Aqueous oral solution

This invention relates to an aqueous oral solution and especially to a 
peroxide-containing aqueous mouthwash or mouthrinse solution. 
It has long been recognized in the art that hydrogen peroxide and other 
peroxygen-containing agents are effective in curative and/or prophylactic 
treatments with respect to caries, dental plaque, gingivitis, 
periodontitis, mouth odor, tooth stains, recurrent aphthous ulcers, 
denture irritations, orthodontic appliance lesions, postextraction and 
postperiodontal surgery, traumatic oral lesions and mucosal infections, 
herpetic stomatitis and the like. Peroxide-containing agents in the oral 
cavity exert a chemomechanical action generating thousands of tiny oxygen 
bubbles produced by interaction with tissue and salivary enzymes. The 
swishing action of a mouthrinse enhances this inherent chemomechanical 
action. Such action has been recommended for delivery of other agents into 
infected gingival crevices. Peroxide mouthrinses prevent colonization and 
multiplication of anaerobic bacteria known to be associated with 
periodontal disease. 
It is however also known that most peroxy compounds such as hydrogen 
peroxide and metal peroxides such as magnesium peroxide in such oral 
compositions, by interaction with other common excipients therein, tend to 
be unstable in storage, continuously losing the capacity to release active 
or nascent oxygen over relatively short periods of time, and tend to 
diminish or destroy the desired function of such excipients. Among such 
excipients are flavors and coloring agents added to enhance the 
acceptability of the mouthrinse to those in need of an oral peroxidizing 
treatment. Numerous proposals have been made for solving the 
aforementioned problems, including encapsulating the peroxide compound 
and/or the peroxide-sensitive excipient, using more stable but more 
expensive peroxy compounds such as organic peroxides and peroxydiphosphate 
salts (e.g. the tetrapotassium salt), etc. 
It is an object of this invention to provide an oral solution which will 
not be subject to one or more of the aforementioned disadvantages and 
deficiencies. Another object of this invention is the provision of a 
foaming oxygenating mouthrinse in ready-to-use form having a pleasant 
flavor and/or color and enhanced stability in storage. Still another 
object of this invention is the provision of such a mouthrinse having a 
basis of the readily available, highly effective and economical hydrogen 
peroxide. Other objects and advantages will appear as the description 
proceeds.

The attainment of one or more of the above objects is made possible by this 
invention which comprises: 
an aqueous oral solution containing, approximately by weight: 
A. 1-3% of hydrogen peroxide, 
B. 3-15% of a polyhydric alcohol selected from the group consisting of 
glycerin and sorbitol, 
C. 3-10% of ethanol 
D. 0.5 to 3% of a nonionic water soluble polyoxyethylenated 
polyoxypropylene polyol surfactant, 
E. 0.3-2% of a nonionic surface active water soluble polyoxyethylenated 
monoester of sorbitol with C.sub.10-18 fatty acid, 
F. an effective sweetening amount of a sweetener compound, and 
G. an effective flavoring amount of a flavor selected from the group 
consisting of 
g1. wintergreen flavor containing methyl salicylate and menthol in a weight 
ratio of about 3:1 to 5:1, and 
g2. cinnamon flavor being a propylene glycol solution containing about 6-9% 
menthol, 32-38% cinnamic aldehyde and 6-9% clove oil. 
The aforementioned component G flavors have surprisingly been found to be 
satisfactorily stable and compatible in the presence of hydrogen peroxide, 
in contrast to other flavors, e.g. fruity flavors such as orange, lemon 
and lime, and even minty flavors other than the aforesaid g1 component 
wintergreen flavor, such as peppermint and spearmint. The other 
aforementioned components are similarly stable and compatible, in contrast 
to other usually known excipients. The critical combination of the 
aforementioned components A-G has been found to enable the attainment of 
the above-mentioned objects of this invention. Effective flavor amounts 
are as desired, typically ranging from about 0.05 to 1.0%, preferably 
about 0.1 to 0.5%, by weight in the solution. 
