Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Biocides; animal or insect repellents or attractants
Reexamination Certificate
1998-04-14
2002-12-31
Levy, Neil S. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Biocides; animal or insect repellents or attractants
C424S401000, C424S405000, C424S406000, C424S450000, C424S078020, C424S078030, C523S122000
Reexamination Certificate
active
06500446
ABSTRACT:
BACKGROUND OF THE INVENTION
The invention relates to compositions for improving the activity or intrinsic activity (activities) of an active molecule by persistence and maintenance (or increase) of this (these) activity (activities), for long periods of time, said compositions being used by application onto living or inert surfaces.
These compositions are usable for example in the fields of human or veterinary medicine, especially in dermatology or cosmetics; in human or veterinary hygiene; in domestic products; in products for use in the environment, especially such as plant treatment products (in particular treatment of their aerial part), and in the fight against insects.
These compositions comprise at least one cationic polymer and at least one active molecule contained in at least one micro or nanoparticulate vector.
Several families of products are known in dermatology and in cosmetology which are presented in many forms and which are used by application onto the skin or the hair in man, and onto the skin and hair of animals, which act:
to wash with rinsing, for example shampoos, liquid soaps, syndets (synthetic detergents),
to clean without rinsing, for example dry shampoos, milks, lotions,
to treat or to embellish, for example lotions, gels, milks, creams, ointments, pressurised or mechanical sprays, sticks.
In every case, these products must bring about, after their use, with or without rinsing, a beneficial embellishing and/or treating action. Hitherto, every preparation has a cosmetic or dermatological activity which appears just after the treatment, but without persistence with time.
Domestic or environmental products are also known which are presented in many forms, solutions or suspensions, creams, gels, pressurised or mechanical sprays, which have various uses such as, for example:
the cleaning of surfaces, objects or linen (detergent products),
the embellishment of surfaces, optionally plant surfaces (polishing or glossing products),
the pest control of premises or plants, with, amongst others, adherence on insects,
the disinfection of surfaces,
plant protection products.
Furthermore, in order to maintain the activity over a long period of time, it is necessary to increase the amounts of active molecules which in many cases leads to the acceptability threshold being surpassed:
in dermatology and cosmetology, skin problems are observed, i.e. the appearance of adverse reactions, irritations, redness, itching, lesions;
in hygiene and during a use in the environment, problems of inconvenience for the living beings present during the use or after the use of the product, a degradation of the surfaces, or bums for the plants, are observed for example.
Such a increase also leads to technical difficulties in introducing these large amounts of active molecules into the formulations.
Compositions having treating and/or embellishing actions have now been developed for these types of products which last over long periods of time so as to prevent the repetition of the applications, (this repetition causing harmful effects while maintaining a treating cover), in particular without a break between the applications recommended in the regimen of use.
SUMMARY OF THE INVENTION
The invention therefore relates to compositions which comprise at least one cationic polymer and at least one active molecule contained in at least one micro or nanoparticulate vector, by virtue of which compositions the drawbacks described above as far as the persistence of the activity is concerned may be avoided.
In the rest of the description, the term <<polymer>> comprises homopolymers as well as copolymers.
In a surprising way, the combination of at least one cationic polymer and at least one active molecule in a micro or nanoparticulate vector gives rise to a synergy between said polymer and the micro or nanoparticles which enables not having to increase the amounts of actives, while maintaining the activity over a long period of time.
In particular, this synergistic effect is observed on the surface of the skin and at the contact with the hair over longer periods of time than those provided by existing vectorial systems, without having to increase the amount of the actives.
Further, it has been established that the choice of the micro or nanoparticulate vector, of the cationic polymer, and more exactly, the combination of the two could modulate the activity of the composition; each combination must of course be the subject of particular studies in order to determine the amounts of actives to be used in the vectors, and in order to determine the period of activity.
These compositions are stable in storage, and present excellent treating and/or embellishing properties. They are also better tolerated and have a better harmlessness vis-à-vis the skin, the hair and the eyes in cosmetology and dermatology, as well as vis-à-vis the environment.
DETAILED DESCRIPTION OF THE INVENTION
The compositions according to the invention are characterised by the fact that they comprise, in a medium acceptable for a pharmaceutical use, in particular a dermatological, veterinary, cosmetic, or hygiene use, or for domestic applications or applications in the environment:
a) 0.001 to 5%, by weight of the total weight of the composition, of a cationic polymer, or of a mixture of cationic polymers;
b) 0.5 to 50%, by weight of the total weight of the microparticle composition or nanoparticle composition which contain one or more active molecules.
The compositions according to the invention can be used in any application set forth above, and in particular for a topical pharmaceutical or veterinary treatment of human skin or hair, or of animal skin or hair, or for eliminating parasites.
The cationic polymers used in accordance with the present invention, are selected for example from:
quaternised polymers or copolymers, such as, for example, quaternised derivatives of polyvinylpyrrolidone (PVP); quaternised copolymers of PVP and hydrophilic polymers (urethane, acrylate, etc.), in particular the copolymers of PVP, dimethylaminoethyl-methacrylate and polyurethane (marketed under the name Aquamere C by the company Hydromer Inc.);
ammonium salts of synthetic polymers or copolymers known under the designation “Polyquaternium” such as described in the International Cosmetic Ingredient Dictionary published by the <<Cosmetic, Toiletry and Fragance Association>>, (C.T.F.A.);
cationic silicones;
cationic polysaccharides of natural, biotechnological or synthetic origin, naturally cationic or quaternised, such as, for example, modified guar gums, chitosan or modified chitosans and their salts; celluloses, modified celluloses and their derivatives, such as, for example, sodium carboxymethylcellulose; chitin derivatives;
polyamine derivatives, optionally substituted with polyethylene glycol chains;
polyaminoacids under pH conditions in which they are cationic;
polyethyleneimine.
Preferably, from the cationic polysaccharide family, chitosan and its derivatives will be used. Chitosan is a polyglucosamine which is obtained by deacetylation of chitin, several uses of which have been proposed in cosmetology and dermatology. In the case of aqueous solutions, chitosan is used in particular in the form of its soluble salts with organic acids or anionic surfactants.
The polysaccharides are defined in greater detail in numerous books. The book by R. A. A. Muzzarelli, “The Polysaccharides”, (1985) Academic-Press, may be referred to in particular.
In a preferred aspect, the polysaccharides usable according to the invention can be selected from chitosan or modified chitosans such as N-acyl chitosans, N-carboxyalkyl chitosans, N-carboxyacyl chitosans, O-carboxyalkyl chitosans, deoxyglycit-1-yl chitosans, hydroxyalkyl chitosans, or salts thereof.
More particularly, the pyrrolidone carboxylic acid salt of chitosan (chitosan PCA), the glycolic acid salt of chitosan (chitosan glycolate), the lactic acid salt of chitosan (chitosan lactate), the monosuccinamide of chitosan (chitosan monosuccinamide or chitosanide) will be used for example
Derrieu Guy
Karst Christian
Monginoux Patricia
Pougnas Jean-Luc
Dennison, Schultz & Dougherty
Levy Neil S.
Virbac
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