Glycyrrhetinic acid hydrogel preparation, its preparation method and its application

A glycyrrhetic acid and hydrogel technology, which is applied in pharmaceutical formulations, antiviral agents, medical preparations with inactive ingredients, etc. problems, to achieve the effects of stable properties, increased transdermal penetration, and simple preparation methods

Inactive Publication Date: 2012-11-21
TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the degradation of the drug in the gastrointestinal tract and the hepatic first-pass effect during oral administration, the bioavailability of the drug is reduced and fluctuating
Although intravenous infusion is effective, it is poorly tolerated by patients and is not suitable for the treatment of long-term and chronic diseases, and systemic application will produce aldosterone-like side effects
Therefore, the traditional oral and intravenous drug delivery methods are not the most ideal drug delivery methods for the treatment of skin diseases.

Method used

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  • Glycyrrhetinic acid hydrogel preparation, its preparation method and its application
  • Glycyrrhetinic acid hydrogel preparation, its preparation method and its application
  • Glycyrrhetinic acid hydrogel preparation, its preparation method and its application

Examples

Experimental program
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Embodiment 1

[0031] Weigh 2.0g of Carbomer 980, add it to 70g of ultrapure water to swell for 12 hours, then add 0.2g of hyaluronic acid, 0.1g of methylparaben and 0.1g of disodium EDTA and stir evenly to obtain a mixture Solution, use an appropriate amount of triethanolamine to adjust the pH value of the mixed solution to 6.0; dissolve 0.3g of glycyrrhetinic acid in 3ml of ethanol solution with a mass concentration of 75%, and add it to the mixed solution with a pH value of 6.0 under stirring conditions In the solution, after the ethanol is completely volatilized, triethanolamine is added while stirring, the pH value of the mixed solution is adjusted to 8.0, and the weight of the mixed solution is replenished to 100g with ultrapure water to obtain The hydrogel preparation (viscosity is 20 Pa.s), the obtained hydrogel preparation is placed in a refrigerator at 4°C for later use. Wherein based on the total weight of the hydrogel preparation, the content of Carbomer 980 in the hydrogel prepa...

Embodiment 2-4

[0034] Prepare the hydrogel preparation according to the method of Example 1, the difference is that the amount of glycyrrhetinic acid added to 100g of the hydrogel preparation is respectively 0.01g, 1.0g and 10.0g, to obtain the amount of glycyrrhetinic acid in the hydrogel preparation The contents are respectively 0.01 wt%, 1.0 wt% and 10.0 wt%.

Embodiment 5

[0036] Weigh 100g of Carbomer 971, add it to 500g of ultrapure water and swell for 12 hours to disperse evenly, then add 100g of butanediol, 25.0g of phenoxyethanol and 25.0g of potassium methylparaben and stir Obtain the mixed solution evenly, add 50g of lysine to adjust the pH value of the mixed solution to 8.0, dissolve 100g sodium glycyrrhetinate in 20ml of ethanol solution with a mass concentration of 25%, and add the above pH value to 8.0 under stirring conditions. In the mixed solution, after the ethanol is completely volatilized, the pH value of the mixed solution is adjusted to 8.5 with an appropriate amount of lysine while stirring, and the weight of the mixed solution is replenished to 1000g with ultrapure water, and the obtained As a hydrogel preparation (viscosity of 200 Pa.s) for external use on the skin, the obtained hydrogel preparation was placed in a refrigerator at 4° C. for later use. Wherein based on the total weight of the hydrogel preparation, the conten...

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Abstract

The invention relates to a hydrogel preparation for improving the permeation of an active component glycyrrhetinic acid and/or its salt through a barrier via skins, its preparation method, and its application in the dermatology. The glycyrrhetinic acid hydrogel preparation comprises 0.01-10wt% of the active component glycyrrhetinic acid and/or its salt, 0.01-10wt% of a gel matrix, 0.01-10wt% of a humectant, 0.01-5wt% of an antiseptic, 0.01-5wt% of a pH adjustment agent, and the balance water. The glycyrrhetinic acid hydrogel preparation has the advantages of simple preparation method, good storage stability, substantial improvement of the penetration amount through the skins, no irritation or anaphylaxis, good absorbency, and good safety, and can be used for preparing medicinal preparations for treating dermatoses comprising chronic urticaria, eczema, contact dermatitis and the like through skin administration.

Description

technical field [0001] The invention relates to a hydrogel preparation for improving active ingredient glycyrrhetinic acid and / or its salt to pass through the skin penetration barrier, a preparation method thereof, and an application of the hydrogel preparation in dermatology. Background technique [0002] Glycyrrhetinic acid (Glycyrrhetinic acid, 18β-GA) is the product of glycyrrhizic acid, a triterpenoid compound contained in licorice, which is hydrolyzed to remove two molecules of glucuronic acid. Glycyrrhetinic acid has anti-inflammatory, anti-ulcer, anti-allergic effects, etc. It is mainly used to treat eczema, hives, dermatitis, acne and other skin diseases. In 1985, Japan's Takizawa et al. found that glycyrrhetinic acid had an inhibitory effect on the proliferation of murine skin tumors. It not only had the effect of anti-mutation and inhibition of carcinogenic factors, but also inhibited the growth of experimental tumors. In addition, glycyrrhetinic acid can inhibit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/56A61K47/32A61K47/36A61K47/38A61K47/42A61P17/00A61P17/06A61P17/10A61P31/22A61P37/02A61P37/08
Inventor 高云华李爽
Owner TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI
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