternized N-(2-hydroxy) propyl-3-trimethyl ammonium chloride, and the mutual action between glycyrrhizin and chitosan. Nano particles of different sizes may be obtained via controlling the molecular weight of chitosan and the concentration and ratio of the components. The nano particle is positively charged and thus favorable to surface modification. The method of the present invention is simple, feasible, repeatable and practical.

Description

technical field [0001] The invention belongs to the technical field of nanomaterials, and in particular relates to a glycyrrhizic acid ternary compound nanoparticle and a preparation method thereof. Background technique [0002] my country is a high-incidence area of ​​viral hepatitis. According to statistics, there are more than 120 million chronic hepatitis B surface antigen carriers in my country, and no less than 12 million chronic persistent and chronic active hepatitis, which seriously threatens the health of the people. Currently, there is no specific treatment for viral hepatitis. In the treatment of chronic hepatitis B and C, interferon-α is the drug with the most in-depth research and definite curative effect in antiviral treatment. However, adverse reactions such as fever, myalgia, even bone marrow suppression, autoantibody production, and high treatment costs often limit the use of alpha interferon. The efficacy of applying a new generation of oral active nucle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/704A61P1/16A61P31/12
Inventor 吴雁郑永丽杨武利府寿宽汪长春胡建华
Owner FUDAN UNIV
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