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Isomorellic acid polylactic acid nano particle preparation and preparing method thereof

A technology of gambogic acid polylactic acid and gambogic acid, which is applied in the field of medicine, can solve problems such as poor stability and easy degradation, and achieve the effects of increasing stability, improving bioavailability, and good solubilization

Inactive Publication Date: 2008-07-30
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, gambogic acid injections have poor stability and are prone to degradation. Therefore, finding new carrier materials, improving the solubility and stability of gambogic acid and improving the effect of drugs are the primary problems to be solved for the improvement of gambogic acid dosage forms

Method used

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  • Isomorellic acid polylactic acid nano particle preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 1) Weigh 20 mg of gambogic acid and 75 mg of polylactic acid, dissolve them in 20 mL of acetonitrile, and make an organic phase;

[0050] 2) Weigh a certain amount of Poloxamer F-68 0.2g and dissolve it in 20mL water to make the water phase;

[0051] 3) Add the organic phase to the water phase drop by drop, and magnetically stir for 4 hours; distill under reduced pressure to remove the organic solvent and a part of the water; filter with a 0.22 μm microporous membrane to obtain milky yellow gambogic acid polylactic acid nanoparticle solution . The measured average particle diameter was 52.6 nm.

Embodiment 2

[0053] 1) Accurately weigh 20 mg of gambogic acid and 50 mg of polylactic acid, and dissolve them in 20 mL of acetone.

[0054] 2) Weigh 0.4g of Poloxamer F-68 and dissolve it in 40mL of water.

[0055] 3) The method is the same as in Example 1.3) to obtain milky yellow gambogic acid polylactic acid nanoparticles. The average particle diameter was measured to be 51.2 nm. Ultra-fast refrigerated centrifugation (4°C, 50 000r·min-1) for 1.5h. Gambogic acid polylactic acid nanoparticle powder was obtained.

Embodiment 3

[0057] 1) Accurately weigh 20 mg of gambogic acid and 75 mg of polylactic acid, and dissolve them in 20 mL of acetone.

[0058] 2) Weigh 0.2 g of poloxamer F-68 and dissolve it in 40 mL of aqueous ethanol (ethanol: water = 1:1).

[0059] 3) The method is the same as in Example 1.3) to obtain milky yellow gambogic acid polylactic acid nanoparticles. The average particle diameter was measured to be 50.6 nm.

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Abstract

The invention discloses a gamboges acid nanometer particle preparation and is prepared by the components of raw material gamboges acid 0.05 to 1.5 percent, polylactic acid 0.05 to 1.5 percent, surfactant 0.1 to 1.5 percent, organic solvent 33 to 50 percent and the allowance of water with the following steps: dissolving the polylactic acid into the organic solvent and dispersing the gamboges acid in the mixed solution of the polylactic acid and the organic solvent; the preparation is obtained by adding the mixed solution with the gamboges acid into water phase with the surfactant, stirring magnetically for 4 hours, vacuum distillation and filtering with a 0.22Mum micro-porous filtering film after the organic solvent and part of water are distillated. The drug with a clear system, the particle size between 10 to 100nm and good dispersion and stability can significantly solubilize drugs, has a targeting effect for reticuloendothelial cells and concentrate at lesion sites, thus improving the curing effect of the drug and reduces the side effect of the drug. Additionally, the drug has a slowly releasing effect, can maintain constant plasma concentration or pharmacologic effect for a long time and improve drug bioavailability.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of gambogic acid extracted from traditional Chinese medicine with antitumor effect, in particular to a nanoscale preparation of gambogic acid and a preparation method thereof. Background technique [0002] Gambogic acid (Gambogic acid, GA) is a dry resin secreted by Garcinia cambogia. Mainly produced in India, Cambodia, Thailand and Vietnam. The solubility in water is poor, but it is easily soluble in organic solvents such as ethanol, methanol, acetone, ethyl acetate, and acetonitrile. [0003] Gambogic acid has the functions of detumescence, detoxification, hemostasis, insecticide, etc. Its main pharmacological effects are: ①Anti-tumor effect, gamboge has effect on ECA, ARS, S 180 , S 37 , MA 737 , U 4 ,ARA 4 , W 256 The inhibition rate is 35% to 38%, and it has different degrees of inhibition or killing effects on the human cancer cell lin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/352A61K47/34A61P35/00
Inventor 欧阳五庆李树珍
Owner NORTHWEST A & F UNIV
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