European Patent Application A61K 7/26, A61K 7/16: Composition of Mouth Spray
European Patent Application A61K 7/26, A61K 7/16: Composition of Mouth Spray
European Patent Application A61K 7/26, A61K 7/16: Composition of Mouth Spray
(19)
*EP001013261A1*
(11)
EP 1 013 261 A1
(12)
(43) Date of publication:
(72) Inventors:
Maki, Hisako, Mitsui & Co. Ltd.
Tokyo 100-0004 (JP)
(54)
EP 1 013 261 A1
(57)
A composition of mouth spray is provided,
which comprises tea-polyphenol, 1-menthol and/or
1-carvone. A concentration of the tea-polyphenol in the
composition of mouth spray is preferably from 10 to
20000 ppm. The tea-polyphenol is preferably at least
one member selected from the group containing (+) -catechin, (-) -catechin, (+) -gallocatechin, (+) -epigallocatechin, (+) -gallocatechin gallate, (+) -epigallocatechin
gallate, (-) -epicatechin, (-)-epicatechin gallate, (-) -catechin gallate, (-) -epigallocatechin, (-) -gallocatechin, (-)
EP 1 013 261 A1
Description
BACKGROUND OF THE INVENTION
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10
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[0006] It is therefore an object of the present invention to solve the above-mentioned problem and to provide a
composition of mouth spray that has good durability with respect to the masking of bad breath and the refreshing effect
and also has the pleasant aftertaste.
[0007] In order to accomplish the above object, a rst aspect of the present invention is to provide a composition of
mouth spray comprising tea-polyphenol, 1-menthol and/or 1-carvone.
[0008] A second aspect of the present invention is to provide the composition of mouth spray, wherein a concentration
of the tea-polyphenol is from 10 to 20000 ppm.
[0009] A third aspect of the present invention is to provide the composition of mouth spray, wherein the tea-polyphenol
is at least one member selected from the group containing (+) - catechin, (-) - catechin, (+) - gallocatechin, (+) - epigallocatechin, (+) - gallocatechin gallate, (+) - epigallocatechin gallate, (-) - epicatechin, (-) - epicatechin gallate, (-) - catechin
gallate, (-) - epigallocatechin, (-) - gallocatechin, (-) - epigallocatechin gallate, (-) - gallocatechin gallate, theaavin monogallate A, theaavin monogallate B, theaavin digallate, and free theaavin.
[0010] The composition of mouth spray according to the present invention keeps a long duration of masking bad
breath and of refreshing effect signicantly. Moreover, the composition of mouth spray produces effects such as improvement in a refreshing feeling and pleasant aftertaste, cancellation of throat unpleasantness, and other useful effects
that the tea-polyphenol has in nature.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
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[0011] The composition of mouth spray according to the present invention is not only used to prevent such as bad
breath or discomfort from causing, but also applied to a variety of purposes in the eld of food, non-pharmaceutical
and pharmaceutical industries and the like. An amount of one spraying is normally 10 to 500 microliters.
[0012] The 1-menthol used in the present invention may be a synthetic or natural product and may include an isomer
thereof. 1-menthol is a main constituent of mint and peppermint oils that may be used as they are in the present
invention. The 1-carvone used in the present invention may also be a synthetic or natural product and may include an
isomer thereof. A spearmint oil having 1-carvone as a main constituent thereof may also be used.
[0013] A concentration of 1-menthol or 1-carvone in the composition of mouth spray according to the present invention is not particularly limited as long as the masking of bad breath and refreshing effect can be obtained, but the
EP 1 013 261 A1
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concentration of either the single component or the mixture thereof is preferably from 100 to 10000 ppm. When the
concentration is lower than 100 ppm, a refreshment due to 1-menthol or 1-carvone is hard to obtain. On the other hand,
when the concentration is higher than 10000 ppm, the suitability to taste is inferior caused by too much stimulation
and bitterness.
[0014] The ingredient of a tea used in the present invention is such as leaf, stem, xylem, root and nut obtained from
a camellia sinensis or a mixture thereof, but is usually a tea leaf for drinking. The tea leaf for drinking includes a
fermented tea such as black tea and puahru tea, half-fermented tea such as oolong tea and paochoncha, non-fermented
tea such as green tea, kamairi (infused in a pot) green tea and houjicha, and a mixture thereof.
