Note: Descriptions are shown in the official language in which they were submitted.
1063935
This invention relates to antacid tablets and
to processes ~or their preparation. More particularly,
the invention deals with such tablets containing the com-
bination of an antacid ingredient, sugar and a high pro-
portion of ~at.
BACKGROUND
Antacid compositions have been prepared in a
wide vaxiety of forms such as suspensions, solutions, emul-
sions, powders and tablets. In each case the composition
includes an ingredient which is an effective antacid sub-
stance and such substances include calcium carbonate, mag-
nesium carbonate, magnesium hydroxide, magnesium trisili-
cate, magnesium oxide, sodium bicarbonate, aluminum hydrox-
ide, aluminum carbonate, aluminum hydroxycarbonate, alumin-
um magnesium glycinate, dihydroxy aluminum amino acetate,
and magnesium aluminate. Many other compounds also come
to be useful as antacid ingredients in compositions of
this type. One such ingredient is aluminum hydroxide-
magnesium carbonate composition which is prepared as a dry
gel by Reheis Chemical Company and sold under the trademark
FMA-40. Another such composition having somewhat different
proportions of the same ingredients is sold under the trade
mar~-FMA-ll. In the specification and claims we use the
term "antacid ingredient" to mean any of the above-mentioned
antac~d substances and mixtures thereo$, together with any
compounds which include any of the above as a part of a
chemical complex.
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Antacid compos~tions containing the antacid in-
gredients above referred to may be more effecti~e when made
up in solutions or suspensions because liquid medication
can more easily reach the affected areas where treatment is
needed whereas in the case of powders or tablets, these do
not break up into the fine particle size of liquid suspen-
sions and some of the medication may never reach the areas
where treatment is needed. This is true especially as to
tablets which require mastication in the mouth. In ~ome
csses antacid tablets or portions of them may even pass
into the body in solid for~ without giving up any substan-
tial medical benefit. Also, antacids in tablet form are as
a general rule slower to take effect and slower to give
relief from symptoms of hyperac.tidy than if the same medica-
ments were contained in the form of solutions or suspensions.
However, the tablet form of antacid medication is
much more convenient to the patient. The tablets may be
carried in small containers or in a purse and may be taken
as needed without any need for extra equipment or for the
measuring of dosages. Despite limitations in giving relief,
the convenience of the tablet form of the antacid make this
form a popular kind of antacid composition.
What has been needed is an antacid tablet which
- is more effective in giving relief to symptoms of hyper-
acidity, a tablet which will release its benefits more
rapidly, which will pass easily to the areas where treat-
ment iL needed, =nd which will also yield benefit= to rhe
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~063935
patient over a longer period of time. At the same time lt i5
desirable that the ingestion of the tablet be pleasant and
without discomfort to the patient such as would be caused by
grittiness or other unpleasant feeling in the patient's mouth.
Accordingly, applicants have set out to discover an
improved antacid tablet which will meet the needs above expressea.
Applicants conceived the idea that an improved tablet
containing fat in combination with an antacid ingredient and
sugar, the fat being contained in a relatively high proportion
in the tablet; also that the tablet have a very limited hardness;
but according to the prior teachings and the prior practice in
the tableting art, such a tablet could not be prepared. For
one thing, a material having such a high proportion of fat
along with sugar and antacid would be expected to stick to the
cavity walls and to the punches of the tableting presses so that
the tablets could not be ejected from the press.
Accordingly applicants set out to provide a process for
preparing the improved antacid tablets which avoids the
difficulties facing the art, a process by which the tablets
may be made with ease.
SUMMARY
In one particular aspect the present invention provides
an antacid tablet containing an antacid ingredient in an amount
of from 5 to 40%, sugar in an amount of from 15 to 80%, fat in
an amount of from 15 to 30%, and water in an amount of from 2
to 12%, said percentages being by weight based on the total
weight of the tablet.
