阅读说明：本技术 甘油葡萄糖苷在透皮吸收组合物中的应用 (Application of glycerol glucoside in transdermal absorption composition ) 是由 吕雪峰 段仰凯 张凯 吴怀之 刘祥 李新 于 2019-12-03 设计创作，主要内容包括：本发明公开了甘油葡萄糖苷在透皮吸收组合物中的应用。本发明首次研究并证明了施用较高浓度的甘油葡萄糖苷能够显著提高其透皮吸收量和渗透率,从而使得组合物的吸收效果增强,同时有利于制备的组合物的活性物质穿过角质层到达相应的真皮层或者其他皮肤层,使得组合物具有更好的保湿、护肤、美白等功效,拓展了甘油葡萄糖苷的应用,因此具有良好的实际应用之价值。(The invention discloses application of glycerol glucoside in a transdermal absorption composition. The invention researches and proves for the first time that the application of the glycerol glucoside with higher concentration can obviously improve the transdermal absorption capacity and the penetration rate of the glycerol glucoside, thereby enhancing the absorption effect of the composition, being beneficial to the active substances of the prepared composition to penetrate through the horny layer to reach the corresponding dermis layer or other skin layers, leading the composition to have better effects of moisturizing, skin care, whitening and the like, expanding the application of the glycerol glucoside and having good value of practical application.)

1. Application of glycerol glucoside in preparing transdermal absorption penetration enhancer is provided.

2. The use according to claim 1, wherein the effective concentration of the glycerol glucoside is not less than 10mg/mL, further 10 to 20mg/mL, and further 20 mg/mL.

3. A percutaneous absorption enhancer, wherein the active component of the percutaneous absorption enhancer at least contains glycerol glucoside;

preferably, the effective concentration of the glycerol glucoside is not less than 10mg/mL, further 10-20 mg/mL, and further 20 mg/mL.

4. Use of a glycerol glucoside and/or a transdermal penetration enhancer of claim 3 in the preparation of a transdermal composition.

5. Use according to claim 4, wherein the composition comprises cosmetics and pharmaceuticals, preferably cosmetics.

6. The use according to claim 5, wherein the effective concentration of the glycerol glucoside is not less than 10mg/mL, further 10-20 mg/mL, and further 20 mg/mL.

7. The use according to any one of claims 4 to 6, wherein the composition has any one or more of the following uses:

1) moisture preservation;

2) whitening;

3) anti-aging;

4) the elasticity of the skin is increased;

5) repairing the cells.

8. A transdermal absorption composition comprising glycerol glucoside and at least one other active ingredient and/or at least one other active ingredient.

9. The composition of claim 8, wherein the other active ingredients have at least one of effects of promoting skin absorption or inhibiting accumulation of neutral lipids in adipocytes, improving cell viability, and increasing cellular hyaluronic acid and collagen synthesis;

other inactive ingredients include pharmaceutically/cosmetically acceptable carriers, excipients and/or diluents.

10. The composition of claim 8, wherein the composition is in a dosage form comprising a spray, cream, ointment, lotion, emulsion, gel, or hydrogel.

Technical Field

The invention belongs to the technical field of medicines/cosmetics, and particularly relates to application of glycerol glucoside in a transdermal absorption composition.

Background

The information in this background section is only for enhancement of understanding of the general background of the invention and is not necessarily to be construed as an admission or any form of suggestion that this information forms the prior art that is already known to a person of ordinary skill in the art.

Glycerol Glucosides (GG) are glycoside compounds formed by connecting glycerol molecules and glucose molecules through glycosidic bonds, and 6 different steric structures exist in nature according to the difference between the steric configurations (α and β) and the glycosidic bond connection positions, wherein the structure with important physiological functions is 2- α configuration (GG represents 2- α GG when not particularly explained below), and researches prove that the GG has the main extremely strong skin moisturizing function and is initially applied to cosmetics.

The primary barrier function of the skin to restrict the communication of substances in and out of the body comes from the compact structure of the stratum corneum. The rate of penetration of the stratum corneum by the substance in vitro is also the major rate-limiting step in transdermal absorption. Taking a human body as an example, the stratum corneum of human skin is the outermost layer of epidermis and consists of 4-8 dead flat lamellar anucleated cells. Among them, keratinocytes together with intercellular lipids constitute the most basic protective layer of the outermost layer of the skin, called the "skin barrier".