[0015] The tea-polyphenol used in the present invention may be a tea itself contained tea-polyphenol, an extract
obtained by extraction from tea using such as water, hot water, organic solvent and water-containing organic solvent,
or a mixture thereof. Such an extract may further be rened to a desirable extent by means of an organic solvent
fractionation method or by using an adsorptive resin. These methods have been described in Japanese Patent Publications No. H1-44234, H2-12474 and H2-22755, and in Japanese Patent Applications Laid-Open No. H4-20589,
H5-260907 and H8-109178.
[0016] The tea-polyphenol used in the present invention may be such as (+) - catechin, (-) - catechin, (+) - gallocatechin, (+) - epigallocatechin, (+) - gallocatechin gallate, (+) - epigallocatechin gallate, (-) - epicatechin, (-) - epicatechin
gallate, (-) - catechin gallate, (-) - epigallocatechin, (-) - gallocatechin, (-) - epigallocatechin gallate, (-) - gallocatechin
gallate, theaavin monogallate A, theaavin monogallate B, theaavin digallate, and free theaavin. Selecting from the
above group, either the single tea-polyphenol or a mixture of a plurality of the tea-polyphenol may be used. A main
constituent of a tea-polyphenol originally from the green tea is (-) - epigallocatechin gallate.
[0017] In the present invention, an amount of the tea-polyphenol is dened as an amount of tannin determined by
an ofcial method of tannin analysis using iron tartrate.
[0018] A concentration of the tea-polyphenol used in the present invention is preferably from 10 to 20000 ppm as
the sole tea-polyphenol or the mixture thereof, and more preferably from 50 to 10000 ppm. The desired effect cannot
be obtained when the concentration of the tea-polyphenol is lower than 10 ppm, while the suitability to taste becomes
inferior caused by giving sour and bitterness when the concentration is higher than 20000ppm.
[0019] The composition of mouth spray according to the present invention keeps a long duration of masking bad
breath and of refreshing effect signicantly. Furthermore, the composition of mouth spray according to the present
invention has newly-found effects such as cancellation of throat unpleasantness and pleasant aftertaste, and also has
a variety of useful effects that the tea-polyphenol has in nature.
[0020] Corresponding to a purpose of use, the composition of mouth spray according to the present invention may
contain various additives such as efcacious ingredient, sweetening, solvent, humectant, solubilizer, surface active
agent, emulsier, antioxidant, pH modier, spice, coloring agent, preservative, buffer, and stabilizer.
[0021] For example, the efcacious ingredient may be such as sodium uoride, sodium monouorophosphate, tin
uoride, cetylpyridinium chloride, chlorhexyzine gluconate, isopropylmethylphenol, iodine, potassium iodide, povidoneiodine, hinokitiol, tranexamic acid, sodium azulene sulfonate, cuppor chlorophyllin sodium, and vitamin E. The sweetening may be monosaccharide or diasaccharide such as cane sugar, grape sugar, fruit sugar and isomerized sugar,
sugar alcohol such as xylitol, erythritol, sorbitol and mannitol, aspartame, stevioside, and saccharin sodium. The humectant may be polyhydric alcohol such as glycerin, polyethylene glycol, and propylene glycol. The solvent may be
such as ethanol. The solubilizer may be non-ionic surface-active agent such as polyoxyethylene stiffened castor oil
and polyoxyethylene polyoxypropylene glycol. The preservative may be such as benzoic acid, sodium benzoate,
paraoxybenzoate ester group, sorbic acid, potassium sorbate, and decomposed pectin. The antioxidant may be such
as ascorbic acid, and erysorbic acid. The pH modier may be such as citric acid, phosphate, malic acid, and sodium
hydrogencarbonate. The emulsier may be such as glycerin fatty acid ester, cane sugar fatty acid ester, sorbitan fatty
acid ester, and soybean saponin.
