Note: Descriptions are shown in the official language in which they were submitted.
The present invention relates to dental health and
food products, and specifically to the reduction of dental caries
and tooth enamel demineralization caused by a wide variety of
food products.
A number of food products have caused concern in
recent years as being possibly related to decreased dental
health in the persons consuming them. This concern has prompted
a good deal of research to either prove or disprove the
relationship, as well as research directed toward finding ways of
eliminating the problems with respect to these products.
Principally cited as having possible connection with
decreased dental health are foods high in acid and those high in
sucrose content. Recent studies with rats, for e~ample, have
indicated that continued consumption of low pH beverages, whether
natural or artificial, can result in a generalized deminerali-
zation of the teeth. In this regard, see for example: Wagg et
al., British Dental Journal, vol. 119/ No. 3, pages 118 through
123, August 3, 1965; and McDonald Jr., et al., J. Dent. Res.,
March-April 1973, pages 211-216. Some investigators have
indicated that certain phosphates, such as calcium phosphates
may inhibit this form of demineralization or may, in fact, effect
remineralization of teeth demineralized in this manner. In this
regard, see for example: Wagg et al., supra; Picket et al.,
The Alabama Journal of Medical Sciences, vol. 2, no. 3, July 1965;
Silverstone et al., Caries Research, 5:323-342, 1971; and U.SO
Patent 3,375,168 to J. H. Curtin et al. Additives such as
calcium phosphates have not, however, completely eliminated the
problem.
While there is evidence on both sides of the question,
it can be safely said that sucrose does, under many circumstances
of use in fcod products, result in increased dental caries.
Exemplary of teachings of this kind is Scherp, Science, Vol. 173,
No. 4003, pages 1199-1205. With all the discussion and research
in this area, there is still a need for an additive which can
mitigate the problem of dental caries caused by food products
which have been identified as troublesome.
The present invention provides additives for food
products which are effective to reduce the causation of dental
caries and tooth enamel demineralization by food products which
would normally foster these problems.
Thus, the instant invention entails adding an amount of
L-aspartyl-L-phenylalanine methyl ester to a food product which
would have the normal tendency toward demineralizing tooth enamel
and/or fostering dental caries, said L~aspartyl-L~phenylalanine
methyl ester having the ability to effect a rise in the pH of a
dilutely acid aqueous solution, which amount is less than or
greater than that amount which would provide a desired level
of sweetness and reduce the tendency of the food product toward
demineralizing tooth enamel and/or fostering dental caries.
More specifically, L-aspartyl-L-phenylalanine methyl
ester (aspartame), is added to fcod compositions normally
causative of dental caries or tooth enamel demineraliæation.
The L-aspartyl-L-phenylalanine methyl ester is added alone or in
combination in any amount effective to cause a decrease in
dental caries and/or tooth enamel demineralization over that
which would normally occur when the food product is consumed.
The use of aspartame, which is well known as a sweetener
(see for example U.S. Patent 3,642,491 to J. M. Schlatter), to
provide food products of improved dental health is believed new
and should be effective over a wide range of concentrations in
the food products. Specifically, preferred concentrations for
aspartame are those above and below the levels thought by those
skilled in the art to provide desirable levels of sweetness.
However, the invention envisa~es all novel levels of aspartame
in food products where they are present, alone or in combination,
in amounts effective to mitigate the causation of dental caries
and/or tooth enamel demineralization over that which would
normally occur. Where sucrose is the cariogenic agent, amounts
of aspartame within the range of ~rom abou~ 0.1 to 10 parts of
aspartame for each lOn parts oE sucrose are believed effective.
Within the conception of the present invention is
L-aspartyl-L-phenylalanine methyl ester which effects a rise in
the pH of a dilutely acid (e.g., pH 2-5) a~ueous solution.
Specifically useful is aspartame.
The types of products in which L-aspartyl-L-phenyl-
alanine methyl ester can be employed for its advantageous effect
on dental health are broad and its effectiveness according to
this invention is not presently known to be limited by any
actors present in food products. A representative listing of
the various food products which can advantageously enjoy the
benefits of the present invention is as Eollows:
Bread
Breakfast Cereals
Cakes
Candies
Carbonated Beverages
Chewing Gum
Chocolates
Coffee L~ghteners
Cookies
Dry Beverage Mixes
F~rinaceous Snack Items
Flavoxed ~ces
Frostings
Frui~ Concentrates
Fruits
Dessexts
Xce C~eam
Juices
Puddings
~herbets
Syrups
Table Sug~r
Whipped Toppings
As indicated r this lis~ is merely representative and is
not exhaustive of the` types of food products contemplated herein.
~0 While the scope of products which can be improved by
the present invention is broad, the following disclosure will
relate specifically to a lo~ p~ beverage mix. This product is
dealt with as only exemplary and should not be taken as limiting
of the invention.