In another particular aspect the present invention provides
in a process for preparing an antacid tablet in which an antacid
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ingre~ient in an ~mount of from 5 to 40%, sugar -in arl amount of
from 15 to 80%, fat in an amount of 15 to 30%, and water in an
amount of from 2 to 12% are combined to provide a powdered
mixture, said percentages being by weight based on the total
weight of the mixture, the step comprislng compressing said
mixture into tablets under a pressure from 150 to 200 pounds
per square inch, using a conventional tableting machine having
at least those parts of the machine contacting said tablets at
a temperature at or above the melting point of the fat contained
in said tablets.
We are aware that each of the antacid ingredients, the
sugar, and the fat have separately been formed into tablets,
but believe that their combination in accordance with disclosures
herein contained constitutes a basic improvement in this art.
DETAILED DESCRIPTION
As the antacid ingredient we may use any of the substances
which have been used in the prior practice in making antacid
compositions including any of those which we have mentioned above
under "Background" but we prefer combinations of aluminum
hydroxide, magnesium oxide and magnesium carbonates, particularly
that combination sold under the trade mark FMA-40. Such
substances may be in the form of a fine powder, the size of the
particles in terms of density being something of the order of
.15 grams per millimeter plus or minus .1 grams.
As the sugar ingredient we prefer to use sucrose.
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We may use also dextrose, lactose, fructose, galactose,
manitol, sorbitol, maltose or sugars of other particular
types. It is pos~ible that the dextrose and other sugar~,
other than sucrose, may give some difficulty by browning,
We prefer also that the sugar be in the form of fine powder
- ~ometimes called "fondant sugar" whlch i8 of a fineness such
that at least 50% will pass through a 200 mesh screen. It
is better that at least 90% of the sugar pass through a 200
mesh screen. This sugar ingredient may contain a small
C amount of a material such as starch in the form of cornstarch
or tapioca--we prefer pregelatinized tapioca--as an anti-
caking agent in the amount o about 2.9% of the weight o the
finished tablet.
As the fat ingredient we may use any natural or
synthetic fat such as animal or vegetable fats and shorten-
ings. We prefer that the fat have a meiting point not higher
than 115F, and find that fat having a melting point of the
order of 101 to 103F is most useful.
In addition to the antacid, sugar and fat ingredi-
ents, we may add a suita~le dye to provide a desired color,
common salt and a flavoring agent to provide a desired fla-
vor, and water as needed in the processing. All materials
should be of pharmaceutically acceptable quality.
- To combine the ingredients, we may put a quantity
of water, for example about 25 liters, into a suitable mixing
container, and add the dye and salt in a water solution and
mix to attain a complete solution. Water may be added to
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10~3935
give the desired amount of water, ~or example, abou~ 27
liters, mixing thoroughly.
The sugar, containing a small amount of an anti-
caking agent, may be placed in a mixer, the mixer qtarted
and the dye qolution added s~owly, mixing for a few mlnutes
until the batch has a creamy consistency and uniform color.
The improved antacid tablets prepared in accord-
ance with our invention may contain the following percent-
ages of essential ingredients:
Usable Preferred
IngredientPercenta~ePercenta~e
Antacfd 5 to 40 12 to 30
Sugar 15 to 80 35 to 65
Starch 0 to 6 1 to 5
Fat 3 to 40 15 to 30
Water 2 to 12 4.5 to 9
The percentage values of ingredients above given
are by weight based on the weight of the tablets which are
prepared.
From the above information as to the primary con-
stituents of the finished tablets, specific amounts of the
ingredients may be selected from the ranges given and the
amount of the respective antacid, sugar and fat starting
materials may be calculated to ma~e the desired proportions
in the finished tablets.
The fat may be heated to a temperature above the
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106393S
melt~ng point of the fat, of the ordcr of 120 to 130F(49 to 54C) to change the fat to a liquid, and the flavor-
ing agent may then be mixed in.
Then the melted fat having the flavoring therein
and the powdered antacid ingredient may be thoroughly mixed
to produce a uniform dispersion o antacid throughout thé
fat. The water, coloring and salt are thoroughly mixed
with the sugar ~o form a fondant-like mixture. These two
separate mixes may then be blended until they are completely
dispersed in each other. Any powdered flavoring agent
which it is desired to use may also be mixed in at this
point. The batch is now ready for granulation.
The batch in the mixer may be cooled a8 it i8 being
mixed by the addition of dry ice until the temperature of
the batch has dropped to something below 40F, or example,
to about 35 to 40F (2 to 4C).