[0022] Prescription examples from 1 to 4 of the composition of mouth spray according to the present invention are
shown in the following Tables from 1 to 4, respectively. In the tables, polyphenon 60 and polyphenon RB are brand
name of products manufactured by Mistui Norin Co., Ltd.
Table 1
polyphenon 60 (contained 60 wt% or more of green tea-polyphenol, manufactured by Mistui Norin
Co., Ltd.)
0.8 wt%
1-menthol
0.5 wt%
ethanol
30 wt%
2.0 wt%
EP 1 013 261 A1
Table 1 (continued)
saccharin sodium
0.1 wt%
rened water
remainder
Table 2
10
0.5 wt%
0.2 wt%
propylene glycol
20 wt%
glycerin
25 wt%
2.0 wt%
spice
1.5 wt%
rened water
remainder
15
20
Table 3
polyphenon 60 (contained 60 wt% or more of green tea-polyphenol, manufactured by Mistui Norin
Co., Ltd.)
0.05 wt%
0.1 wt%
xylitol
20 wt%
1.5 wt%
rened water
remainder
25
30
Table 4
35
0.01 wt%
1-menthol
0.3 wt%
0.01 wt%
ethanol
20 wt%
sorbitol
30 wt%
2.0 wt%
rened water
remainder
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EXAMPLES
[0023] The composition of mouth spray according to the present invention will now be described by the following
examples that by no means limit the scope of the invention.
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EP 1 013 261 A1
was from 100 to 10000 ppm.
Table 5
1-menthol
ethanol
35 wt%
3 wt%
rened water
remainder
10
Table 6
concentration of 1 - menthol (ppm)
15
20
25
30
35
refreshing effect
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11
100
43
61
500
66
73
1000
80
91
2000
87
96
5000
90
84
10000
89
42
20000
25
[0026] Polyphenon 100 (brand name of a product manufactured by Mistui Norin Co., Ltd.), active ingredients of which
are shown in Table 7, was used as a source of green tea-polyphenol. Mouth spray solutions containing green teapolyphenol of seven kinds of concentrations were prepared according to a prescription described in Table 8, then a
sensuous test (B-type) by 10 panelists was conducted. The test (B-type) was performed to evaluate degrees of sour
and bitterness of the sample solutions by marking scores out of 3 for each panelist, and then scores answered by the
10 panelists were summed up (full marks 30). The each score out of 3 corresponds as follows: not felt sour and bitterness 3, felt to some extent 2, felt considerably 1, felt very strongly 0.
[0027] Then, a sensuous test (A-type) by 10 panelists was conducted in a similar way as described above.
[0028] These results are shown together in Table 9.
Table 7
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1.4
(-) - epigallocatechin
17.6
(-) - epicatechin
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5.8
53.9
12.5
total
91.2
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Table 8
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green tea-polyphenol
ethanol
35 wt%
3 wt%
rened water
remainder
EP 1 013 261 A1
Table 9
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20
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refreshing effect
30
10
29
50
25
13
100
20
20
1000
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10000
22
20000
[0029] Polyphenon TF (brand name of a product manufactured by Mistui Norin Co., Ltd.), active ingredients of which
are shown in Table 10, was used as a source of black tea-polyphenol. Mouth spray solutions containing black teapolyphenol of seven kinds of concentrations were prepared according to the same prescription described in Table 8
except that green tea-polyphenol is replaced by black tea-polyphenol, and sensuous tests (A-type and B-type) by 10
panelists were conducted. Both the preparation and the tests were carried out in a similar way to the green tea-polyphenol case as described above. The results are shown in Table 11.
[0030] The results shown in tables 9 and 11 reveal as follows: (1) the masking of bad breath that seems to be due
to the green or black tea-polyphenol was positively observed, however, (2) the degree of sore and bitterness was
signicant when the tea-polyphenol concentration was 1000 ppm or higher, and (3) the refreshing effect was hardly
observed.
