Patent Application
20070224230
The present invention relates to cosmetic formulations containing sucralfate in combination with copper sulfate and zinc sulfate, used as tissue regenerators, cicatrizing agents and antiinflammatory agents.
Sucralfate is basic aluminum sucrose sulfate, and is used as a medicinal product in the treatment of gastric and duodenal ulcers under the brand names Ulcar® and Keal®.
When absorbed at a dose of from 0.5 to 2 g per day in a dry form such as a tablet or chewable granules, sucralfate acts on the digestive tract by lining the mucous membrane of the stomach and the duodenum with a protective gel.
The formation of this gel is consecutive to the reaction that takes place between sucralfate and the hydrochloric acid of the gastric and duodenal medium, and, as a result of the electromagnetic tropism it displays toward positively charged protein molecules, it forms a complex with them that insulates and protects gastric ulcers.
Moreover, sucralfate inhibits the proteolytic activity of pepsin. Thus, it allows and promotes the natural cicatrization of ulcers.
The present invention relates to the cosmetic use, thus via the topical route, of formulations containing sucralfate in combination with copper sulfate and zinc sulfate, as tissue regenerators, cicatrizing agents and calmatives.
According to one particular characteristic of the present invention, the cosmetic composition has a sucralfate content of between 0.01% and 5% by weight and preferably about 1% by weight.
According to another characteristic of the present invention, the cosmetic composition comprises from 0.02% to 2% by weight and preferably between 0.3% and 2% by weight of sulfates.
According to another characteristic of the present invention, the composition comprises a weight ratio of sucralfate to sulfates of between 0.5 and 20 and preferably between 0.5 and 1.
According to another characteristic of the present invention, the cosmetic composition contains a weight ratio of copper sulfate to zinc sulfate of between 1 and 3.
The formulation examples given below are intended to illustrate the invention and are cited in a purely nonlimiting manner.
Dermocosmetic Evaluation
The aim of this study was to evaluate the regenerating, cicatrizing and calmative properties of the cream of Example 1.
The experimental model adopted was the skin blister model. This is a standard technique generally used to comparatively study, on an untreated skin surface, the effect of a product on the rate and quality of re-epidermization of a fully delimited area of skin from which the epidermal layer above the dermo-epidermal function has been cut away beforehand.
Methodology
The test was performed on 6 volunteers. The experimental region selected is the inner face of the forearm (a region that is little exposed to ultraviolet radiation and to any external mechanical attack), on which six skin blisters with fully delimited contours were made.
After removing the detached epidermis, five blisters received the cream of Example 1 and/or the excipients of this cream (i.e. without the sucralfate, the copper sulfate and the zinc sulfate). The 6th blister was considered as the untreated control. The application of the excipient(s) was performed daily by a dermatologist for 14 consecutive days.
Each product was taken up using a disposable sterile syringe (without a needle) and then placed over the entire surface of the skin blister so as to form a uniform layer about 1 mm thick.
Each application was preceded by cleaning the blisters to be treated using sterile compresses impregnated with sterile physiological saline, by gentle vertical padding. Each blister was then covered with a sterile compress attached using an adhesive dressing. The dressings were left in place until the next clinical observation.
The regenerating properties were assessed by means of a quanti-qualitative method for measuring the rate and quality of epidermization over a 14-day period. The rate of epidermization was calculated (after measuring the injured areas by image analysis) according to the formula ST−S0/T with ST=area injured at time T and S0=area injured at time T0, T being the time in which a first total epidermization is obtained in a volunteer.
The quality of the epidermization was assessed by comparison of the clinical criteria relating to the quality of skin obtained during the controls at D14 and D1 (before the formation of the skin blisters).
The evaluation criteria were the following:
The cream of Example 1 shows a mean rate of epidermization (Vi=11.72 mm2/day) that is twice as fast as that observed on an untreated blister and total reepidermization of 100% of the blisters on D4.
The excipient of this cream shows a mean rate of epidermization (V2=8 mm2/day) that is 1.5 times faster than that observed on untreated control blisters, and a reepidermization of 70% of the blisters at D4.
Intensity of the Erythema
Cream of Example 1<excipient of Example 1<control
Thinness of the Skin
Cream of Example 1>excipient of Example 1>control
Suppleness of the Skin
Cream of Example 1>excipient of Example 1>control
Normal Epidermization (at D14)
Cream of Example 1>excipient of Example 1>control
The present invention thus also extends to the use of a combination of sucralfate and of copper and zinc sulfates in the amounts and proportions already mentioned above, for the manufacture of a dermocosmetic composition for a regenerative, cicatrizing and/or antiinflammatory treatment of the skin.
| Number | Date | Country | Kind |
|---|---|---|---|
| FR01/06242 | May 2001 | FR | national |
| Number | Date | Country | |
|---|---|---|---|
| Parent | 10477259 | Apr 2004 | US |
| Child | 11786577 | Apr 2007 | US |
