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Madecassoside lipidosome and preparation method and application thereof

The technology of madecassoside and madecassoside lipid is applied in the field of madecassoside liposome and its preparation, and can solve the problem of large molecular weight of madecassoside, less application of madecassoside, and difficulty in penetration Skin absorption and other problems, to achieve the effect of promoting transdermal absorption, avoiding systemic adverse reactions, and promoting permeability

Active Publication Date: 2014-07-02
西安雷博士药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the high molecular weight of madecassoside, it is difficult to absorb through the skin, and the application is limited, resulting in less application of madecassoside in external medicine and cosmetics

Method used

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  • Madecassoside lipidosome and preparation method and application thereof
  • Madecassoside lipidosome and preparation method and application thereof
  • Madecassoside lipidosome and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] A kind of madecassoside liposome is prepared by the following method:

[0045] (1) Weigh 4.0g egg yolk lecithin and 0.5g cholesterol into a 100ml eggplant-shaped bottle, add 30ml chloroform to prepare lipid solution;

[0046] (2) Place the above-mentioned eggplant-shaped bottle in a constant temperature water bath at 30°C, evaporate chloroform under reduced pressure on a rotary evaporator, and form a layer of lipid film on the inner wall of the eggplant-shaped bottle;

[0047] (3) Add 30ml of pH=6.5 phosphate buffer solution with 1.0g of madecassoside dissolved in the eggplant-shaped bottle, rotate and shake to make the lipid film fall off the inner wall of the eggplant-shaped bottle, and hydrate to form a uniform emulsion ;

[0048] (4) The above emulsion was sonicated for 60 s in an ice-water bath by a water-bath sonicator to obtain the madecassoside liposomes, which were stored at 4°C.

Embodiment 2

[0050] A kind of madecassoside liposome is prepared by the following method:

[0051] (1) Weigh 4.0g of egg yolk lecithin, 0.5g of cholesterol, and 0.1g of VE acetate into a 100ml eggplant-shaped bottle, add 30ml of chloroform to prepare a lipid solution;

[0052] (2) Place the above-mentioned eggplant-shaped bottle in a constant temperature water bath at 30°C, evaporate chloroform under reduced pressure on a rotary evaporator, and form a layer of lipid film on the inner wall of the eggplant-shaped bottle;

[0053] (3) Weigh 1.5g of sodium dihydrogen phosphate, make it to volume in a 250ml volumetric flask, add sodium hydroxide to adjust the pH to 6.5, and obtain a phosphate buffer solution with pH=6.5;

[0054] (4) Add 30ml of the above-mentioned phosphate buffer solution with 1.0g of madecassoside dissolved in the eggplant-shaped bottle in step (2), rotate and shake to make the lipid film fall off the inner wall, and the hydrated lipid film is formed evenly lotion;

[0055...

Embodiment 3

[0057] A kind of madecassoside liposome is prepared by the following method:

[0058] (1) Weigh 4.0g egg yolk lecithin, 0.5g cholesterol, 0.1g VE acetate and dissolve in 30ml absolute ethanol, heat and shake the flask to completely dissolve the additives, and prepare a lipid solution.

[0059] (2) Place the flask containing the lipid solution on a rotary evaporator, evaporate under reduced pressure at 50°C to remove ethanol, and form a lipid film;

[0060] (3) Add 1.0g of madecassoside to 30ml of phosphate buffered saline solution (PBS, pH=6.5) to make a madecassoside solution; add the madecassoside solution to the flask in step (2), Shake to hydrate the lipid film, forming an emulsion;

[0061] (4) Squeeze the above emulsion through a microporous membrane to obtain the madecassoside liposome.

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Abstract

The invention belongs to the fields of drug preparations and cosmetics, and particularly relates to madecassoside lipidosome and a preparation method and application thereof. The method comprises the following steps: dissolving or heating and fusing madecassoside and lipidosome components through an organic solvent; concentrating or drying; adding a hydration medium containing the madecassoside to hydrate, so as to prepare a lipid disperse aqueous solution; and forming the madecassoside lipidosome by homogeneous treatment. The madecassoside lipidosome can be prepared into the forms such as emulsion, cream, paste, turunda or freeze-dried powder, and all adopted traditional use forms. The lipid component is taken as a carrier, so that the transdermal performance, slow release and the bioavailability of the madecassoside can be improved, and the madecassoside can be reserved in the skin to the maximal extent. Thus, the efficacy is effectively played, and especially, transdermal absorption can be achieved by local skin or mucous membrane painting.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and cosmetics, and in particular relates to a madecassoside liposome, a preparation method and application thereof. Background technique [0002] Madecassoside is one of the main triterpenoid saponins in Centella asiatica (L.) Urban. Centella asiatica has the effects of clearing heat and dampness, reducing swelling and detoxification, and can treat burns and skin ulcers, such as intractable wounds, skin tuberculosis, and leprosy. Madecassoside is one of the main active ingredients of Centella asiatica in the treatment of skin diseases. Its biological activities are: (1) Promote wound healing and scar repair. Madecassoside can promote cell growth (Liu M, Dai Y ,Li Y et al.Planta Med,2008,74(8):809-815.); (2) Antioxidant effect, improve cell viability, increase glutathione level, reduce lactate dehydrogenase level, protect human endothelial Umbilical vein endothelial cells are not oxidiz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7024A61K8/14A61K8/63A61P17/02A61Q19/02A61Q19/00
Inventor 刘美凤王慧娟
Owner 西安雷博士药业有限公司
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