Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2000-09-11
2002-06-25
Dees, Jose′ G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
Reexamination Certificate
active
06410037
ABSTRACT:
BACKGROUND OF THE INVENTION
The present invention relates to compositions for blocking histamine release by mastocytes.
Degranulation of cutaneous mastocytes leads to the release of several mediators, including histamine. Histamine is responsible for different reactions, such as pruritus (itching). Histamine release can be amplified or inhibited by several substances. Histamine inhibitors can be used as active compounds in medicaments.
Glycine is an amino acid occurring naturally in most animal species. It inhibits histamine release by mastocytes. The effect of glycine on mastocyte degranulation is described, for instance, in M. Paubert-Braquet, G. Lefranqois, S. Picquot, D. Rod,
Thérapeutique,
95, 1992, 2. A decrease in the amount of mediators released into the extra-cellular environment (e.g. histamine) has been observed, resulting from the inhibition of mastocyte degranulation.
The use of glycine for treating dermatological disorders which involve mastocyte degranulation is furthermore described in A. Siboulet, J M Bohbot,
Gyn. Obs.,
1987, 166 by means of a study on pruriti in the genital area.
For a certain types of pruritus, such as allergic pruritus, the stimulus responsible for the degranulation of the mastocytes is a modification of the mastocyte membrane structure by a bipolar antigen. The antigen is fixed on two IgE which are nonspecifically attached to the cell membrane by their Fc extremities.
For many other types of pruritus, the mechanisms are still obscure. The stimuli maybe in fact of different nature, both chemical and physical, and may involve the presence of a neurotransmitter such as substance P. This substance, present naturally in the mammalian body, is capable of initiating mastocyte degranulation. Pruritus can be therefore treated in different ways, e.g. by blocking message transmission from the central nervous system, by blocking the stimulus and/or by inhibiting the degranulation process.
Pantothenic acid, which is also known as D(+) N-(2,4-dihydroxy-3,3-dimethylbutyryl)&bgr;-alanine, is a member of the B complex vitamins and is sometimes referred to as vitamin B
5
.
Pantothenic acid plays a key role in cellular metabolism. After incorporation into coenzyme A (CoA), it participates in the synthesis of fatty acids, cholesterol and sterols. Through its participation in the Krebs cycle, coenzyme CoA is also instrumental in the generation of energy by the cells. Pantothenic acid is hence essential for epithelial regeneration and development in the event of skin damage when a high rate of lipid synthesis and cellular renewal is needed.
Dexpanthenol, the alcohol of pantothenic acid, is well absorbed by the skin. After penetration in the skin it is rapidly transformed into pantothenic acid. Dexpanthenol has therefore been used for many years in topical products such as ointments and creams. The clinical effectiveness of the topical application of dexpanthenol in promoting wound healing has been confirmed by several studies in cases of wounds, burns, cracked nipples, ulcers, and bedsores (e.g. P. Girard, A. Béraud, C. Goujon, A. Sirvent, J-L Foyatier, B. Alleaume, R. de Bony,
Les Nouvelles Dermatologiques,
17, 1998, pp. 559-570).
SUMMARY OF THE INVENTION
It has been found that compositions containing pantothenic acid and/or its derivatives can be used for treating pruritic conditions. It has been observed that pantothenic acid and/or its derivatives inhibit mastocyte degranulation, thus diminishing the amount of mediators released into the extra-cellular environment. Pantothenic acid and/or its derivatives can be therefore used for all dermatological disorders which involve mastocyte degranulation, such as atopic dermatitis, psoriasis, contact eczema, skin allergies, skin inflammation due to insect bites, skin allergies, senile pruritus, etc.
It has also been found that the inhibition effect on mastocyte degranulation is strongly increased if pantothenic acid and/or its derivatives are combined with glycine. A synergistic effect in the inhibition by the mixture in comparison with the single compounds is therefore observed.
Therefore, this invention is directed to a method of treating a dermatological disorder related to mastocyte degranulation (such as atopic dermatitis, psoriasis, contact eczema, skin allergies, skin inflammation due to insect bites, skin allergies, senile pruritus) which comprises administering pantothenic acid or a derivative thereof in an amount effective to alleviate the dermatological disorder.
This invention is also directed to compositions comprising pantothenic acid or a derivative thereof and glycine. These compositions are synergistic in their effects on dermatological disorders. Methods of treating dermatological disorders with these compositions are another part of this invention. The synergistic effect obtained by mixing the above compounds together leads to several important advantages. For the same effect, it is possible to reduce the concentrations of the active compounds, thus decreasing the risk of intolerance for the patients. A lower concentration of the active compounds lead also to lower manufacturing costs and, therefore, to lower selling prices of the compositions. With the same therapeutic effect, the compositions according to the present invention are therefore more tolerable and more competitive than the conventional ones.
In preferred methods and compositions of the present invention, pantothenic acid and/or its derivatives are used in an amount from 0.1% to 10%, inclusive, in other words varying between 0.1 and 10%, of total weight of the pharmaceutical and/or cosmetic composition and, preferably, in an amount from 2% to 5% inclusive, in other words varying between 2 and 5%, of the total weight. All ranges given herein are considered inclusive of each end of the range.
DETAILED DESCRIPTION OF THE INVENTION
This invention is directed to a method of treating a dermatological disorder related to mastocyte degranulation (such as atopic dermatitis, psoriasis, contact eczema, skin allergies, skin inflammation due to insect bites, skin allergies, senile pruritus) which comprises administering pantothenic acid or a derivative thereof in an amount effective to alleviate the dermatological disorder. Preferably the effective amount of pantothenic acid or a derivative thereof is from 0.1% to 10% (more preferably from 2% to 5%) of the total weight of the composition in which it is administered.
This invention is also directed to a method of treating a dermatological disorder related to mastocyte degranulation (such as atopic dermatitis, psoriasis, contact eczema, skin allergies, skin inflammation due to insect bites, skin allergies, senile pruritus) which comprises administering pantothenic acid or a derivative thereof and glycine in an amount effective to alleviate the dermatological disorder. Preferably the ratio of pantothenic acid to glycine varies from 0.13 to 13.3 wt/wt. in the composition in which they are administered. In one embodiment, the effective amounts of pantothenic acid or a derivative thereof and the glycine are each from 0.1% and 10% (preferably from 2% and 5%) of the total weight of the composition in which they are administered. In this embodiment, the ratio of the two components may be from 0.13 to 13.3 as above.
By “alleviate” is meant remove or reduce symptoms in the humans or animals to which the compositions of this invention are administered. For example a perceived reduction in itching constitutes alleviation, as does reduction in rash area, or fading of color. Reduction in histamine production as measured by any conventional assay is another example of alleviation.
This invention is further directed to a pharmaceutical composition comprising pantothenic acid or a derivative thereof, glycine, and a pharmaceutically acceptable carrier, and a composition for topical application comprising pantothenic acid or a derivative thereof, glycine, and an acceptable carrier for topical application. In each composition, it is preferred that the ratio of pantothenic acid or a pantothenic acid derivat
De Bony Raymond
Gooris Eric
Dawson Arthur D.
Dees Jose′ G.
George Konata M.
Johnston George W.
Rocha-Tramaloni Patricia
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