Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2002-06-10
2004-04-06
Dodson, Shelley A. (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S065000, C424S404000
Reexamination Certificate
active
06716438
ABSTRACT:
BACKGROUND OF THE INVENTION
This invention relates to the use of antimicrobial agents in nanoscale form for the production of body deodorants.
Body deodorants, also known simply as deodorants, are formulations which counteract, mask or eliminate body odors. Body odors are formed by the action of skin bacteria on apocrine perspiration which results in the formation of unpleasant-smelling degradation products. Accordingly, deodorants contain active principles which act as antibacterial agents, enzyme inhibitors, odor absorbers or odor maskers.
Nanoscale materials are materials whose particle diameter in the direction of the largest dimension of the particles is less than 1000 nm (nanometers). In the present specification, the term “nanoparticulate” is used synonymously with the term “nanoscale”. Nanoscale active principles are described in the literature in particular as agents for achieving a controlled release of the active principle over a prolonged period. For example, WO 98/14174 describes nanoparticles for parenteral therapeutic use which consist of a pharmacologically active substance encapsulated in a shell of a biodegradable polymer. The document in question mentions inter alia antibacterial agents, such as chloramphenicol and vanomycin, and antimicrobial agents, such as penicillins and cephalosporins, as examples of pharmacologically active substances. Antimicrobial products containing nanoscale Schiff—s bases of aromatic aldehydes are known from DE 4402103 which describes the use of these products for the lasting antimicrobial finishing of textiles. Patent application CA 2,111,523 describes disinfectants which, besides other constituents, also contain surface-modified nanoparticulate antimicrobial agents. A disinfecting cleaner formulation is mentioned as an example. Patent application CA 2,111,522 describes compositions with a long-lasting germicidal effect which contain surface-modified nanoparticulate antimicrobial agents. Disinfectants for surface treatment which form permanent antimicrobial films on the treated surface are mentioned as applications of these compositions. However, there is nothing in the prior art to suggest that nanoparticulate antimicrobial agents can be used with advantage as active principles in body deodorants. Although it is known to the expert that antimicrobial agents are used, for example, both in surface disinfection and in body deodorants, the expert also knows that the form of application and the requirements in regard to strength of effect, action spectrum and the formulation of the active principles are so different in the various fields of application that the knowledge acquired in one field of application cannot obviously be applied to another field of application.
Because of their physiochemical properties and their own odors, the active principles used in body deodorants are often attended in practice by the problem that they only be incorporated in deodorant formulations with difficulty or in inadequate concentrations so that the formulations obtained show unsatisfactory antimicrobial activity. In addition, there is a demand among consumers for body deodorants which work with reduced concentrations of the active principle without any loss of deodorizing effect and hence offer physiological, economic and/or ecological advantages.
Accordingly, one problem addressed by the present invention was to enable body deodorants to be produced using antimicrobial agents which, due for example to their poor solubility or their strong odor, can only be conventionally incorporated in body deodorants with difficulty or in inadequate concentrations.
Another problem addressed by the invention was to provide body deodorants with sufficient antimicrobial activity for practical application and, at the same time, a reduced content of antimicrobial agents.
The problems stated above have been solved by the use of the antimicrobial agents in the form of nanoparticles with a particle diameter of 5 to 500 nm and preferably 10 to 150 nm for the production of body deodorants.
SUMMARY OF THE INVENTION
In a first embodiment, therefore, the present invention relates to the use of nanoscale antimicrobial agents with a particle diameter of 5 to 500 nm and preferably 10 to 150 nm for the production of body deodorants, more especially deodorizing aerosols, pump sprays, roll-ons and sticks. The use of the nanoscale antimicrobial agents is particularly suitable for the production of products which are required to show only bacteriostatic activity and not bactericidal activity.
It has surprisingly been found that the following advantages, for example, are achieved in this way:
a) The incorporation of antimicrobial agents in deodorant formulations is improved to the extent that lipophilic active principles can be incorporated more easily in aqueous formulations while hydrophilic active principles can be incorporated more easily in nonaqueous or low-water formulations.
b) the effectiveness of the active principles from the formulations is increased. This means that, for the same quantity by weight, the nanoparticulate active principle has a stronger antimicrobial effect than the same active principle in a larger particle size corresponding to the prior art.
c) In the case of active principles with a strong odor of their own, the odor can be weakened or even suppressed by surface modification of the nanoscale particles.
DETAILED DESCRIPTION OF THE INVENTION
Antibacterial agents with substantially selective activity against bacteria involved in the formation of odor-generating substances in bodily perspiration are particularly suitable for the use according to the invention. Where antimicrobial agents are used, it is important to ensure that the population of the bacteria concerned is merely controlled to prevent excessive growth (bacteriostatic effect) and not to destroy the bacteria completely (which would correspond to bactericidal activity).
Any substances active against gram-positive bacteria are particularly suitable as antimicrobial agents according to the invention. Substances active against Corynebacterium xerosis are particularly preferred. The active substances according to the invention include, for example,
4-hydroxybenzoic acid, its salts with alkali or alkaline earth metals or its esters with linear or branched C
1-10
alcohols,
N-(4-chlorophenyl)-N′-(3,4-dichlorophenyl)-urea,
2,4,4′-trichloro-2′-hydroxy diphenyl ether (triclosan),
4-chloro-3,5-dimethyl phenol,
2,2′-methylene-bis-(6-bromo-4-chlorophenol),
3-methyl-4-(1-methylethyl)-phenol,
2-benzyl-4-chlorophenol,
3-(4-chloropenoxy)-propane-1,2-diol,
3-iodo-2-propinyl butyl carbamate,
chlorohexidine,
3,4,4′-trichlorocarbanilide (TTC),
1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl )-2-(1H)-pyridinone, ethanolamine salt (1:1) (Octopirox)
antimicrobial perfumes such as, for example, thymol or menthol,
glycerol monolaurate (GML),
diglycerol monocaprate (DMC),
zinc salts such as, for example, zinc glycinate, zinc lactate or zinc phenol sulfonate,
phytosphingosines,
dodecane-1,2-diol,
undecylenic acid, its salts with alkali or alkaline earth metals or its esters with linear or branched C
1-10
alcohols,
salicylic acid-N-alkyl amides where the alkyl groups contain 1 to 22 carbon atoms and may be linear or branched and mixtures thereof.
Particularly preferred antimicrobial agents according to the invention are salicylic acid-N-octyl amide and/or salicylic acid-N-decyl amide, 2,4,4′-trichloro-2′-hydroxydiphenyl ether and antimicrobially active perfumes.
The nanoscale active principles consist of a discrete phase of the active principle with preferably at least one surface modifier adsorbed onto its surface. Particularly suitable surface modifiers are emulsifiers and/or protective colloids. The coating of the particles with emulsifiers and/or protective colloids prevents subsequent agglomeration of the particles.
Suitable emulsifiers are, for example, nonionic surfactants from at least one of the following groups:
(1) products of the addition of 2 to 30 moles of ethylene oxid
Banowski Bernhard
Glasl Johann
Leinen Hans-Theo
Roth Marcel
Schroeder Christine
Cognis Deutschland GmbH & Co. KG
Dodson Shelley A.
Drach John E.
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