Mouthrinse

Drug – bio-affecting and body treating compositions – Dentifrices

Patent

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Details

424 48, 424435, A61K 716

Patent

active

058855521

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/US92/11083 filed Jan. 19, 1993.
This invention relates to a mouthrinse and to its use.
It is well known to use a mouthrinse composition to provide various orally active materials in the mouth cavity. There is a problem, however, in maintaining an effective concentration of these materials in the mouth over a period of time because, after use of the mouthrinse, the normal flushing of gums and teeth by saliva tends to wash away the deposited mouthrinse materials. Although some highly charged cation materials do adsorb preferentially on to the buccal mucosa and are slowly released therefrom, many other mouthrinse materials become diluted and are removed from the mouth much more quickly than is desirable.
We have now found a way in which this problem can be reduced or eliminated. According to the present invention, we provide in the mouthrinse a material which, when in the mouth, can be gelled to form a water-insoluble thin coating from which the active material is slowly released over a period of time. In this way, effective concentrations of active material can be maintained in the mouth for extended periods after use of the mouthrinse.
According to the present invention, there is provided a three component mouthrinse which comprises (a) a mouthrinse active material, (b) a polymeric material which can be gelled when in the mouth, and (c) means for gelling the polymeric material in the mouth, to form a water-insoluble gel in the mouth from which gel the active material is slowly released over a period of time, wherein each of components (a), (b) and (c) is in aqueous solution for rinsing the mouth.
The invention also includes a method of depositing an active material for slow release in the mouth, which comprises rinsing the mouth with a mouthrinse according to the invention, to form in the mouth a water-insoluble gel containing the active material.
The mouthrinses of the invention have three essential components (a), (b) and (c) as defined above, and these components are each in either aqueous solution or aqueous mixtures with other safe solvents such as ethanol, so that they are suitable for rinsing the mouth. In one embodiment of the invention, all three components can be in admixture in a single solution, whereas in other embodiments the components may be used separately or in sub-mixtures in which case the mouthrinse will comprise two, or three individual solutions to be used to rinse the mouth sequentially. The preferred mouthrinses of the invention consist of a single aqueous solution containing all three components.
Component (a) is an active material for slow release into the oral cavity. There are many such active materials which are conventionally administered by mouthrinses, among which materials are, for example, bactericides, anti-inflammatories, remineralising solutions, fluorides, desensitisers, antifungal agents, salivary gland stimulators, deodorants and antibiotics. In accordance with the invention, this mouthrinse active material (component (a)) becomes encapsulated or trapped within the gel which forms in the mouth, and is released only slowly therefrom to maintain an effective concentration of the material in the mouth over a considerable period of time following use of the mouthrinse.
The precise nature of components (b) and (c) will depend on whether the mouthrinse is to be in the form of a single solution (containing all three components) or whether it is to consist of two (or three) separate solutions. The preferred arrangement is the single solution and this will now be described. In a most preferred embodiment of the single solution mouthrinse of the invention, component (b) is a polymer which gels in the presence of dissolved calcium ions, and component (c) is an etchant polyacid capable of releasing calcium ions into solution when in contact with teeth. In use of this embodiment of mouthrinse of the invention, the aqueous solution first wets a tooth surface, and the acid dissolves any pellicle present and then releases calcium ions from the enamel

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patent: 5401723 (1995-03-01), Gaffar et al.

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