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Psoralen-quercetin composite solid lipid nanoparticle preparation and preparation thereof

A technology of solid lipid nano and psoralen, which is applied in the direction of drug combination, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve the problem of limiting absorption and bioavailability, psoralen and quercetin Poor water solubility of corticosteroids and other problems, to improve stability and bioavailability, facilitate industrial production, and improve the effect of treatment

Inactive Publication Date: 2014-12-24
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor water solubility of psoralen and quercetin greatly limits their in vivo absorption and bioavailability. Therefore, it is necessary to seek an effective preparation to improve the bioavailability of the drug and enhance its clinical practicability

Method used

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  • Psoralen-quercetin composite solid lipid nanoparticle preparation and preparation thereof
  • Psoralen-quercetin composite solid lipid nanoparticle preparation and preparation thereof
  • Psoralen-quercetin composite solid lipid nanoparticle preparation and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Put 2.0mg of psoralen, 5.0mg of quercetin, 100mg of glyceryl monostearate, 100mg of glyceryl behenate (ATO888) and 150mg of soybean lecithin into a 25ml beaker, accurately measure 5ml of absolute ethanol and pour Put the beaker into the above 25ml beaker, put the beaker into a 78°C water bath and heat it with magnetic stirring to melt the lipid to obtain an oil phase dispersion; accurately weigh 400mg Tween 80, and add Tween 80 to a 25ml beaker containing 20ml water for injection , stir and dissolve (1000r / min) to obtain an aqueous phase solution; put the aqueous solution of Tween 80 into a 78°C water bath to heat, and use a 1ml glass syringe at a stirring speed of 1000r / min to dissolve the oil phase dispersion in 3ml Inject into the water phase solution at a speed of 1 / min, stir and emulsify at 78°C for 1.5h, after emulsification, pour the emulsion into 20ml of ice water (0-4°C) and solidify for 1h to obtain psoralen-quercetin solid lipid The quality nanoparticle collo...

Embodiment 2

[0042] Put 2.5mg of psoralen, 5mg of quercetin, 200mg of stearic acid, and 100mg of synthetic phospholipids into a 25ml beaker, accurately measure 5ml of absolute ethanol and pour it into the above-mentioned 25ml beaker, put the beaker into a 70°C water bath to heat Melt the lipid to obtain an oil phase dispersion; accurately weigh 200mg of poloxamer 188, add poloxamer 188 into a 25ml beaker filled with 20ml of water for injection, stir to dissolve poloxamer 188, and obtain water phase solution; put the aqueous solution of poloxamer 188 in a 70°C water bath and heat it, and inject the oil phase dispersion into the aqueous phase solution at a speed of 2ml / min with a 1ml glass syringe at a stirring speed of 1200r / min, and set the temperature at 70°C Stir and emulsify for 1 hour under the same conditions, after emulsification, pour the emulsion into 20ml (0-4°C) ice water and solidify for 1.5 hours to obtain a psoralen-quercetin solid lipid nanoparticle emulsion, pass through a 0....

Embodiment 3

[0044]Put 1.0mg of psoralen, 3mg of quercetin, 212mg of glyceryl distearate, and 112mg of soybean lecithin into a 25ml beaker, accurately measure 5ml of absolute ethanol and pour it into the above-mentioned 25ml beaker, and put the beaker into 80 Heat in a water bath at ℃ to melt the lipid to obtain an oil phase dispersion; accurately weigh 100mg of Poloxamer 188 and 400mg of Tween 80, add Poloxamer 188 and Tween 80 into a 25ml beaker containing 20ml of water for injection , stir to dissolve Poloxamer 188 and Tween 80 to obtain an aqueous phase solution; put the aqueous solution of Poloxamer 188 and Tween 80 in a water bath at 80°C, and use 1ml of glass at a stirring speed of 1000r / min Inject the oil phase dispersion into the water phase solution with a syringe at a rate of 2ml / min, stir and emulsify at 80°C for 0.5h, after emulsification, pour the emulsion into 20ml (0-4°C) ice water to solidify for 2h to obtain psoralen Psoralen-quercetin solid lipid nanoparticle emulsion is...

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Abstract

The invention belongs to the field of Chinese pharmaceutics, and discloses a psoralen-quercetin composite solid lipid nanoparticle preparation and a preparation method thereof. The preparation comprises psoralen, quercetin, solid lipid, a fat soluble emulsifier, a water soluble emulsifier, an organic solvent, water for injection and ice water, wherein the weight ratio of the five materials is (1-4): (1-5): (60-200): (100-300): (200-800). By means of the prepared preparation, the solubility of psoralen and quercetin is improved, the physical and chemical stability and bioavailability of medicine are improved, the anti-tumor and reverse activity of multidrug resistance of the medicine are enhanced, and meanwhile, the preparation has sustained release, controlled release and targeting functions, and can improve the treatment effect of the medicine remarkably. Besides, the preparation process is simple, industrial production is facilitated, and innovativeness and practicability are achieved.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine preparations, and in particular relates to a psoralen-quercetin composite solid lipid nanoparticle preparation and its preparation. Background technique [0002] Tumor is one of the main killers that threaten human life and health today. Drug treatment can kill tumor cell lesions to a certain extent, but tumor cells are multidrug resistant. Psoralen (PSO) is a natural coumarin compound with various pharmacological activities such as anti-tumor, estrogen-like and multi-drug resistance. Quercetin belongs to flavonoids and is widely found in vegetables, fruits, In herbs, tea and other plants, it has various biological activities such as anti-oxidation, anti-virus, anti-tumor, and reversal of multi-drug resistance. However, the poor water solubility of psoralen and quercetin greatly limits their in vivo absorption and bioavailability. Therefore, it is necessary to find an effective prepara...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/37A61P35/00A61K31/352
Inventor 蔡宇邵长丽张荣华杨丽宁杰周甜甜黄英红杜楚玲夏喜
Owner JINAN UNIVERSITY
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