A coloring agent is also often desirable for enhanced appearance and 
acceptability, but must be carefully selected for compatibility with the 
other named components, particularly the hydrogen peroxide. Green coloring 
agents for example have been generally found to be unacceptable in this 
regard. FD & C Blue No. 1 and Red No. 40 have been found to satisfy the 
requirements of this invention, employed in effective coloring amounts as 
desired, typically in concentrations of about 0.0002 to 0.004% by weight 
in the solution. 
The preferred component F sweetener compound is saccharin, expecially 
sodium saccharin, but other known orally acceptable sweetener compounds 
may be employed, typically in concentrations of about 0.01 to 5 wt. %, 
such as xylitol, sodium cyclamate, perillartine, D-trypotophan, aspartame, 
dihydrochalcones and the like. 
The component D nonionic surfactant is well known, being a block polymer 
readily available under the Pluronic trademark. These surfactants are 
straight chain polymers containing a hydrophobic (water insoluble) 
polyoxypropylene moiety polyoxyethylenated at both ends with sufficient 
water-solubilizing oxyethylene groups to achieve the desired 
water-solubility, HLB (hydrophyliclipophylic balance) and dispersing 
surfactant activity. The solid F series of Pluronics are preferred in 
which the molecular weight of the polyoxypropylene moiety ranges from 
about 950 to 4,000 and constitutes about 20-30% of the molecule (i.e. 
80-70% polyoxyethylene in the molecule). Pluronic F 108 is especially 
preferred, in which the said hydrophobic moiety has a molecular weight of 
about 3250 and constitutes about 20% of the molecule. This surfactant has 
a molecular weight of about 14,000-16,000 and an HLB of about 28. 
The component E nonionic surfactant is also well known under the generic 
term "polysorbate," being readily available under the Tween and other 
trademarks. These surfactants are mixtures of C.sub.10-18 fatty acid 
esters of sorbitol (and sorbitol anhydrides), consisting predominantly of 
the monoester, condensed with about 10-30, preferably about 20, moles of 
ethyleneoxide. The fatty acid (aliphatic hydrocarbyl monocarboxylic acid) 
may be saturated or unsaturated, e.g. lauric, palmitic, stearic, oleic 
acids. Polysorbate 20(e.g. Tween 20) is especially preferred, commonly 
referred to as polyoxyethylene (20) sorbitan monolaurate. 
The surfactant components serve as solubilizing, dispersing, emulsifying, 
wetting and viscosity-control agents in combination, being especially 
effective to solubilize the flavor. 
Sorbitol is preferred as the component B polyhydric alcohol since although 
glycerin is sufficiently compatible with the other components, 
particularly the hydrogen peroxide, it interferes with at least 1 common 
method for analysis of the peroxide content. Component B serves as 
humectant, carrier (with the ethanol) and viscosity-control agent. 
The solutions of this invention may contain other functional agents such as 
anticaries agents and the like. Fluorine-providing anticaries compounds 
optionally present in these solutions may be partially or fully 
water-soluble. They are characterized by their ability to release 
fluorine-containing ions in water and by substantial freedom from reaction 
with other compounds of the oral preparation. Among these materials are 
inorganic fluoride salts, such as soluble alkali metal, alkaline earth 
metal and heavy metal salts, for example, sodium fluoride, potassium 
fluoride, ammonium fluoride, calcium fluoride, a copper fluoride such as 
cuprous fluoride, zinc fluoride, a tin fluoride such as stannic fluoride 
or stannous chlorofluoride, barium fluoride, sodium fluorosilicate, 
ammonium fluorosilicate, sodium florozirconate, sodium 
monofluorophosphate, aluminum mono- and di-fluorophosphate, and 
fluorinated sodium calcium pyrophosphate. Alkali metal and tin fluorides, 
such as sodium and stannous fluorides, sodium monofluorophosphate (MFP) 
and mixtures thereof, are preferred. 
