U.S. patent number 3,886,265 [Application Number 05/375,615] was granted by the patent office on 1975-05-27 for mouth cleansing preparation.
This patent grant is currently assigned to Astra Lakemedel Aktiebolag. Invention is credited to Hans Christer Arvid Evers, Max Fischler.
United States Patent |
3,886,265 |
Evers , et al. |
May 27, 1975 |
Mouth cleansing preparation
Abstract
The use of at least one ene-diol compound having at most 6
carbon atoms and selected from the group consisting of ascorbic
acid, isoascorbic acid, dihydroxymaleic acid, dihydroxyfumaric
acid, and reductic acid, or salts or derivatives thereof, and an
oxidizing agent in the form of a water soluble peroxide selected
from the group consisting of alkali metal percarbonate, alkaline
earth peroxide, carbamide peroxide, and hydrogen peroxide in the
manufacture of preparations effective against bad breath,
preferably in the form of peroral dosage units.
Inventors: |
Evers; Hans Christer Arvid
(Sodertalje, SW), Fischler; Max (Enskede,
SW) |
Assignee: |
Astra Lakemedel Aktiebolag
(Sodertalje, SW)
|
Family
ID: |
20274522 |
Appl.
No.: |
05/375,615 |
Filed: |
July 2, 1973 |
Foreign Application Priority Data
|
|
|
|
|
Jun 30, 1972 [SW] |
|
|
8597/72 |
|
Current U.S.
Class: |
424/49 |
Current CPC
Class: |
A61Q
11/00 (20130101); A61K 9/0056 (20130101); A61K
8/22 (20130101); A61K 9/0007 (20130101); A61K
8/676 (20130101) |
Current International
Class: |
A61K
9/00 (20060101); A61K 9/46 (20060101); A61k
007/16 () |
Field of
Search: |
;424/49-58 |
References Cited
[Referenced By]
U.S. Patent Documents
|
|
|
3065139 |
November 1972 |
Ericsson et al. |
|
Primary Examiner: Huff; Richard L.
Attorney, Agent or Firm: Brumbaugh, Graves, Donohue and
Raymond
Claims
We claim:
1. A composition effective in combatting bad breath consisting
essentially of an ene-diol compound selected from the group
consisting of ascorbic acid and isoascorbic acid, said compound
being present in an amount of at least 10 mg, and an oxidizing
agent in the form of a water soluble peroxide selected from the
group consisting of alkali metal percarbonates, alkaline earth
peroxides and carbamide peroxide, wherein said oxidizing agent is
present in an amount corresponding to active oxygen in an amount of
at least 1 mg., in each case per peroral dosage unit.
2. A composition according to claim 1 wherein the ene-diol compound
is ascorbic acid.
3. A composition according to claim 1 wherein the ene-diol compound
is ascorbic acid present in an amount at least 10 mg and the
oxidizing agent is sodium percarbonate present in an amount
corresponding to active oxygen in an amount of at least 1 mg, in
each case per peroral dosage unit.
4. A composition according to claim 1, wherein the oxidizing agent
is sodium percarbonate.
5. A method of inhibiting bad breath by administering perorally at
least 10 mg. of an ene-diol compound selected from the group
consisting of ascorbic acid, isoascorbic acid, and salts or
derivatives thereof, together with an oxidizing agent in the form
of a water soluble peroxide selected from the group consisting of
alkali metal percarbonates, alkaline earth peroxides, carbamide
peroxide, and hydrogen peroxide, in an amount corresponding to
active oxygen in an amount of at least 1 mg., in each case per
peroral dosage unit.
Description
The present invention relates to the use of an oxidizing agent
together with at least one ene-diol compound having at most 6
carbon atoms, in the manufacture of preparations which are
effective against bad breath.
The object of the present invention is to eliminate fetor ex ore,
bad breath, without influencing the natural micro flora of the
mouth.
