Daidzein micelles and preparation method thereof

A technology of daidzein and micelles, which is applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of poor solubility of daidzein, cloudy micellar suspension, and low drug loading rate, etc. problem, to achieve the effect of improving bioavailability, solubility and bioavailability

Inactive Publication Date: 2011-05-18
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

For daidzein, the biggest difficulty in preparing micelles is that the solubility of daidzein in various pharmaceutically acceptable organic solvents is very poor. Since it cannot be dissolved in such organic solvents, soybeans prepared by conventional methods The drug-loading rate of aglycon micelles is very low, even after the micelles are barely formed, the stability is poor, and daidzein is easy to precipitate, and it can be observed that the prepared micellar suspension quickly becomes cloudy

Method used

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  • Daidzein micelles and preparation method thereof
  • Daidzein micelles and preparation method thereof
  • Daidzein micelles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 (in this example, daidzein: phospholipids: the weight ratio of the additive is 1: 12: 10)

[0039] Take 1.0g of daidzein and 10g of soybean lecithin, add 10mL of acetone, heat to 60°C under reduced pressure and reflux, heat and stir for 10 hours, recover the acetone, dry, and pulverize to obtain the phospholipid complex; add soybean lecithin 2.0 to the phospholipid complex g, 10 g of glycerin, dissolved in 200 mL of ethanol, rotatively evaporated to form a film, and hydrated at 50 ° C to obtain daidzein micelles. The average particle diameter measured is 30nm, and the in vitro dissolution rate in 24 hours is 82%. Determination of its oral bioavailability, AUC of daidzein micelles 0-∞ 97152ng·h·mL -1 . Add water for injection and dilute to make 10mg / mL injection.

Embodiment 2

[0040] Embodiment 2 (in this embodiment, daidzein: phospholipid: the weight ratio of additive is 1: 25: 20)

[0041] Take 1.0g of daidzein and 20g of egg yolk lecithin, add 50mL of ethanol, heat to 40°C and reflux under reduced pressure, keep warm and stir for 5 hours, recover the ethanol, dry, and pulverize to obtain the phospholipid complex; add egg yolk egg to the phospholipid complex Dissolve 5.0 g of phospholipids and 20 g of sodium cholate in 200 mL of ethanol, rotatively evaporate to form a film, and hydrate at 50°C to obtain daidzein micelles. The average particle diameter measured is 20nm, and the in vitro dissolution rate in 24 hours is 92%. Determination of its oral bioavailability, AUC of daidzein micelles 0-∞ 131571ng·h·mL -1 . Add 0.02% sodium saccharin and distilled water to make 50mg / mL oral solution.

Embodiment 3

[0042] Example 3 (in this example, daidzein: phospholipids: the weight ratio of the additive is 1:30:4)

[0043] Take 1.0g of daidzein and 15g of soybean lecithin, add 20mL of methanol, heat to 60°C and reflux under reduced pressure, heat and stir for 2 hours, recover methanol, dry, and pulverize to obtain the phospholipid complex; add 15g of soybean lecithin to the phospholipid complex , Sodium cholate 4g, dissolved in 300mL ether, rotary evaporation to form a film, and hydrated at 50°C to obtain daidzein micelles. The measured average particle diameter is 30nm, and the in vitro dissolution rate in 24 hours is 84%. Determination of its oral bioavailability, AUC of daidzein micelles 0-∞ 116254ng·h·mL -1 . Add mannitol and water for injection, and freeze-dry to make freeze-dried powder for injection.

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Abstract

The invention relates to daidzein micelles and a preparation method thereof. The daidzein micelles contain 1 part of daidzein, 12 to 30 parts of phospholipid and 1 to 25 parts of additive. The preparation method comprises: preparing a daidzein and phospholipid composite, namely, adding daidzein and 50 to 95 percent of phospholipid into an organic solvent, heating the solution to 40 to 60 DEG C, refluxing under reduced pressure, keeping temperature and stirring for 2 to 10 hours, recovering the organic solvent, drying and crushing to obtain the daidzein and phospholipid composite; and preparing daidzein micelles from the phospholipid composite, namely, dissolving the daidzein and phospholipid composite, the rest phospholipid and the additive in an organic solvent, subjecting the solution to rotary evaporation to form a film, and hydrating at 40 to 60 DEG C to obtain daidzein micelle suspension with opalescence. The average particle size of the daidzein micelles is less than 50 nanometers. The daidzein micelles can be further prepared into oral or injection preparations including capsules, oral mixed suspension, oral liquid, injection, injection freeze-dried powder injection.

Description

technical field [0001] The invention relates to a daidzein micelle and a preparation method of the micelle. Background technique [0002] Daidzein, also known as daidzein and daidzein, is an isoflavone compound extracted and isolated from the dried roots of kudzu and kudzu root or soybean. It can obviously relieve angina pectoris, has the pharmacological effects of antiarrhythmia, antioxidation, and hypoglycemia, and also has protective effects on acute myocardial ischemia and cerebral ischemia. At present, daidzein is mainly used in the treatment of cardiovascular and cerebrovascular diseases clinically, and has significant curative effects on hypertension, coronary heart disease, cerebral thrombosis, brain injury, prevention of arteriosclerosis, and cerebral ischemia. However, due to its poor water solubility and fat solubility, it affects the absorption and distribution after oral administration, so its bioavailability is poor. It is reported in the literature that the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/48A61K9/08A61K9/19A61K31/352A61K47/24A61K47/28A61P9/12A61P9/10A61P7/02A61P25/00
Inventor 李亚平张志文黄彦陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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