In the low pH beverage products as with the other
products encompassed by the presen~ invention, the amount of
L-aspartyl-L-phenylalanine methyl ester employed can be any
amount which is effective to attain the objects of the invention.
Preferably, however, aspartame is employed at a level insuficient
by itsel~ to provide a desirable sweet beverage or at a le~Tel
greater than that necessary, when used alone or in comhination
with another sweetener, to provide the desirable sweetness in
the beverage. While these variations in level of ~weetne$s from
conventional beverages may at first seem unusual to the consumer,
it is believed that the improvement in dental health achieved
over conventional beverages should outweigh any ~dverse reaction
in this regard.
For the purpose'of t~e present invention ~ low ~H
beverage is define~ as Qne having ~n acid p~ e,g., below about
6 and preferably beIo~ about 5, and containi~g from about ~.015
to about 0.15 gram equivalents of ~n edible acid pex ~uart of ;
beverage.
Beverage~ of this type are well known and typ~Gally
comprise an aqueous solution of a flavorant, a colorant, a sweet-
ener, a food acidulent. ~lso, these beverages can contain bufers
to control acidity, ~ums to provide texture and clouding compo-
sitions to pro~ide a degree`o~ opacity to the beverage. Beveragesof this kind can also include var;ous food and nutritional
supplements such as vitamins and minerals. Vltamins A and C are
typical of such additives.
Typicàl of the edible acids ~hich can be employed are
citric, malic, adipic and fumaric acids. These acids can be
employed alone or in combination and can be supplemented or
replaced by other conventional food acidulents.
A wide variety of fla~orants are known for use in
beverages of the kind considered here. Typical of these are
~o natural and artificial flavorants such as cherry, strawberry,
grape, orange, lemon, lime, root beer, cola, raspberry,
~rapefruit, fruit punch, and the like, which are employed in
suitably effective amounts.
Apart from the asp~rtame which has a sweetening effect
at known concentrations, ~ut ~hich i$ not employed according to
the present in~ention primarily ~s a,s~eetener, sweetness can be
obtained using any of the known,,edibIe natural or synthetic
sweeteners.
- 5
.
The aspartame is employed to effect the objects of the
present inVention at levels of fro~ about Q~25 to ab~ut 2.Q0
grams per quart of beverage or an amount of dry mîx for preparing
the same. Prefera~ly .it ~5 employed at levels o from ~bout
0.50 to about ~75 ~rams per quart of bever~ge or mix therefor.
One'preferred beverage contains a less than sweetening
amount of aspartame ~long with sucrose in a sweetening amount,
e.g., about 25 to about 100 grams of sucrose per quart of bevexage
or mix therefor, and from about ~.25 to about 0.50 grams of
aspartame per quart of beverage, the beverage, thus, having a
total amount of sweetener greater than would be normally desired.
This beverage preferably contains from'0.015 to 0.08 gram
equivalents of acid per quart of beverage. In this embodiment,
the caloric value'of the' sucrose is present in the beverage, but
the cariogenic propensities thereof are reduced, not only due to
the reduced leveI of sucrbse added, but also due to the protective - '
effect of the aspartame. The excess sweetness can be reduced, if
desired, by adding to the beverage a sweetness modulating ;~
material such as alum, naringin, or the like. '
The ingredients are preferably dry blended to form the
mix and can be agglomerated, as by steam agglomeration, if desired.
The mix ingredients are preferably packaged by volumetric
metering devices into conventional plastic coated foil packs to
preserve freshness.
The follo~in~ specific examples are presented for the
purpose of further illustrating the pxesent invention, and are not
to be taken as limiting in any re~ard~ Unless other~ise indicated,
all parts and percentages-are by weight.
" , ,; , '; ., : '
~XAMPT,E I `~
~ xelativel~ low :acid inst~nt beverage m~x ~cco~ding
to the Pxesent invention is pxepared by dry mixing ~he following
material5:
In~redients Parts
Citric acid, anhydrous
Monocalcium Phosp~ate 34.3
Aspartame 12,6
Carrier for aspartame
(hydrolyzed cereal solids~ 8,4
Flavorant 1.8
Vitamin C 1~3
Colorant 0,5
Vitamin A a. 14
About 4.4 grams of this mix are added to a quart of
water to provide a pleasing beverage ha~ing the advantages of ~.
the present invention.
EXAMPLE II
A beverage mix having a slightly higher acid con~ent
than that of Example I is prepared by dry mixing ~he following
ingredients:
Ingre~ients Parts
Citric acid, anhydrous 57.5
Monocalcium Phosphate 16~4
Trisodium Citrate 8.8
Aspartame 5,5
Carrier for ~spartame
(hydrolyzed cereal solids~ 1.8
Flavorant 6,0
Clouding composition 3.3
Vitamin C 0.6
Vitamin A 0.07
About 9 grams of this mix are added to a quart o water
to provide a pleasing beverage having the advantages of the
present invention.
