MX2007006059A - Composition for removal of skin pigmentation. - Google Patents

Abstract

The present invention is related to skin creams in general, and specifically to a cream composition for removal of skin pigmentation acting as a topical melanin reducing agent for the treatment of hyperchromia, chloasma and acne, which gradually reduces the hyperpigmentation of skin and acne in a short term showing satisfactory results without side effects. The inventive composition is characterised in that it comprises tretinoine, clobetasol propionate, hydroquinone, and excipients with or without a sun screen agent; the invention quantitatively comprises 0.050 gr of tretinoine, 0.044 gr of clobetasol propionate, 4.100 gr of hydroquinone and 100 gr of c.b.p. excipient.

Description

COMPOSITION OF SKIN DETACHING CREAM FIELD OF THE INVENTION The present invention relates to skin creams in general, in particular with a skin-removing cream composition as topical demeaning agent for the treatment of hyperchromias, chloasma and acne, which gradually reduces hyperpigmetation of the skin.

BACKGROUND OF THE INVENTION Currently the cosmetic industry in terms of skin care has had a great development, so the topical creams for the face and body have made great progress not only in terms of cleaning and moisturizing the skin, but also in the prevention, treatment and elimination of hyperpigmentation of the skin due to the localized or generalized increase of melanin pigmentation whose causes can be endocrine, metabolic, by drugs; in conditions such as chloasma, residual hyperchromias of inflammatory processes, drug or chemical photosensitization, cosmetic, senile lentigo and freckles.

? For example, there are some topical creams on the market that try to eliminate hyperpigmentation of the skin, which base their composition on hydroquinone with some sunscreen agent; hydroquinone whose chemical name is 1,4-dihydroxybenzene, is also known as p-dioxobenzene, 1,4 p-benzenediol, hydroquinol, quinol or teequinol, is the substance used as an active ingredient for the production of skin whitening agents more common in the world. Within the health hazards, hydroquinone has been classified as "toxic" by direct ingestion, and as "noxious" by contact with eyes, skin and inhalation in large doses.

Acne treatment creams have also been developed that try to keep the exit orifices of the sebaceous glands free for the expulsion of the comedones.

However, existing creams on the market offer long-term results, since hydroquinone has difficulty penetrating the stratum corneum of the epidermis, delaying its arrival in the basal stratum of the epidermis where the melanocytes that cause hyperpigmentation are accumulated. makes treatments expensive and time consuming; In addition, the results are poor and generate secondary reactions such as irritation, burning, inflammation, etc.

Seeing the need to offer a highly effective topical application cream for the elimination of hyperpigmentation of the skin in a short period of time with satisfactory results and without secondary reactions, it was that the composition of skin-removing cream was developed, in accordance with the present description.

OBJECTIVES OF THE INVENTION The main objective of the present invention is to provide a novel composition of skin-removing cream for the elimination of hyperpigmentation of the skin and of acne, in the short term with satisfactory results and without secondary reactions.

Another objective of the invention is to allow said novel composition of skin-removing cream, which also removes the stained scars of the skin caused by acne.

A further objective of the present invention is to make available said novel composition of skin-removing cream, which also improves the clinical image of the skin.

Another object of the invention is to allow said composition Novelty of skin-removing cream, which also in the case of acne, prevents the formation of comedones and allows the expulsion of existing ones by keeping the pilo-sebaceous ducts free.

Still another objective of the invention is to allow said novel composition of skin-removing cream, which also stimulates the metabolic activity of the epidermis to allow a keratinization modulation, accelerate cell renewal and desquamation of cells of the stratum corneum.

And all those qualities and objectives that will become apparent when making a general and detailed description of the present invention supported by the illustrated modalities.

BRIEF DESCRIPTION OF THE INVENTION Generally speaking, the skin-removing cream according to the present invention has a composition Tretinoin, Clobetasol Propanate, Hydroquinone and an excipient, which may or may not include a sunscreen.

During the formulation of the cream, average concentrations were used both in the use of tretinoin and in the of hydroquinone at a dose of 2% with an effect is very slight and at concentrations greater than 5% with undesirable effects, so it was decided to use it at 3% and then at 4%, obtaining better results with the latter. In tretinoin, 0.050% was used with good results, clobetasol was used at therapeutic doses. Thus some formulations were used like the following. 1) Tretinoin 0.050%, Hydroquinone 4.1 gr., Clobetasol .044 gr. 2) Tretinoin 0.050%, Hydroquinone 3 gr., Clobetasol .044 gr.

Quantitatively, the preferred composition of the invention consists of every 100 mg. of cream: • Tretinoin 0.050 gr. · Clobetasol Propyanate equivalent to 0.044 gr. Hydroquinone 4.100 g r.; Y «Excipient c.b.p. 100 grs.