The amount of the fluorine-providing compound is dependent to some extent 
upon the type of compound, its solubility, and the type of oral 
preparation, but it must be a nontoxic amount. An amount of such compound 
which releases a maximum of about 1% of fluoride ion by weight of the 
preparation is considered satisfactory. Any suitable minimum amount of 
such compound may be used, but it is preferable to employ sufficient 
compound to release about 0.005 to 1%, and preferably about 0.1% of 
fluoride ion. Typically, especially in the cases of MFP, alkali metal 
fluorides and stannous fluoride, this component is optionally present in 
these solutions in an amount of about 0.01 to 2 wt. %, preferably about 
0.05 to 1 wt. %, especially about 0.76 wt. %. 
The pH of the solutions of this invention generally range from about 4 to 
6, preferably about 5. Other common mouthrinse excipients may be included 
in these solutions such as thickeners, preservatives, and the like. The 
solutions of this invention may be prepared by judiciously mixing the 
various components for proper solubilization in the ethanol/polyhydric 
alcohol/water carrier medium, coloring agent and hydrogen peroxide in 
order being preferably added after the other components. 
The following examples of preferred embodiments of this invention are only 
illustrative. All amounts and proportions referred to herein and in the 
appended claims are by weight unless otherwise indicated. Typically, in 
preparing these exemplified formulations, the flavor is first added to the 
ethanol with agitation. The component D and E surfactants are then slowly 
sprinkled in with constant stirring, after which sufficient water is added 
slowly with stirring for abou ten minutes or until all the surfactants are 
dissolved and the solution is clear. The component B polyhydric alcohol is 
then added slowly with stirring followed by addition of the component F 
sweetener, preferably previously solubilized in a little water. Coloring 
agent, hydrogen peroxide (in the form of a 35% aqueous solution), and the 
remainder of the water are then added in succession. 
TABLE I 
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Examples (% w/v) 
1 2 3 4 5 6 
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Ethanol.sup.1 
4.75 4.75 4.75 
4.75 4.75 
4.75 
Wintergreen 
Flavor.sup.2 
0.22 0.22 0.22 0.22 
Cinnamon Flavor.sup.3 0.15 0.15 
Pluronic F 108 
1.0 1.0 1.0 1.0 1.0 1.0 
Polysorbate 20.sup.4 
0.6 0.6 0.6 0.6 0.6 0.6 
Sorbitol.sup.5 
10.5 10.5 10.5 
Glycerin 5.0 5.0 5.0 
Sodium saccharin 
0.04 0.04 0.04 0.04 0.04 0.04 
FD & C Blue .0004 .0004 
No. 1.sup.6 
FD & C Red .002 .002 
No. 40.sup.6 
Hydrogen peroxide .sup.7 
1.5 1.5 1.5 1.5 1.5 1.5 
Purified Water 
.rarw. qs. to 100 v. 
.fwdarw. 
.fwdarw. 
(USP Deionized) 
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.sup.1 in form of 95% soln 
.sup.2 80% methyl salicylate, 20% menthol 
.sup.3 7.5% menthol, 35% cinnamic aldehyde, 7.5% clove oil in propylene 
glycol soln. 
.sup.4 Tween 20polyoxyethylene (20) sorbitan monolaurate 
.sup.5 in form of 70% soln 
.sup.6 in form of 1% soln 
.sup.7 in form of 35% soln 
All the above-exemplified formulations represent satisfactory, pleasing, 
acceptable and effective foaming oxygenating mouthrinses having 
satisfactory storage stability with respect to flavor, color, appearance, 
taste, peroxy content and the like. 
This invention has been disclosed with respect to preferred embodiments, 
and various modifications and variations thereof obvious to those skilled 
in the art are to be included within the spirit and purview of this 
application and the scope of the appended claims.