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Triptolide solid lipid nanoparticle as well as preparation method and application thereof

A technology of solid lipid nanometer and triptolide, which can be used in pharmaceutical formulations, medical preparations with inactive ingredients, inactive ingredients of oil/fat/wax, etc., and can solve the problems of poor reproducibility, accurate particle size and distribution. control and other issues, to achieve the effects of mild conditions, simple and fast preparation methods, and stable processes

Inactive Publication Date: 2012-11-28
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The invention provides a preparation method of triptolide solid lipid nanoparticles, which solves the problem that the existing preparation methods of solid lipid nanoparticles cannot accurately control the particle size and distribution, and has poor reproducibility. Provide APIs with good monodispersity, high encapsulation efficiency and stable process

Method used

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  • Triptolide solid lipid nanoparticle as well as preparation method and application thereof
  • Triptolide solid lipid nanoparticle as well as preparation method and application thereof
  • Triptolide solid lipid nanoparticle as well as preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0040] The preparation method of triptolide solid lipid nanoparticles described in this embodiment comprises the following steps:

[0041] (1) Preparation of pre-emulsion: Dissolve 600 mg of triptolide, 2.0 g of egg yolk lecithin, 3.2 g of glyceryl palmitate, and 0.8 g of glyceryl monolinoleate in 30 mL of dichloromethane as the oil phase, lipids and lipids The mass ratio of the carrier is 1:2, the mass ratio of triptolide and the mixed lipid is 1:10, and the ratio of the mixed lipid to the organic solvent is 1g:5mL;

[0042] Then disperse the oil phase in 60mL water phase, containing 6.0g polyoxyethylene hydrogenated castor oil in the water phase, heating to 60°C, 30,000r / min, high shear for 1min to obtain the oil-in-water type pre-emulsion; oil phase and water The phase volume ratio is 1:2, and the mass ratio of emulsifier to deionized water is 1:10;

[0043] (2) Emulsion preparation: Using rapid membrane emulsification equipment, the oil-in-water pre-emulsion was circulate...

Embodiment 2

[0048] The preparation method of triptolide solid lipid nanoparticles described in this embodiment comprises the following steps:

[0049] (1) Preparation of pre-emulsion: Dissolve 600 mg of triptolide, 2.0 g of egg yolk lecithin, 3.2 g of glyceryl palmitate, and 0.8 g of glyceryl monolinoleate in 30 mL of ethyl acetate as the oil phase, lipids and lipids The mass ratio of the carrier is 1:2, the mass ratio of triptolide and the mixed lipid is 1:10, and the ratio of the mixed lipid to the organic solvent is 1g:5mL;

[0050] Then disperse the oil phase in 60mL water phase, containing 6.0g of polyoxyethylene hydrogenated castor oil in the water phase, heating to 60°C, 30,000r / min, high shear for 5min to obtain the oil-in-water type pre-emulsion; oil phase and water The phase volume ratio is 1:2, and the mass ratio of emulsifier to deionized water is 1:10;

[0051] (2) Emulsion preparation: Using rapid membrane emulsification equipment, the oil-in-water pre-emulsion is circulate...

Embodiment 3

[0056] The preparation method of triptolide solid lipid nanoparticles described in this embodiment comprises the following steps:

[0057] (1) Preparation of pre-emulsion: Dissolve 600 mg of triptolide, 2.0 g of egg yolk lecithin, 3.2 g of glyceryl palmitate, and 0.8 g of glyceryl monolinoleate in 30 mL of dichloromethane as the oil phase, lipids and lipids The mass ratio of the carrier is 1:2, the mass ratio of triptolide and the mixed lipid is 1:10, and the ratio of the mixed lipid to the organic solvent is 1g:5mL;

[0058] Then disperse the oil phase in 60mL water phase, containing 6.0g of polyoxyethylene hydrogenated castor oil in the water phase, heating to 60°C, 10,000r / min, high shear for 5min to obtain the oil-in-water type pre-emulsion; oil phase and water The phase volume ratio is 1:2, and the mass ratio of emulsifier to deionized water is 1:10;

[0059] (2) Emulsion preparation: using fast membrane emulsification equipment, the oil-in-water pre-emulsion is circulat...

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Abstract

The invention discloses a method for preparing triptolide solid lipid nanoparticles by quick membrane emulsification. The method comprises the following steps of: dissolving triptolide and mixed lipid into an organic solvent to serve as an oil phase, and dispersing into deionized water with an emulsifying agent; performing high-speed shearing emulsification at temperature higher than a melting point of the mixed lipid to obtain O / W type pre-emulsion; circulating the pre-emulsion under nitrogen pressure by adopting quick membrane emulsification equipment, and obtaining O / W type emulsion; and removing the organic solvent, and solidifying the lipid particles to obtain a solid lipid nanoparticle dispersion solution, or centrifugally separating the dispersion solution to collect the nanoparticles, or performing spraying drying or freezing drying to obtain the triptolide solid lipid nanoparticles. The triptolide solid lipid nanoparticles are high in monodispersity, high in entrapment efficiency and stable in process.

Description

technical field [0001] The invention belongs to a method for preparing a nanoparticle raw material drug, and in particular relates to a triptolide solid lipid nanoparticle and a preparation method and application thereof. Background technique [0002] Triptolide (Triptolide, TP), also known as triptolide, is a diterpene lactone compound isolated from Tripterygium Wilfordii Hook.f (TWHf) of the Euonymus family. One of the main active ingredients in rattan, the molecular formula is C 20 h 24 o 6 , the molecular weight is 360.4, hardly soluble in water, soluble in organic solvents such as methanol, ethanol, propylene glycol, acetone, dimethyl sulfoxide, etc., and the maximum ultraviolet absorption wavelength is 218nm. Its chemical structure is as figure 1 shown. [0003] Triptolide has a significant immunosuppressive effect and can be used to treat rheumatoid arthritis, chronic nephritis, lupus erythematosus, psoriasis and other skin diseases, and has a strong anti-graft r...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/585A61K47/44A61K47/14A61K47/12A61P19/02A61P19/04A61P29/00A61P13/12A61P37/06
Inventor 杨祥良林伟基徐辉碧易涛刘卫张聪方伟彭帆邵莉
Owner MACAU UNIV OF SCI & TECH
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