As is known, melanin is a pigment that is formed in the melanosomes of cells called melanocytes, these cells are found among the keratinocytes of the basal layer of the epidermis, which is the deepest of this; the melanocytes have dendrites or branches that disperse between the keratinocytes and lead their pigment (melanin) to the surface of the skin. Melanosomes synthesize melanin, by tyrosine, which is transformed to melanin, by means of an enzyme called tyrosinase Hydroquinone, are used to reduce hyperpigmentation of the skin, since it is a topical demelanizing, its topical application depletes melanin deposits and prevents the synthesis of melanin, inhibiting the tyrosinase enzyme that transforms tyrosine into melanin. Exposure to sunlight reduces the depigmenting effect of hydroquinone so that repigmentation can occur, so when using hydroquinone, exposure to the rays of the sun alone or using a sunscreen should be avoided.

As is known, the epidermis has several layers or layers, of which the most superficial is the corneal layer or stratum corneum. The stratum corneum is formed by rows of dead cells, which no longer have a nucleus and are dehydrated. These small cells contain keratin and fat inside; the tretinoin that is a keratolytic, breaks the keratin achieving a thinning of the stratum corneum and with this a more soft and radiant skin appearance, also accelerates the normal desquamation of the cells of the cornea layer, to achieve this, the tretinoin penetrates the cellular cytoplasm by means of a specific transporter, or CRABP, to which it is linked. The penetration in the nucleus is always done thanks to the transport by the CRABP and the acid vitamin A is linked, in the nucleus, to a specific receptor called Retinoic acid receptor or RAR, which allows its attachment to DNA at a specific site, thereby influencing the synthesis of proteins of the cell's cytoskeleton (keratin, etc.). At the epidermal level this allows a modulation of the q uera ti n ization, acceleration of cell renewal, acceleration of desquamation of corneal layer cells, etc.

Tretinoin It is used as an adjuvant in the treatment of acne, in acne, the glands are stimulated by androgens and increases their secretion of sebum .; at the same time, and due to an unknown cause, some sebaceous glands increase their follicular keratinization at the level of the infundibulum, which leads to an obstruction in the exit channel of the sebaceous gland. In this way, sebum begins to accumulate inside the gland; the process continues and the sebaceous gland grows accumulating this secretion of sebum to form a large sac called comedon. Tretinoin decreases the hyperkeratinization of the exit duct of the sebaceous gland, it is keratolytic, so it helps to keep the sebaceous glands free and also accelerates the release of old cells from the superficial layers, favoring the expulsion of comedones.

With regard to clobetasol, which is a topical corticosteroid which has a mainly anti-inflammatory effect, antipruritic and vasoconstrictor.

Thus, the three components consisting of Clobetasol Propyanate, Hydroquinone, and Tretinoin, exert their properties each, but as the main effect for which this cream is used is to remove the face or diminish areas of hyperpigmentation, this composition what it does is that tretinoin increases the penetration effect of hydroquinone, which will make the effect stronger and faster, the corticoid was added since tretinoin and hydroquinone have a common side effect that is irritation and with the Corticoid help is about limiting this effect.

The cream, according to the composition described above, has great advantages such as those mentioned below: Reduces areas of hyperpigmentation of the skin. Improves the clinical image of the skin. It helps to avoid new injuries and eliminate existing ones. In case of acne, avoid the formation of comedones and allow the expulsion of existing ones, as well as helping to keep sebaceous pilo ducts free, and with all this help the self-esteem of patients.

The invention has been sufficiently described so that a person with average skill in the art can reproduce and obtain the results that we mentioned in the present invention. However, any person skilled in the art who is competent in the present invention may be able to make modifications not described in the present application, however, if for the application of these modifications in a certain structure or in the manufacturing process thereof, the subject matter claimed in the following claims is required, said structures should be understood within the scope of the invention.

Claims (4)

R E I V I N D I C A C I O N S Having sufficiently described the invention, the content of the following claim clauses is claimed as property.

1. - A composition of skin-removing cream characterized by comprising tretinoin, propylate of clobetasol, hydroquinone and an excipient,

2. - A composition of skin-removing cream, according to claim 1, further characterized by comprising a sun blocking agent.

3. - A skin-removing cream composition, according to claim 1, characterized in that the hydroquinone is used in doses of 2% to 5%.

4. - A skin-removing cream composition, according to claim 1, characterized in that it quantitatively comprises: Tretinoin 0.050 gr. Clobetasol propionate equivalent to 0.044 gr. and Hydroquinone 4.100 g r.; Y »Excipient c.b.p. 100 grs. SUMMARY The present invention is related to skin creams in general, in particular with a skin-removing cream composition as topical demeaning agent for the treatment of hyperchromias, chloasma and acne, which gradually reduces the hyperpigmetation of the skin; whose objective is the elimination of hyperpigmentation of the skin and acne, in a short term with satisfactory results and without secondary reactions; which is characterized by comprising tretinoin, clobetasol propyanate, hydroquinone and an excipient, with or without some sun blocking agent and quantitatively comprises preferably 0.050 gr. of tretinoin, 0.044 gr. of propianate of clobetasol, 4.100 gr. of hydroquinone and excipient c.b.p. 100 grs.