The stratum corneum can protect the skin, prevent in vivo interstitial fluid from exosmosis, limit the barrier function of water, lipid or cosmetic ingredient skin stratum corneum, the stratum corneum has hindered the percutaneous permeation of most foreign substances, there is research that, in the transdermal experiment of the separation, after stripping the stratum corneum of skin, the permeability of the substance can be increased by tens of times or even hundreds of times. However, regarding the research on transdermal absorption, at present, many studies on transdermal absorption of drugs are conducted at home and abroad, and the research mainly focuses on several aspects such as drug penetration characteristics, pharmacokinetic analysis, selection of penetration enhancer and the like, while the research on cosmetic transdermal absorbents and action mechanisms is very limited.

Meanwhile, at present, the cell physiological function of GG is only limited to cell culture tests, and the skin transdermal property and the skin penetration rate of GG determine the practical application of the cell physiological function of GG to a certain extent, however, no report about whether GG can be absorbed transdermally is available at present.

Disclosure of Invention

In view of the above-mentioned deficiencies of the prior art, the present invention provides a use of glycerol glucoside in a transdermal absorption composition. Researches prove that the transdermal absorption capacity and the permeability of the GG can be remarkably improved by improving the concentration of the glycerol glucoside in a proper concentration range, so that a feasible theoretical basis is provided for expanding the application of other compositions except for a moisturizing product.

In order to achieve the purpose, the invention adopts the following technical scheme:

in a first aspect of the invention, there is provided the use of a glycerol glucoside in the preparation of a penetration enhancer for transdermal absorption.

In a second aspect of the present invention, there is provided a transdermal absorption enhancer, wherein the active ingredient of the transdermal absorption enhancer contains at least glycerol glucoside.

In a third aspect of the present invention, there is provided the use of the above-mentioned glycerol glucoside and/or transdermal absorption enhancer for the preparation of a transdermal absorption composition.

The composition includes, but is not limited to, cosmetics and pharmaceuticals, and further preferably cosmetics.

The composition has any one or more of the following uses:

1) moisture preservation;

2) whitening;

3) anti-aging;

4) the elasticity of the skin is increased;

5) repairing the cells.

According to the present invention, not only the effect of glycerol glucoside as a means for preparing a transdermal absorption composition is disclosed, but also it is disclosed that such effect can be enhanced when glycerol glucoside is administered in combination with at least one other active ingredient, such as a cosmetic active ingredient or a pharmaceutical active ingredient. As an alternative or in addition to the other active ingredients, it is also possible to use them in combination with other inactive ingredients.

In view of the above, the fourth aspect of the present invention discloses a cosmetic or pharmaceutical composition with transdermal absorption, which is composed of glycerol glucoside and at least one other active ingredient and/or at least one other active ingredient.

According to the use of the invention, the administration of the composition can be carried out topically, transdermally, as an aerosol or dry powder formulation. Specific dosage forms of the composition include, but are not limited to, sprays, creams, ointments, lotions, emulsions, gels or hydrogels.

The invention has the beneficial effects that:

the invention researches and proves for the first time that the application of the glycerol glucoside with higher concentration can obviously improve the transdermal absorption capacity and the penetration rate of the glycerol glucoside, thereby enhancing the absorption effect of the composition, being beneficial to the active substances of the prepared composition to penetrate through the horny layer to reach the corresponding dermis layer or other skin layers, leading the composition to have better effects of moisturizing, skin care, whitening and the like, expanding the application of the glycerol glucoside and having good value of practical application.

Drawings

In order to more clearly illustrate the technical solutions of the embodiments of the present invention, the drawings needed to be used in the description of the embodiments are briefly introduced below, and it is obvious that the drawings in the following description are only embodiments of the present invention, and it is obvious for those skilled in the art to obtain other drawings according to the provided drawings without creative efforts.

FIG. 1 is a graph of the cumulative mean osmolarity of glycerol glucoside at various concentrations in accordance with the present invention.

FIG. 2 is a graph of mean permeability of glycerol glucoside at different concentrations according to the present invention.

Detailed Description

It is to be understood that the following detailed description is exemplary and is intended to provide further explanation of the invention as claimed. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.

It is noted that the terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting of example embodiments in accordance with the present application. As used herein, the singular forms "a", "an" and "the" are intended to include the plural forms as well, and it should be understood that when the terms "comprises" and/or "comprising" are used in this specification, they specify the presence of stated features, steps, operations, devices, components, and/or combinations thereof, unless the context clearly indicates otherwise.

As mentioned above, at present, the cell physiological function of the glycerol glucoside is only limited to cell culture tests, and the skin transdermal property and the skin penetration rate of the glycerol glucoside determine the practical application of the cell physiological function of the glycerol glucoside to a certain extent, however, at present, no report on whether the glycerol glucoside can be transdermally absorbed through skin exists.

In view of the above, one embodiment of the present invention discloses the use of glycerol glucoside in the preparation of transdermal penetration enhancers.