The hammermill, one type of which is known as a
Fitzmill, may be prepared by passing dry ice through it
while operating at high speed with impact forward.
The cooled batch may then be passed through the
hammermill operating at high speed with impact forward. The
cooled temperature may be maintained by the introduction of
a coolant uch as liquid nitrogen. Preferably the tempera-
ture of the batch as it comes from the hammer is near or
below 0C. The temperature may be substantially below O~C,
there being no limit on the lower side except that when the
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1063935
temperature is very low, heat ~s required to bring it back
to the temperature at which continued processing can take
place.
The material rom the h~mermill may be put ~nto
a dryer and drlet at a temperature, for example, o about
70 to 75F. The moisture may be brouzht down at this point
to about 8 to 10% based on the weight of the material. Then
we prefer to pass the dried material through an agglomerator
to make a more uniform size of particles. We prefer that
the operation be continued until all of it will paQs through
à 4 mesh screen so that a maximum of 15% will pass a 40 mesh
screen. If desired, the agglomerated material may be fur-
ther dried to as low as 3% moisture, desirably in the range
of about 6.8 to 7.8% based on the weight of the material
has proved to be quite satisfactory.
The foregoing detailed description of the prepar-
ation of material for tableting sets forth what Applicants
believe to be the best procedure but it will be apparent
that this procedure may be abbreviated by omission of non-
essential steps. For example, the flavoring and dye ingredi-
ents may or may not be included and the material prepared
using only the essential antacid ingredient, the sugar and
the fat along with a small amount of moisture Also, the
various-detailed steps may be varied or changed in many
respects in accordance with the knowledge of the art.
- The proportions of the antacid ingredient, the
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1063935
sugar and the fat may also vary. ~hé improved tablet may
contain from 5 to 40% antacid ingredient, from 3 to 40Z
fat, from 15 to 80% sugar, with the preferred fat range
being from 15 to 30% and water in the proportion of from
2 to 12% with from 4.5 to 9~ preferred. Pregelatinized
tapioca starch may be included in the preferred range of
1 to 5%. All of the above percentages are weight amounts
based on the total weight of the mixture after drying.
The quantities of these ingredients for any particular
batch may be determined as required to result in the
selected proportion of ingredients, the size of the batch,
etc.
The antacid powder composition prepared as above
described may be compressed into tablets of desired form
using a standard tableting machine by operating the machine
in a prescribed way. It is important first that the tablet-
ing machine, or at least those parts of the machine which
contact the tablets under compression, be maintained at a
temperatu~e at or above the melting point of the fat con-
tained in the tablets. This may be don~ by heating the
room in which the tableting operation is performed to an
elevated temperature above normal room temperature and
above the melting point of the fat, suitably about 110 to
125F (~3 to 51C), or by enclosing the tableting machine
in a shroud and maintaining the temperature within the shroud
at the elevated temperature just referred to. The dies and
punches of the press are maintained at a temperature which
keeps the fat liquid at the punch/tablet interface and
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allows the tablets to come off the tableting machine with-
out sticking. This may be accomplished by the use of
lamps which direct infrared light toward the machine, I
the temperature of the punches on the tableting machine
is below the melting point of the fat, then the fat wh~ch
melts at the interface on compression solidifies before
the tablet is released, causing sticking of the tablet to
the punches.
C It is also important to limit th2 pressure used
in forming the tablets. The pressures commonly used in
tableting are of the orter of 2000 or 3000 pounds per square
inch, but we find it advantageous in forming our improved
antacid tablets to use pressures substantially lower than
this and within the range of from about 50 to 600 pounds per
square inch, preferably from about lS0 to 400 pounds per
square inch.
The tablets which are formed using the conditions
above described may be collected, packaged and distributed
through regular trade channels.