Bad breath is a great social handicap to many people and therefore
there is a demand for preparations which can eliminate it. Although
frequent tooth brushing is carried out it has been shown that bad
breath persists. The flavoring and aroma agents present in tooth
paste, such as menthol, mask bad breath for a period immediately
following brushing, but this is temporary, because the bad breath
is caused primarily by methyl mercaptan formed in the mouth cavity,
and also to a less extent by dimethylsulphide, ethanol and
n-propanol.
Other mouth-washes intended to be used against bad breath are
known. However, such mouth-washes do not reduce the amount of e.g.
methyl mercaptan but only mask it.
It has been previously known (see U.S. Pat. No. 3,065,139) to use
bactericide preparations containing an ene-diol compound, a
peroxide, and a metal ion catalyst for infections in the mouth
cavity, such as gingivits and stomatitis. The present inventors
have shown that such preparations have a certain effect against bad
breath by reducing the amount of methyl mercaptan. Such
preparations have, in order to obtain an acceptable antibacterial
effect, been used in an amount of 170 mg calculated on the active
compounds for each administration.
It has now surprisingly been found possible to reduce the amounts
of compounds creating bad breath by preparing and using mouth
cleansing preparations containing a peroxide and an ene-diol
compound, preferably without a metal ion catalyst.
According to a preferred embodiment of the invention ascorbic acid
and sodium percarbonate are used.
As suitable ene-diol compounds besides ascorbic acid, isoascorbic
acid, dihydroxymaleic acid, dihydroxyfumaric acid, or reductic acid
(2,3-dihydroxy-2-cyclopenten-1-one), may be used, or salt thereof,
such as the sodium, potassium or calcium salt, or derivatives
thereof such as the esters of fatty acids having 2-18 carbon atoms,
such as the acetate, palmitate or stearate. As a peroxide besides
sodium percarbonate, other alkali percarbonates, alkaline earth
peroxides, carbamide peroxide (carbamide crystallized with H.sub.2
O.sub.2 instead of H.sub.2 o), and hydrogen peroxide may be
used.
Furthermore, in the preparation of solid preparations, inert
filling agents and lubricants known per se are used.
Such filling agents are e.g. mannitol, sodium bicarbonate, tartaric
acid and starch.
As lubricants, magnesium stearate, and paraffin may be used.
Binding agents used in the granulation of the compounds prior to
the manufacture of e.g. tablets and the like are e.g.
polyvinylpyrrolidone and gelatin.
If a special flavor is desired, flavoring agents may be added.
Suitable flavors are spearmint, peppermint, menthol, spiced fruits,
orange, lemon, lime, etc.
In the utilization of a preparation according to the present
invention, one obtains a considerable reduction in the amount of
compounds creating bad breath, a weak interference with the micro
flora of the mouth cavity and moreover a cheaper and more storage
stable product than previously known products.
The preparation ready for use in the form of tablets, pellets or
granules is chewed, whereby a reaction between the two active
components, the ene-diol compound and the oxidizing agent is
obtained and a destruction of the bad smelling compounds takes
place. The amount of active oxygen produced per occasion of
administration is at least 1 mg, preferably 3 mg, and the amount of
the ene-diol compound is at least 10 mg. The administration takes
place 3 to 4 times per day. The preparation may also be
manufactured as soaking tablets, lozenges, chewing gum or in
aerosol or spray form. Tablets may be chewed, or dissolved in water
to produce a mouth wash. The amount of ene-diol compound should not
exceed 200 mg per occasion of administration and the amount of
peroxide should thus not exceed 20 mg as active oxygen.
The present invention will be described more in detail below with
reference to the examples given.
EXAMPLE 1
Chewable tablets were prepared containing Ascorbic acid 100 mg
Sodium percarbonate corresponding to active oxygen 9 mg Sodium
bicarbonate 50 mg Tartaric acid 80 mg Cetyl pyridinium chloride
0.05 mg Flavoring agents q.s. Mannitol ad 750 mg
The tablets were prepared by granulating the mannitol and the
sodium percarbonate with a solution of gelatin in water. The sodium
bicarbonate was granulated with a 50% solution of
polyvinylpyrrolidone in ethanol. Thirdly, the ascorbic acid and
tartaric acid were granulated with a solution of polyethylene
glycol in ethanol. After drying, the different granulates were
passed through an oscillating granulator where the granulates are
mixed with flavoring agents. Finally, tablets were pressed in a
common tablet punching machine.