Table 10
active ingredient
free theaavin
6.0
theaavin monogallate A
13.4
theaavin monogallate B
11.7
theaavin digallate
19.5
(+) -catechin
0.2
(-) - epicatechin
1.1
2.8
0.6
2.3
theaavin isomer
2.4
total
60
30
35
40
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Table 11
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refreshing effect
30
10
30
50
27
11
100
24
19
1000
11
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EP 1 013 261 A1
Table 11 (continued)
concentration of black teapolyphenol (ppm)
5
refreshing effect
10000
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20000
Example No. 1
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[0031] Mouth spray solutions containing 1-menthol of three kinds of concentrations and green tea-polyphenol
(polyphenon 100, containing active ingredients shown in Table 7) of six kinds of concentrations were prepared according
to a prescription described in Table 12 and a sensuous test (C-type) by 15 panelists was conducted. The test (C-type)
includes (1) duration of masking of bad breath and refreshing effect and (2) improvement effect on aftertaste due to
refreshed and clean feelings. In the test (1), placebos that include no green tea-polyphenol were prepared besides the
sample solutions and a number of panelists who answered that the sample was better than the corresponding placebo
with respect to the duration of masking of bad breath and refreshing effect was counted (full marks 15). In the test (2),
a number of panelists who answered that the sample had the improvement effect on aftertaste was counted (full marks
15). As for the improvement effect on aftertaste, the sample solution was evaluated to have no such an improvement
effect if each panelist felt unpleasant sore or bitterness.
[0032] The result is shown in Tables 13 to 15.
Table 12
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1- menthol
green tea-polyphenol
ethanol
35 wt%
3 wt%
rened water
remainder
30
Table 13
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concentration of
1-menthol (ppm)
concentration of
green teapolyphenol (ppm)
duration of masking
of bad breath
duration of
refreshing effect
improvement effect
on aftertaste
500
10
12
500
50
11
14
500
100
13
12
14
500
1000
14
15
13
500
10000
14
13
11
500
20000
12
Table 14
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concentration of
1-menthol (ppm)
concentration of
green teapolyphenol (ppm)
duration of masking
of bad breath
duration of
refreshing effect
improvement effect
on aftertaste
2000
10
12
2000
50
11
14
2000
100
12
11
14
2000
1000
14
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EP 1 013 261 A1
Table 14 (continued)
concentration of
1-menthol (ppm)
5
concentration of
green teapolyphenol (ppm)
duration of masking
of bad breath
10000
15
14
11
2000
20000
11
Table 15
concentration of
1-menthol (ppm)
20
25
improvement effect
on aftertaste
2000
10
15
duration of
refreshing effect
concentration of
green teapolyphenol (ppm)
duration of masking
of bad breath
duration of
refreshing effect
improvement effect
on aftertaste
5000
10
11
5000
50
10
13
5000
100
12
13
14
5000
1000
14
15
15
5000
10000
15
14
12
5000
20000
13
[0033] The result shown in tables 13 to 15 reveals as follows: (1) by using 1-menthol together with green tea-polyphenol that gives poor masking of bad breath and refreshing effect when used solely, obtained were a signicantly long
duration of masking of bad breath and refreshing effect as well as a signicant improvement effect on aftertaste compared to single usage of 1-menthol, and (2) sour and bitterness due to the green tea-polyphenol were masked by using
1-menthol together with the green tea-polyphenol.
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Example No. 2
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[0034] Mouth spray solutions containing 1 - menthol (concentration of 2000 ppm) and black tea-polyphenol (polyphenon TF, active ingredients shown in Table 10) of six kinds of concentrations were prepared according to a prescription
described in Table 16 and a sensuous test (C-type) by 15 panelists was conducted. The test was carried out in a similar
way to the green tea-polyphenol case in Example No. 1 as described above.
[0035] The result is shown in Table 17, revealing as follows: (1) by using 1 - menthol together with the black teapolyphenol, obtained were a signicantly long duration of masking of bad breath and refreshing effect as well as a
signicant improvement effect on aftertaste compared to sole usage of 1-menthol, and (2) sour and bitterness due to
the black tea-polyphenol were masked by using 1-menthol together with the black tea-polyphenol.