EXAMPLE III
A further beverage mix, having a relatively high acid
content, is prepared by dry mixing the following ingredients:
Ingredlents Parts
Dextrin 58.4
Aspartame 1.8
Citric Acid 19.0
Clouding composition 5.6
Monocalcium Phosphate 4.0
Potassium Citrate 2.8
Tricalcium Phosphate 2.4
Vitamin C 1.5
Orange Flavorant 2.6
Vegetable Gum 1.8
Vitamin A 0.1
Color 0.15
About 34 grams of this mix are added to a quart of
water to provide a pleasing simulated orange juice having the
advantages of the present invention.
EXAMPLE I~
A gelatin dessert mix is prepared by dry mixing the
following ingredients:
. . . ..
Ing~edients Parts
Gelatin 55,6
Adipic ~cid 23.3
Fumaric Acid 2.6
Potassium Citrate 9~4
Stra~berry Flavor5 -Eixed in
vegetable ~um 1~0
Strawberry Color fixed in
vegetable gum 0.3
Aspartame 7~9
About 13 grams of this mix are dissolved in one cup of
boiling water by stirring. One cup of cold water is then added
and mixed. The total solution is then chilled to set the
gelatin, thereby providing a strawberry flavored gelatin dessert
having the benefits of the present in~ention.
EX~MPLE V
An improved table sugar is obtained by mixing 1.0
parts of aspartame according to the present invention with about
100 parts of sucrose. If desired, the aspartame can be sprayed
on in an aqueous solution while subjecting the sucrose to tumbling
in drying air.
- EXAMPLE VI
A liquid coffee lightener ~s prepared from the
following ingredients:
~ngredients Parts
Sucrose 46.6
Hydrogenated Coconut Oil 25~0
~ater 23.4
Sodium stearoyl-2-lactylate 5.0
Aspartame 0.5
_ g _
The coffee lightener is prepared by first blending 233 g
of sucrose with 25 g of finely ground sodium stearoyl~2-lactylate
in a blender for 10 minutes. This mixture is then added slowly
to 117 ml of tap water. The water is stirred gently and held at
120F. ~fter about 10 minutes of ~tirring, the sodium stearoyl-
2-lactylate is e~enly dispersedO This dispersion is then
transerred to a W~RING BLENDOR* and 125 g of hydrogenated
coconut oil at 120 is added. Blending at high speed is continued
for 10 minutes at which point the emulsion temperature reaches
160F. Upon cooling to room temperature, it gradually loses air
to give a translucent pourable emulsion of low viscosity. Upon
dilution with distilled water, the dilute emulsion is opaque and
has a pH of 6.7. The undiluted emulsion has a water activity of
0.80. This coffee lightener is used in the same manner as cream.
EXAMPLE VII
A dried coffee lightener is prepared by employing the
same procedure as that in Example VI but substituting a
combination of 40 parts 42 D.E. hydrolyæed cereal solids 2 parts
sodium caseinate and 1 part vegetable gum for the sucrose, and
spray drying the emulsion.
EXAMPLE VIII
A two-week rat feeding study was conducted with male
Caesarean-derived Sprague-Dawley rats approximately 200 grams
in body weight using the following protocol.
The animals were fed a standard animal chow diet ad
libitum throughout the study. They were housed individually in
open mesh stainless steel suspended cages in an air conditioned
room with the temperature controlled in the range 75F. + 3F.
Fifteen rats were randomly assigned to each test group after
blocking on body weightr
The following lo~ pH test beverages were fed to the
various test groups:
(Il low pH grape flavored be~erage havin~ the
following ~ormulation: :
. Gxams ~er 1 quart
Dry Ingredients of ~eVera~e
Citric Acid 1.8
Monocalcium Phosphate 1.5
Grape Flavor Q,075
~scorb~c ~cid 0.055
Grape Shade 0.023
Vitamin A 0.006
Aspartame 0.55
(2) beverage (1) with 100 gxams of sucrose per quart
of beverage in place of of the aspartame;
(3) beverage (1~ without monocalcium phosphate, but
containing an additional 0.2 grams per quart of citric acid to
balance the taste and tartness due to the removal of the
monocalcium phosphate;
(4~ beverage`(~ with 100 grams of sucrose per quart
of beverage in place of the`aspartame; and
(5) deionized water.
After the two week feediny period the rats were ::
sacrificed by decapitation and then the heads were defleshed
by scrubbing with`a toothbrush ate~ an autoclavin~ procedure
for 20 minutes at 15 pounds pressure.
The mandibular molaxs were stained by.placin~ them
in a 0.125% alcoholic solution of ~lizarin Red S, rinsed with
water and dried in a hot air oven at 150F.