EXAMPLE 2
Effervescing granules were prepared and packed in dosage units,
whereby each dose contained
Ascorbic acid 10 mg Sodium percarbonate corresponding to active
oxygen 1 mg Sodium bicarbonate 4 mg Tartaric acid 5 mg Polyvinyl
pyrrolidone 0.02 mg Flavoring agents q.s. Coloring agents q.s.
Mannitol 0.03 g
The granules were prepared in accordance with the tablets above,
excluding the tableting step.
EXAMPLE 3
Effervescing tablets were prepared containing
Ascorbic acid 50 mg Sodium percarbonate corresponding to active
oxygen 5 mg Tartaric acid 5 mg Sodium bicarbonate 25 mg Starch 10
mg Polyvinyl pyrrolidone 2.5 mg Flavoring agents q.s. Coloring
agents q.s.
The tablets were prepared in accordance with the tablets of Example
1.
EXAMPLE 4
Chewable tablets were prepared containing
Isoascorbic acid 35 mg Sodium percarbonate corresponding to active
oxygen 3.5 mg Sodium bicarbonate 20 mg Tartaric acid 5 mg Cetyl
pyridinium chloride 0.02 mg Flavoring agents q.s. Mannitol ad 300
mg
The tablets were prepared in accordance with the tablets of Example
1.
The reducing effect of the above preparations on bad breath has
been studied in vitro. Morning saliva from a number of tested
persons was incubated at 36.degree.C for 5 to 12 hours until great
amounts of methyl mercaptan had been formed, whereupon the saliva
was divided into samples each containing 3 ml in 20 ml injection
flasks, which were deep-frozen in a Dewer-vessel using CO.sub.2
-ice. The different compared preparations were then added in the
amounts stated by opening the capsule of the deep-frozen flasks,
introducing the preparation, rapidly removing the air by sweeping
with nitrogen gas, and closing the flasks again. Thereupon, the
flasks were thawed and after 20 minutes at 36.degree.C a sample was
taken and analyzed on a gas chromatograph.
The results are given in Table 1 below, where the values for A, a
control sample; B, a preparation according to the invention, based
on ascorbic acid as described above in Example 1; C, a preparation
according to the invention containing in addition 0.2% of a heavy
metal catalyst in the form of copper sulphate calculated on the
ene-diol compound; and D, a known mouth-wash containing menthol as
masking agent are given. In Table 2 a comparison between a control
sample A, and the preparations B and C and in addition, E, a liquid
antibacterial iodine composition having oxidizing properties is
given. The results are given in mm peak height of the gas
chromatograms.
Table 1
__________________________________________________________________________
Compound in MeSH EtOH n-PrOH MeSSMe the breath Preparation Mean
SD.sup.xx) Mean SD Mean SD Mean SD value value value value
__________________________________________________________________________
A 3584 224.0 336 40.6 84 6.1 -- -- C 10 mg 69 85.7 360 17.4 88 1.0
29 10.0 B 10 mg 23 18.8 368 13.9 88 2.6 33 12.2 D 10 .mu.l 1872 --
4160.sup.x) -- 83 -- 18 --
__________________________________________________________________________
.sup.x) The preparation contained ethanol .sup.xx) Standard
Deviation
Table 2 ______________________________________ Compound in the
breath MeSH n-PrOH MeSSMe Preparation
______________________________________ A 1600 50 2 C 50 mg 86 48 5
B 50 mg 30 45 5 E 10 .mu.1 840 48 2
______________________________________
As evident from Tables 1 and 2 above, a marked decrease in the
amount of methyl mercaptan present after the addition of a
preparation of the invention was obtained. Thus, the preparation of
the invention shows an even better result than the corresponding
preparation containing a heavy metal ion catalyst. The great
decrease i.e. from 3584 mm peak height in the blank to 23 mm peak
height is to be noted.
* * * * *