HK1069102B - Pharmaceutical and cosmetic compositions against skin aging - Google Patents

Description

Pharmaceutical and cosmetic composition for resisting skin aging

The present invention relates to pharmaceutical and cosmetic compositions containing ingredients of plant origin for combating skin ageing.

More particularly, the present invention relates to pharmaceutical and cosmetic compositions for preventing skin aging, which contain a phospholipid complex of an extract of Vitis vinifera (Vitis vinifera) and a phospholipid complex of a triterpenoid extracted from centella asiatica (centellasian).

Skin aging is a complex biological process that can affect various layers of the skin, but its major effects are seen in the dermis layer. There are two biologically independent, simultaneous aging processes. The first is endogenous aging, which can affect the skin and possibly the internal organs. The second is extrinsic aging or photoaging, which is the result of exposure to the environment, primarily ultraviolet radiation. The consequences of endogenous aging are seen in the whole body of the skin, including areas not exposed to sunlight. Photoaging damage works in conjunction with tissue degradation from endogenous aging at sites exposed to sunlight, particularly in the face and back of the hands. Thus, the most obvious changes in the skin of the face and neck, the major areas of interest to the patient, are the result of a combination of endogenous and exogenous aging processes. Although other factors (e.g., smoking) may lead to the premature development of wrinkles, up to 80% of facial aging has been shown to be attributable to exposure to sunlight.

From a biochemical point of view, photoaging is thought to be mainly due to the excessive production and release of several proteases, mainly metalloproteinases (these are degrading enzymes that irreversibly damage collagen, elastin and hyaluronic acid, leaving scars and visible wrinkles in the dermis) by the interaction of keratinocytes and fibroblasts with ultraviolet radiation, and to the ability to eliminate in a very short time the oxidative stress of the normal skin antioxidant defence system.

For these common reasons, it is clear that there is a need to avoid premature aging of the skin by means of a means capable of counteracting the action of proteases on the dermis (and increasing the capacity of fibroblasts to produce and release new collagen fibres) and preventing the disappearance of the antioxidant defence system of the skin.

The present invention meets this need by providing pharmaceutical and cosmetic compositions containing the following ingredients of plant origin:

a) phospholipid complexes of standard grape extract 0.1 to 2.5%

b) Phospholipid complexes of standard centella asiatica extracts 0.1 to 2.5%

More preferably, the pharmaceutical and cosmetic compositions of the invention contain the following ingredients of vegetable origin, and have the following percentages:

a) phospholipid Complex of Standard grape extract 1%

b) Phospholipid Complex of Standard centella asiatica extract 1%

EP275,224 discloses a phospholipid complex (also referred to as "component a") of a standard grape extract. The extract consists of the polyphenolic fraction contained in the grape seeds and comprises gallic acid, free and gallated catechins and epicatechin monomers, dimers, trimers, tetramers, pentamers, hexamers and heptamers.

In vitro and in vivo studies have demonstrated that: said extract has a high antioxidant activity (10 to 200 times that of vitamin E based on experimental models), which includes scavenging the most reactive group classes and counteracting all phenomena related to the action of free radicals. Said extract is also characterized by the ability to inhibit xanthine oxidase and to react with Cu⁺⁺And Fe⁺⁺⁺Chelation, thereby preventing the release of enzyme-catalyzed free radicals in the tissue. Finally, the grape extract inhibits collagenase and other proteases, thereby causing connective tissue and skin to growThe skin is protected from the damaging effects of proteolytic enzymes released after uv irradiation and during the progression of inflammatory skin reactions, and it has a selective affinity for the skin and circulating tissues such as the capillaries and capillaries, and thus also protects the microcirculatory zone.

EP 283,713 discloses a phospholipid complex of standard centella asiatica extracts (also referred to as "component b").

The extract consists of a 4: 3 mixture of three different molecules with a powerful effect on collagen metabolism, said molecules being asiaticoside, asiatic acid and madecassic acid. These molecules can increase the ability of fibroblasts to take up amino acids such as L-proline and L-hydroxyproline (the most important amino acids in collagen composition from a qualitative-quantitative standpoint). The increased synthesis of collagen means that degraded old collagen fibres can be replaced more quickly by new collagen fibres.

WO 0178674 discloses compositions useful for the treatment and prevention of skin aging and wrinkles, comprising (1) leucocyanidin in the form of a grape extract, (2) triterpenoids in the form of a centella asiatica extract and (3) a fish cartilage extract, in preferred embodiments, components (1) and (2) may also be complexed with phospholipids in order to enhance bioavailability.

When subjected to toxicological tests, components a) and b) exhibit neither toxic nor irritating effects on the treated tissue.