After the staining process was completed the linyual
surfaces of the molars were scored for the extent of tooth enamel
demineralization using a modification of the scoring scale
developed by Restarski, Science, Vol. 102: 404-40s, 1945.
Before scoring with the aid of a binocular microscope at 13X
the molars were assigned random numbers.
The up-take of stain and the extent of ridging were
to estimate the amount of tooth enamel demineralization for each
mandibular molar using the following grading scale with an
increase in severity:
0 ~ No demineralization - no detactable lingual stain
1 - Slight demineralization - slight stain
2 - Mild demineralization - moderate stain
3 - Moderate demineralization - slight ridging, strong
stain
4 - Moderate demineralization - moderate ridging, 1/3
of dentin exposed
5 - Strong demineralization - strong ridging, 1/3 to
2/3 of dentin exposed
6 - Strong demineralization - very strong ridging,
greater than 2/3 of dentin exposed.
The results are summarized in the following table:
Tooth Enamel Demineralization
% Decrease Due
Beverage Score to Aspartame
2 1.5 --
1 0.8 47
4 3.5 __
3 2.5 ~9
0.2 __
- 12 -
.
Due to the fact that the aspartame can degrade in
aqueous system to diketopiperazine and mixtures of dikeiopipera-
zine, aspartic acid and phenylalanine, it is suggested that the
breakdown products of aspartame are similarly effective ln im-
proving dental health as is the aspartame.
EXAMPLE IX
A 60-day rat Eeeding study was conducted with weanling
Caesarean-derived male wistar caries-susceptible rats using the
following protocol:
The test group were fed semi-synthetic diets containing
5% alpha-cellulose, 20% lactalbumin, 3% corn oil, 1% Association
of Official Analytical Chemists vitamin mix and 3% of a
Massachusetts Institute of Technolog~ 200 mineral mix modified
to contain 30% dicalcium phosphate. The remaining 68% of the
diet consisted of either 68% confectionary 10X sucrose or coated
corn flakesc The animals were housed in open mesh stainless
steel suspended cages in an air conditioned room with the
temperature controlled in the range of 75F. ~ 3F. Fifteen
rats were randomly assigned to each treatment after blocking on
body weight.
After the termination of the study, the heads of the
animals were autoclaved at 15 pounds pressure for 15 minu-tes
and then the mandibles were removed and cleaned with a coarse
bristle toothbrush. After the mandibles are dried, they are
stained with 0.0208% murexide in 70% ethanol. After -the
mandibles are revised and dried, they are scored for caries
~:2
~ .
using a modification of the Keyes method in J. Dental Research
37, 1088-99 (1958). The caries scores are a combination of -the
occlusal and smooth surface caries severity scores on the
nlandibular molars using scores of 0, 1, 2 and 3 for designating
severity of the lesions.
The following treatments were included in the study:
1) beverage (1) con-taining aspartame described in
Example VIII as the drinking fluid and the semi-synthetic diet
containing 68% confectionary lOX sucrose as the carbohydrate.
2) beverage (2) containing sucrose described in
Example VIII as the drinking fluid and the semi-synthetic diet
containing 68~ confectionary lOX sucrose as the carbohydrate.
3) distilled water as the drinking fluid and the
semi-synthetic diet containing 68% corn flakes containing 0.3
aspartame.
4) distilled water as the drinking fluid and the
semi-synthetic diet containing 68% corn flakes with a 40% sucrose
syrup coating in place of the aspartame.
The results are summarized in the following table:
Caries Severit~ Scores
Decrease Due
Treatment Score to Aspartame
2 11.4 --
1 7.0 39
4 3.3 __
3 1.7 48
EXAMPLE X
A 60-day rat feeding study was conducted with weanling
Caesarean-derived male caries-susceptible rates. The protocol
was identical to that described in Example IX with the ex-
ceptions that casein was substituted for lacta]bumin as the
source of protein and the dicalcium phospha-te level in
the Massachusetts Institute of Technology 200 salt mix
- 14 -
3L~ ~r ~
was decreased to 27.5%. Distilled water was provided as the
drinking fluid. The aspartame in the diet replaced part of the
alpha cellulose.
The following dietary treatments were included in the
study:
1) Basal cariogenic diet containing 68% confectionary
lOX sucrose.
2) Same as treatment (1) with 0.341% aspartame.
The results summarized in the following table:
Caries~Severity Scores
% Decrease Due
Treatment Score to As~ rtame
1 15.5 --
2 11.6 25
The above disclosure has provided a description of
the invention for the purpose of enabling the person skilled
in the art how to make and use the same and has not been
made for the purpose of detailing all things known or obvious to
the skilled worker. Upon reading this disclosure, many
modifications and variations of this invention will become
apparent to those skilled in the art. It is intended that all
such modifications and variations be included within the scope
of the present invention which is defined by the claims,