Table 16
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1-menthol
2000 ppm
black tea-polyphenol
ethanol
35 wt%
3 wt%
rened water
remainder
50
Table 17
55
concentration of
1-menthol (ppm)
2000
concentration of
black teapolyphenol (ppm)
10
duration of masking
of bad breath
8
duration of
refreshing effect
5
improvement effect
on aftertaste
11
EP 1 013 261 A1
Table 17 (continued)
concentration of
1-menthol (ppm)
concentration of
black teapolyphenol (ppm)
10
duration of masking
of bad breath
duration of
refreshing effect
improvement effect
on aftertaste
2000
50
10
13
2000
100
12
11
13
2000
1000
13
13
14
2000
10000
14
11
10
2000
20000
11
20
[0036] Mouth spray solutions containinging (-) - epigallocatechin gallate (purity 98 wt% or higher, manufactured by
Mistui Norin Co., Ltd.) of seven kinds of concentrations were prepared according to a prescription described in Table
18 and sensuous tests (A-type and B-type) by 10 panelists were conducted in a similar way as comparative example
No. 1.
[0037] The results are shown together in Table 19.
Table 18
(-) - epigallocatechin gallate
ethanol
35 wt%
3 wt%
rened water
remainder
25
30
Table 19
concentration of ( - )
-epigallocatechin gallate (ppm)
35
40
45
50
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refreshing effect
30
10
28
50
23
16
100
17
23
1000
40
10000
24
20000
[0038] The results shown in table 19 reveal as follows: (1) the masking of bad breath that seems to be due to (-) epigallocatechin gallate was positively observed, however, (2) the degree of sore and bitterness was signicant when
(-) -epigallocatechin gallate concentration was 1000 ppm or higher, and (3) the refreshing effect was hardly observed.
Example No. 3
[0039] Mouth spray solutions containing 1-menthol (concentration 2000 ppm) and ( - ) - epigallocatechin gallate (the
same as used in comparative example No. 2) of six kinds of concentrations were prepared according to a prescription
described in Table 20 and a sensuous test (C-type) by 15 panelists was conducted. The test was carried out in a similar
way to the black tea-polyphenol case in Example No. 2 as described above.
[0040] The result is shown in Table 21, revealing as follows: (1) by using 1 - menthol together with (-) -epigallocatechin
gallate, obtained are a signicantly long duration of masking of bad breath and refreshing effect as well as a signicant
improvement effect on aftertaste compared to sole usage of 1 - menthol, and (2) sour and bitterness due to (-) - epi-
EP 1 013 261 A1
gallocatechin gallate were masked by using 1-menthol together with (-) - epigallocatechin gallate.
Table 20
5
1-menthol
2000 ppm
ethanol
35 wt%
3 wt%
rened water
remainder
10
Table 21
15
concentration of
1-menthol (ppm)
20
25
concentration of (-)
-epigallo-catechin
gallate (ppm)
duration of masking
of bad breath
duration of
refreshing effect
improvement effect
on aftertaste
2000
10
13
2000
50
12
10
14
2000
100
13
12
15
2000
1000
15
15
13
2000
10000
14
14
2000
20000
10
Claims
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1.
2.
The composition of mouth spray according to claim 1, comprising (a) tea-polyphenol and (b) 1-menthol or 1-carvone.
3.
The composition of mouth spray according to claim 1 or claim 2, wherein the concentration of the tea-polyphenol
is from 10 to 20000 ppm.
4.
The composition of mouth spray according to claim 3, wherein the concentration of the tea-polyphenol is from 50
to 10000 ppm.
5.
The composition of mouth spray according to any preceding claim, wherein the total concentration of 1-menthol
and/or 1-carvone is from 100 to 10000 ppm.
6.
The composition of mouth spray according to any preceding claim, wherein the tea-polyphenol is at least one
member selected from the group containing (+)-catechin, (-)-catechin, (+) -gallocatechin, (+) - epigallocatechin,
(+)-gallocatechin gallate, (+) - epigallocatechin gallate, (-)-epicatechin, (-)- epicatehin gallate, (-)-catechin gallate,
(-) -epigallocatechin, (-)-gallocatechin, (-)-epigallocatechin gallate, (-)-gallocatechin gallate, theaavin monogallate
A, theaavin monogallate B, theaavin digallate, and free theaavin.
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