The improved tablets have been found to be very
effective in use. We believe this is due in part to the
use of fat in the tablets in combination with the antacid
ingredient and sugar constituents. This gives the tablets
a better eating quality and mouth feeling, and helps to
form a coating which lines the esophagus and which resists
the effects of stomach acid juices. The fat also helps to
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106393S
densify the s~tive antacid ingredient in thé process o
manufscture since the fat and antacld are premixed and th$s
permits the whole batch to be more easily mixed in a uni-
form manner. Further, it is believed that the efect of
the fat extends the time during which the tablet gives
beneficial effect. Also, the lower values oi~ hardness
are believed to contribute to the easy breakup o the tablet
in the' mouth, and this provides more surface area of ant-
acid material and therefore quicker and more complete action.
The following specific examples demonstrate the
practice of our invention in the preparation of the improved
antacid tablets:
Example I
A dye solution was prepared using the following
supplies:
Constituent Quantity Percent
C Dye, PD&C Yellow #56.38 g .0226
- ~ye, FD&C Blue ~12.13 g .0076
Sodium Chloride USP1215. g' 4.3049
Tap water 27.0 L 95.6649
Total28.225 Kg 100.00 %
25 liters of filtered tap water was placed in a --
mixer and the dye solution added to it. Water was added to
make 27 liters.
44.65 Kg of powdered sucrose having a fineness
such'that more than 90% passes a 200 mesh'screen and
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containing 2.6 Kg of pregelatinized tapiocaj was placed
in a Si~ma Day mixer, the mixer started and the dye solution
added to the sucrose, Mixing was continued until the batch
had a creamy consistency.
22.5 Kg of hydrogenated vegetable ~at ~having
the trade mark Duromel) was liquefied by heating to 120F.
20.0 g of spearmint oil and 35.0 g of peppermint oii were
added to the fat and mixed in.
Q
C ` 13.5 Kg of FMA-4~rwere intermixed and added to
the Sigma Day mixer. Mixing was continued until the mass
became completely uniform. Dry ice was added to keep the
batch at a temperature of between 35 and 40F,.
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The batch was put through a hammermill operated
at high speed with impact forward while introducing liqui~
nitrogen to maintain the batch temperature at about -10 -to
-20F. The temperature of the batch coming from the ham-
mermill was about 0 to -10C.
.
The batch was then transferred to a fluid bed
drier operated at about 70- ?5 F until the batch came to this
same temperature and a moisture of 8 to 8.6%. The batch
was then transferred to a blender where agglomeration took
place and the agglomerated mass was then classified by
passing the same through a No. 4 screen, and then further
dried to a moisture content of about 7%.
In the tableting operation we used a tableting
~achine preheated to 120F and a shroud of polyethylene
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1063935
film about the tableting machine and heated the air within
the shroud to about 75 to 100F, and used a pres6ure on the
plungers of the machine of 300 pounds pex square inch,
We used heating lamps to maintain the machine temperature
of from 105 to 120F.
Then the batch material was fed to the tableting
machine and tablets formed. The tablets were collected
and packaged in polyethylene-lined cans.
Example II
1212 g of dried fondant sugar were blended with
10.5 g of salt and 43 g water containing 15 drops of color
and 30 drops of peppermint flavor. 319.05 g of ~inely
powdered antacid material (FMA-l~ and FMA-40~ each of
which is a mixture of aluminum hydroxide and magnesium
carbonate) was dispersed in 584.85 g of melted shortening
(melting point 102-105F). The two abo~e-described mix-
tures were blended together and allowed to cool and solid-
ify. The cooled mass was ground in a Fitzpatrick hammer-
mill using liquid nitrogen injected into the milling head
as a coolant. The mill was operated at 5800 rpm and the.
screen through which the material must pass was .0156 inches
in diameter. The resulting powder was used to make antacid
tablets using a compression pressure of 250 pounds per
square inch with the machine shrouded by a polyethylene
film and the temperature of the machine maintained at 100
to 125F.
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~xample III
606 g of dr~ed fondant sugar, 60 g of corn ~yrup,
5.5 g of salt and 25 g of water were mixed together ln a
Hobart mixer. To this mixture was added gradually 292,5 g
of melted shortening having a melting point of 102 to 105F,
To this was added 7 drops of green food coloring and 15
drops of peppermint flavor. Mixing was continued until the
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mass was uniform. At this point 399 g of FM~-ll was added
This was mixed in thoroughly and the mass allowed to cool
and crystallize out. The cooled, crystallized mass was put
through a "finishing machine" (a swept screen type of machine
in which the material is forced through the screen by revolv-
ing blades). The powder from this procedure wa~ tableted as
set forth in Example II.
