Daidzein solid lipid nanoparticles and preparation method thereof

A technology of solid lipid nanometer and daidzein, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as poor solubility of daidzein, and achieve oral bioavailability. The effect of increasing the degree of metabolism, reducing the metabolism, and increasing the adhesion ability

Inactive Publication Date: 2013-05-22
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

During the preparation process, the drug needs to be dissolved in a suitable pharmaceutically acceptable organic solvent, but the solubility of daidzein in these solvents is very poor, and it is difficult to directly prepare it into solid lipid nanoparticles

Method used

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  • Daidzein solid lipid nanoparticles and preparation method thereof
  • Daidzein solid lipid nanoparticles and preparation method thereof
  • Daidzein solid lipid nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] composition:

[0070] Daidzein 100mg

[0071] Soy Lecithin 1.0g

[0072] Sodium Oleate 1.0g

[0073] Glyceryl Behenate 0.2g

[0074] Preparation method: It is prepared by thin film ultrasonic dispersion method, and the specific preparation operation is as follows:

[0075] Take 100 mg of daidzein and 0.5 g of soybean lecithin, add 100 mL of methanol, reflux under reduced pressure at 50 ° C, while maintaining the temperature and magnetic stirring for 2 hours, then remove the organic solvent by rotary evaporation under reduced pressure to obtain a solid residue, and dry it in vacuum for 12 hours. Obtain the complex of daidzein and phospholipid;

[0076] Add 0.5g of soybean lecithin, 1.0g of sodium oleate, and 0.2g of glyceryl behenate to the complex of daidzein and phospholipid, dissolve them in 20mL of dichloromethane, and then rotary evaporate to form a thin film; 20mL of distilled water preheated to 50°C was shaken horizontally in a 50°C water bath for 5 minutes t...

Embodiment 2

[0079] composition:

[0080] Daidzein 100mg

[0081] Yolk Lecithin 1.0g

[0082] Sodium Oleate 1.0g

[0083] Glyceryl monostearate 0.5g

[0084] Preparation method: It is prepared by thin film-high pressure homogeneous method, and the specific preparation operation is as follows:

[0085] Take 100 mg of daidzein and 0.5 g of egg yolk lecithin, add 100 mL of methanol, reflux under reduced pressure at 50 ° C, while maintaining the temperature and magnetic stirring for 4 hours, then remove the organic solvent by rotary evaporation under reduced pressure to obtain a solid residue, and dry it in vacuum for 8 hours. Obtain the complex of daidzein and phospholipid;

[0086] Add 0.5g of egg yolk lecithin, 1.0g of sodium oleate, and 0.5g of glyceryl monostearate to the complex of daidzein and phospholipids, dissolve in 50mL of methanol, and then rotary evaporate to form a film; add 20mL of pre- Heat distilled water at 50°C, shake horizontally in a water bath at 50°C for 5 minutes ...

Embodiment 3

[0089] composition:

[0090] Daidzein 100mg

[0091] Hydrogenated Soy Lecithin 1.0g

[0092] Tween 80 1.0g

[0093] Stearic acid 0.5g

[0094] Preparation method: It is prepared by hot-melt-high-pressure homogeneous method, and the specific preparation operation is as follows:

[0095] Take 100 mg of daidzein and 0.6 g of hydrogenated soybean lecithin, add 100 mL of methanol, reflux under reduced pressure at 50 ° C, and maintain the temperature with magnetic stirring for 6 hours, then remove the organic solvent by rotary evaporation under reduced pressure to obtain a solid residue, and dry it in vacuum for 10 hours , to obtain the complex of daidzein and phospholipid;

[0096] Add 0.4g of hydrogenated soybean lecithin to the complex of daidzein and phospholipid, dissolve it in 5mL of chloroform, then add it into molten stearic acid (0.5g, 80°C), mix well, stir continuously, and evaporate the organic solvent , to obtain a uniformly mixed solid lipid mixture;

[0097] At t...

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Abstract

The invention relates to solid lipid nanoparticles of daidzein which is a hydrophobic medicine and a preparation method thereof. The average particle size of the solid lipid nanoparticles of daidzein is less than 100 nanometers; and based on weight part, the solid lipid nanoparticles comprise 1 part of daidzein, 5 to 30 parts of phospholipid, 1 to 50 parts of surfactant and 1 to 40 parts of solidlipid material, wherein the daidzein and phospholipid form a composite which is covered by solid lipid or the solid lipid and phospholipid. The daidzein solid lipid nanoparticles are prepared by a thin-film dispersion method or hot-melt dispersion method. The preparation method comprises: forming a composite of the daidzein and phospholipid; and covering the composite with the solid lipid nanoparticles for solving the problems of low solubility, low stability and preparation difficulty in preparation process of the daidzein. The average particle size of the solid lipid nanoparticles is less than 100 nanometers, and the rate of in-vitro release in 8 hours reaches 58.4 percent, and the oral bioavailability is high; and the solid lipid nanoparticles can be further prepared into capsules, oral suspension, oral liquid and other oral preparation, and can make the medicine taken by the patient easily.

Description

technical field [0001] The invention relates to a hydrophobic drug daidzein solid lipid nanoparticle and a preparation method of the solid lipid nanoparticle. Background technique [0002] Daidzein (Daidzein, also known as daidzein) is an isoflavone compound, mainly found in the dried roots or soybeans of the leguminous plants Pueraria mirifica and Pueraria puerariae, which can dilate coronary arteries, femoral arteries, and cerebral arteries. The role of blood flow can reduce myocardial oxygen consumption and improve coronary blood flow. Clinically, it is mainly used for the treatment of cardiovascular and cerebrovascular diseases. It has definite curative effect on hypertension, coronary heart disease, cerebral thrombosis, brain injury, prevention of arteriosclerosis, cerebral ischemia, etc. It can also be used for menopausal syndrome, angina pectoris, myocardial infarction, elderly Prevention and treatment of dementia, osteoporosis and other diseases. However, daidzein ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K47/48A61K31/352A61P9/00A61P9/12A61P9/10A61P15/12A61P25/28A61P19/10
Inventor 李亚平高芳黄彦张志文顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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