In addition to the above indicated components a) and b), the composition of the invention may optionally comprise other active ingredients such as vitamin E (0.2 to 1%), zinc (0.1 to 0.3%), hydroxy acids (0.1 to 1%) and glycyrrhetinic acid or its complex with phospholipids (0.1 to 2.5%) to improve the antioxidant, anti-aging and anti-inflammatory properties of the composition.

The compositions of the present invention may be topically applied in the form of suitable liquid formulations (e.g., gels, lotions, milks (milks), emulsions, foams, and the like) or solid or semi-solid formulations (e.g., creams, ointments, lipsticks, and the like). The formulations may be prepared according to conventional methods such as those described in "Remington's Pharmaceutical Handbook" (Mack publishing company, new york, usa), together with suitable excipients such as lubricants, humectants, thickeners, emulsifiers, dyes, flavouring agents and the like.

Certain examples of inventive compositions are reported below.

Example 1 oil-in-Water emulsion

100 grams of emulsion contains:

phospholipid Complex of grape extract 0.20 g

1.00 g of phospholipid complex of triterpenoids extracted from centella asiatica

Isostearyl isostearate (Gattefose) 2.50 g

2.50 g of polyisoprene (Syntesqual-Vevy)

Decyl oleate (Cetiol V-Henkel) 2.00 g

Cetyl palmitate (Cutina CP-Henkel) 2.00 g

Cetearyl alcohol isononanoate

(cetearyl isononanoate, Cetiol SN-Henkel) 2.00 g

Polysorbate 80 (Tween 80-ICI) 1.00 g

Imidazolidinyl urea 0.30 g

Tocopherol 0.20 g

Ascorbyl palmitate 0.10 g

Methylchloroisothiazolinone (e) methylisothiazolinone

(Kathon CG-Rohm & Haas) 0.05 g

EDTA disodium 0.10 g

Butylated hydroxytoluene 0.05 g

Polyacrylamide (e) C_13-14Isoparaffin (e)

Laureth-7(Spiegel 305-Seppic) 2.50 g

Perfume 0.10 g

Adding pure water to 100.0 g

Example 2 oil-in-Water emulsion

100 grams of emulsion contains:

phospholipid Complex of grape extract 0.50 g

0.50 g of phospholipid complex of triterpenoid extracted from centella asiatica

Glycyrrhetinic acid phospholipid complex 1.50 g

C_12-15Alkyl benzoate (Finsolv TN-Finetex) 4.00 g

Cetyl palmitate (Cutina CP-Henkel) 3.00 g

2.50 g of polyisoprene (Syntesqual-Vevy)

Isostearyl isostearate (Gattefose) 2.50 g

Polysorbate 80 (Tween 80-ICI) 1.00 g

Imidazolidinyl urea 0.30 g

Methylchloroisothiazolinone (e) methylisothiazolinone

(Kathon CG-Rohm & Haas) 0.05 g

Tocopherol 0.20 g

Ascorbyl palmitate 0.10 g

EDTA disodium 0.10 g

Citric acid 0.05 g

Polyacrylamide (e) C_13-14Isoparaffin (e)

Laureth-7(Spiegel 305-Seppic) 2.00 g

Butylated hydroxytoluene 0.05 g

Perfume 0.10 g

Adding pure water to 100.0 g

Claims (6)

1. Comprises the following components of plant origin:

a) phospholipid complexes of standard grape extract 0.1 to 2.5%

b) Phospholipid complexes of standard centella asiatica extracts 0.1 to 2.5%

And conventional excipients and carriers.

2. Pharmaceutical and cosmetic compositions according to claim 1, containing the following ingredients of vegetable origin:

a) phospholipid Complex of Standard grape extract 1%

b) Phospholipid Complex of Standard centella asiatica extract 1%

And conventional excipients and carriers.

3. Pharmaceutical and cosmetic compositions according to claims 1 and 2, further comprising other active ingredients selected from the group consisting of vitamin E, zinc, hydroxy acids and glycyrrhetinic acid or complexes thereof with phospholipids.

4. The pharmaceutical and cosmetic composition of claim 3, wherein the percentage of other active ingredients is:

0.2 to 1 percent of vitamin E

0.1 to 0.3 percent of zinc

Hydroxy acid 0.1-1%

Glycyrrhetinic acid or its compound with phospholipid 0.1-2.5%

A) phospholipid complexes of standard grape extracts, and

b) phospholipid complexes of standard centella asiatica extracts

Use in the preparation of pharmaceutical and cosmetic compositions for combating skin ageing.

A) phospholipid complexes of standard grape extracts, and

b) phospholipid complexes of standard centella asiatica extracts

Use of a combination with other active ingredients selected from the group consisting of vitamin E, zinc, hydroxy acids and glycyrrhetinic acid or complexes thereof with phospholipids for the preparation of pharmaceutical and cosmetic compositions for combating skin ageing.