Glycyrrhetinic acid emulsion and preparation method thereof

A technology of glycyrrhetinic acid and acid emulsion, which is applied in antiviral agents, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of liposome instability, industrial pollution, high cost, etc., and achieve reduced dosage volume and bioavailability The effect of high and small individual differences

Active Publication Date: 2011-06-08
北京中海康医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] Although the glycyrrhetinic acid salt disclosed in the above Chinese patent can improve the water solubility of the drug, the synthesis reaction steps of glycyrrhetinic acid structure modification are various, the conditions are harsh, and the cost is high, which is easy to cause environmental pollution, and it may be difficult to introduce impurities into the preparation production. Control and other issues, especially the quality standards of raw materials for injections need to

Method used

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  • Glycyrrhetinic acid emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1. Prescription: Glycyrrhetinic acid 6g

[0043] Refined soybean oil 50g

[0044] Soy Lecithin 1g

[0045] Oleic acid 0.01g

[0046] Add water to 1000ml

[0047] 2. Process:

[0048] (1) Preparation of the oil phase: add 1 g of soybean lecithin, 0.01 g of oleic acid and 60 mg of glycyrrhetinic acid to 50 g of refined soybean oil, stir to dissolve it, and use it as the oil phase;

[0049] (2) Preparation of colostrum: add the oil phase obtained in the step (1) into water, disperse at high speed for 10 minutes, and the shear rate is 10,000 rpm to form colostrum, and keep the temperature of the solution at about 80°C;

[0050] (3) High-pressure homogenization: the pH of the colostrum obtained in the step (2) was adjusted to 6.0, and the high-pressure homogenization was performed 3 times at a homogenization pressure of 2000 bar to obtain a glycyrrhetinic acid oral emulsion.

Embodiment 2

[0052] 1. Prescription: Glycyrrhetinic acid 20g

[0053] Refined soybean oil 300g

[0054] Soy Lecithin 60g

[0055] Oleic acid 30g

[0056] Glycerin 22g

[0057] Add water for injection to 1000ml

[0058] 2. Process:

[0059] (1) Preparation of the oil phase: add 60 g of soybean lecithin, 30 g of oleic acid and 20 g of glycyrrhetinic acid respectively in 300 g of refined soybean oil, stir to make it dissolve, as the oil phase;

[0060] (2) Preparation of the water phase: add glycerin to water, stir to dissolve it, and use it as the water phase;

[0061](3) Preparation of colostrum: add the oil phase obtained in the step (1) into the water phase obtained in the step (2), disperse at high speed for 30 minutes, and the shear speed is 6000 rpm to form colostrum and keep the solution The temperature is around 60°C;

[0062] (4) High-pressure homogenization: adjust the pH of the colostrum obtained in the step (3) to 7.0, high-pressure homogenize 4 times, and the homogenizati...

Embodiment 3

[0066] 1. Prescription: Glycyrrhetinic acid 8g

[0067] Refined soybean oil 100g

[0068] Soy Lecithin 20g

[0069] Oleic acid 5g

[0070] Glycerin 22g

[0071] Add water for injection to 1000ml

[0072] 2. Process:

[0073] (1) Preparation of the oil phase: add 20 g of soybean lecithin, 5 g of oleic acid and 8 g of glycyrrhetinic acid respectively in 100 g of refined soybean oil, stir to dissolve it, and use it as the oil phase;

[0074] (2) Preparation of the water phase: add glycerin to water, stir to dissolve it, and use it as the water phase;

[0075] (3) Preparation of colostrum: add the oil phase obtained in the step (1) into the water phase obtained in the step (2), disperse at high speed for 60 min, and the shear rate is 1000 rpm to form colostrum and keep the solution The temperature is around 50°C;

[0076] (4) High-pressure homogenization: adjust the pH of the colostrum obtained in the step (3) to 7.5, high-pressure homogenize 6 times, and the homogenization...

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Abstract

The invention relates to glycyrrhetinic acid emulsion and a preparation method thereof, and the emulsion contains glycyrrhetinic acid, oil, an emulsifier and a stabilizer, wherein the weight-volume percent of the glycyrrhetinic acid is 0.6-2%, the weight-volume percent of the oil is 5-30%, the weight-volume percent of the emulsifier is 0.1-6%, and the weight-volume percent of the stabilizer is 0.01-3%. The structure of the glycyrrhetinic acid does not need to be transformed, thereby keeping the original efficacy; simultaneously, the use of an organic solvent can be avoided, the potential safety hazard can be reduced, and the industrial production can be facilitated.

Description

technical field [0001] The invention relates to an emulsion containing insoluble drug glycyrrhetinic acid and a preparation method thereof. Background technique [0002] Glycyrrhetinic acid (Glycyrrhetinic acid), also known as glycyrrhetinic acid, is a kind of triterpenoid saponin glycyrrhizic acid in licorice hydrolyzed to remove the product of sugar acid chain. Glycyrrhetinic acid is the active ingredient after the metabolism of glycyrrhizic acid (such as monoammonium glycyrrhizinate, diammonium glycyrrhizinate) in vivo. Glycyrrhetinic acid has anti-ulcer, antibacterial, anti-tumor, anti-hepatitis, hypolipidemic and anti-HIV activities [Xie Shi Rong, Zhao Jie, Liu Lin, etc. Research and Prospect of Glycyrrhetinic Acid. Journal of Dalian University. 2005, 26(4): 85-88]. Glycyrrhetinic acid has made a breakthrough in the application research of anti-liver disease. It can protect the liver by improving the adsorption capacity of liver cells, and has the effect of inhibiting ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/14A61K9/19A61K31/56A61P1/04A61P31/04A61P35/00A61P1/16A61P3/06A61P31/18
Inventor 伞红男郑建华黄海宋华先王娟徐庆春
Owner 北京中海康医药科技发展有限公司
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