Example IV
2 pounds of fondant sugar (fine enough that 90%
or more will pass a 200 mesh screen), 1/4 oz. of salt,
2-1/2 oz. of water, and ll drops of green ood coloring
were mixed together in a Hobart mixer. 8-1/2 oz. of finely
powdered antacid mixture (FMA-ll) were dispersed in 15-1/2
oz. of melted shortening (102 to 105F melting point). The
shortening and antacid mixture was added to the ~obart
mixer with the sugar mixture, and mixing was continued until
a homogenous smooth mass was obtained. The mass was allowed
to cool and crystallize out. It was then ground through a
hammermill equipped for liquid nitrogen injection into the
grinding chamber. The mill was operated at 5800 rpm-and
had a .0156 inch screen. The powder from this procedure
was tableted as set forth in Example IX.
Example V
2 pounds of fondant sugar, il4 oz. of salt, 10 oz.
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of finely powdered antacid mixture (FMA-ll), 1 pound 2 oz.- -
of melted shortening, 3-1/2 oz. water, 6 drops of green food
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coloring and 23 drops of peppermint flavor were mixed
together and rolled into dough of desired thickness. Pi~ls
were cut into tablets using a cookie cutter and the resulting
tablets allowed to dry.
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Example VI
21 oz. of sucrose and 4.1 g of salt were dissolved
in 8 oz. of water. The solution was brought to a boil and
kept boiling until a temperature of about 2S6F was reached.
At this point the heated mass was cooled on a marble slab.
4 oz. of butter was melted and m~xed with 1 oz. of cotton-
seed oil. 3-1/2 oz. of finely powdered antacid mixture - -
(designated F~-ll and composed of a mixture of aluminum
hydroxide and magnesium carbonate) was then dispersed
throughout the liquid mixture using a Hobart mechanical
mixer. The antacid and fat mixture was then foIded into
the cooled boiled sugar mass along with 17 drops of pepper-
mint oil and 7 drops of green food coloring. This mass
was then pulled until crystallization began to take place.
At this point the mass was formed into ropes and cut into
pillow shapes.
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To demonstrate the "hardness" of the tablets
made as in Example I, we subjected the tablets to tests
on the Instron testing machine using a probe having a cone-
shaped end with rounded end tip and measured the peak force
neéded to drive the probe 0.075 inches into the tablet at a
8peed of 0.5 inches per minute.
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A critical element of such a test is the shape
of the end of the probe which is pressed into the surface
of the tablet. In our har~ness tests, we used a probe
having a blunt point resembling a half sphere with a diame-
ter of .175 inches and this blunt tip was pre8Bed 810wly
into ehe surface of the tablet at a rate of 0.5 inches per
minute. The peak force necessary to move the tip to a
depth of .075 inches was then taken as a measure of the
hardness of the tablet.
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We find that tablets made as set forth in Example
I have a peaX penetration force of less than 9 pounds
whereas any other antacid tablet known to us and in com-
mercial use today requires much higher force for this stan-
dard penetration under similar test conditions.
Table I contains data obtained by testing the
improved tablets of this invention and comparing these with
other antacid tablets known to the trade.
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TABLE I
Peak Force Required
(lbs. per sq. in,)
for Penetration .075 inches
Make of Tablet in Surface of Tablet
Tablet as prepared in
Example I:
Average of 40 sample
from 8 lots 3.5
Mylanta II
Avexage of 10 samples 28.4
Di-Gel~9
Average of 10 samples 23.8
`: Maalox No. 2
Average of 7 samples 34.?
Tums~
Average of 6 samples 15.2
Alka~2 .
Average of 6 samples 15.~
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. While our invention has been set forth and demon-
`. strated in terms of certain embodiments, it must bé under-
: stood that other embodiments may be utilized, and many
- changes and variations may be made both as to the ~rmula-
tion of the improved tablets and as to their process of -
manufacture all within the spirit of the invention and
within the scope of the appended claims.
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