In another embodiment of the present invention, the effective concentration of the glycerol glucoside is not less than 10mg/mL, more preferably 10 to 20mg/mL, and still more preferably 20 mg/mL.

In another embodiment of the present invention, there is provided a transdermal absorption enhancer, wherein the active ingredient of the transdermal absorption enhancer contains at least glycerol glucoside.

The effective concentration of the glycerol glucoside is not less than 10mg/mL, further 10-20 mg/mL, and further 20 mg/mL.

In another embodiment of the present invention, there is provided a use of the above-mentioned glycerol glucoside and/or transdermal absorption enhancer for the preparation of a transdermal absorption composition.

In yet another embodiment of the present invention, the composition includes, but is not limited to, cosmetics and pharmaceuticals, and further preferably cosmetics.

In another embodiment of the present invention, the effective concentration of the glycerol glucoside is not less than 10mg/mL, more preferably 10 to 20mg/mL, and still more preferably 20 mg/mL.

In yet another embodiment of the invention, the composition has any one or more of the following uses:

1) moisture preservation;

2) whitening;

3) anti-aging;

4) the elasticity of the skin is increased;

5) repairing the cells.

The experimental research proves that the transdermal absorption capacity and the permeability of the glycerol glucoside can be effectively improved by improving the concentration of the glycerol glucoside in a proper range, so that the application of the glycerol glucoside in the fields of cosmetics and the like is effectively expanded. Therefore, the composition containing the glycerol glucoside with higher effective concentration is not only suitable for nursing daily skin, but also suitable for the problem skin with fatigue, stress (such as UV radiation and PM2.5 pollution relief), aging, sensitivity, eczema and the like.

According to the present invention, not only the effect of glycerol glucoside as a means for preparing a transdermal absorption composition is disclosed, but also it is disclosed that such effect can be enhanced when glycerol glucoside is administered in combination with at least one other active ingredient, such as a cosmetic active ingredient or a pharmaceutical active ingredient. As an alternative or in addition to the other active ingredients, it is also possible to use them in combination with other inactive ingredients.

In view of the above, in yet another embodiment of the present invention, a transdermally absorbable cosmetic or pharmaceutical composition comprising glycerol glucoside and at least one other active ingredient and/or at least one other active ingredient is disclosed.

Wherein other active ingredients have the effects of promoting skin absorption or inhibiting accumulation of neutral lipid in fat cells, improving cell activity, and improving cell hyaluronic acid and collagen synthesis.

Other inactive ingredients include pharmaceutically/cosmetically acceptable carriers, excipients and/or diluents. Such as pharmaceutically compatible inorganic or organic acids or bases, polymers, copolymers, block copolymers, monosaccharides, polysaccharides, ionic and non-ionic surfactants or lipids, pharmacologically harmless salts such as sodium chloride, flavoring agents, vitamins such as vitamin a or vitamin E, tocopherols or similar vitamins or provitamins present in the human organism, antioxidants such as ascorbic acid, and stabilizers and/or preservatives for prolonging the use and shelf life of the pharmaceutically active ingredient or formulation, and other common non-pharmaceutically active ingredients or adjuvants and additives known in the art, and mixtures thereof. Other non-pharmaceutically active ingredients preferred according to the invention are in particular all substances which can form hydrogels, for example natural or synthetic water-soluble polymers which can form networks.

According to the use of the invention, the administration of the composition can be carried out topically, transdermally, as an aerosol or dry powder formulation. Specific dosage forms of the composition include, but are not limited to, sprays, creams, ointments, lotions, emulsions, gels or hydrogels.

The mode of application is preferably topical and transdermal, by applying the composition on the skin, preferably a liquid, gas (aerosol or vapor), formulation containing the glycerol glucoside, preferably as a cream, ointment, lotion, emulsion, or gel or hydrogel.

Wherein the effective concentration of the glycerol glucoside is not less than 10mg/mL, further 10-20 mg/mL, and further 20 mg/mL.

The preferred topical or transdermal application according to the invention allows to apply a high effective glycerol glucoside concentration locally on the skin, to promote the penetration of the active principle (including glycerol glucoside) into the epidermal cells for repair, hydration, etc., while reducing or completely avoiding the load of the system (blood circulation) and possible side effects on healthy skin tissues and tissues of other organs which do not require application.

In still another embodiment of the present invention, the glycerol glucoside has a 2- α configuration.

The present invention is further illustrated, but is not intended to be limited, by the following examples, which are set forth in the accompanying drawings, it being understood that these examples are included merely for purposes of illustration and are not intended to limit the scope of the invention, the glycerol glucosides in the examples being in the 2- α configuration.