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Патент USA US3035995

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"1c
3,035,985
7 I Patented May 22, 1%62
2
compositions having particularly objectionable tastes, such
3,035,985
as, for example, reduced iron, ferrous sulfate, ferrous
gluconate, ferrous glutamate, ferric pyrophosphate, ferric
Lewis E. Stoyle, Jr., West?eld, Philip A. Ouellette, Rah
objectionable taste of the iron compositions is primarily
CHEWABLE FATTY COATING OF IRON
PARTICLES
ammonium citrate and the like may be used. Since the
way, and Edward J. Hanus, Palisade, N.J., assignors to
Merck & Co., Inc, Rahway, N.J., a corporation of
New Jersey
‘No Drawing. Filed Sept. 30, 1959, Ser. No. 843,371
4 Claims. (Cl. 167-82)
attributable to the presence of iron contained therein, this
invention contemplates the use of various other solid iron
compositions which meet the requirements as de?ned
above.
10
Fatty compositions having a melting point of at least
This invention relates to pharmaceutical preparations
45° C. and not greater than a temperature at which the
and more particularly to coated iron preparations which
iron composition present in the molten fatty suspension
are substantially tasteless.
'
would tend to ‘decompose, and consisting entirely or pre
dominantly of a mixture of saturated fatty acids having
positions for the treatment and prevention of iron de 15 from 14 t0‘18 carbon atoms, may be used in practicing
?ciencies in humans and animals is well known. Most
the instant invention. Fatty compositions consisting en
of these compositions today are administered in the form
tirely of mixtures of saturated fatty acids, such as, for
The use of reduced iron and various other iron com
“Pi
"
of tablets, capsules, elixirs and the like. However, be
cause of their inherently unpleasant taste, which is pri
example, stearic and palmitic, stearic and myristic, pal
mitic and myristic, stearic, plalmitic and myristic, are
marily attributable to the presence of iron contained 20 quite satisfactory. Fatty compositions consisting pre
therein, these compositions are difficult to formulate into
dominantly of a mixture of saturated fatty acids and con
a palatable product. Various types of formulations have
taining up to about 11% by weight unsaturated fatty acid
been suggested to overcome the taste problem, but, ‘for
selected from the group consisting of oleic acid, linoleic
the most part, these formulations are generally not com
acid ‘and mixtures thereof may be used with equal facility.
pletely satisfactory. In general, the taste problem has 25 Fatty compositions of the latter type are particularly
been attacked by various techniques which were aimed
at masking the taste of these compositions by substituting
for their undesirable and unpalatable ?avor an overriding
and availability. Speci?cally, fatty compositions com
mercially available from Emery Industries, Inc., Cin
or overwhelming ?avor which was somewhat more agree
cinnati, Ohio, under the name Emersol, such as, for ex
able to one taking these compositions. These techniques
included the use of ?avoring agents in tableting or capsule
coating operations and the use of various ?avored solu
tions and emulsions.
However, the addition of a masking ?avor is not a
completely satisfactory technique because the objection
useful and preferred by reason of their relative cheapness
ample, Emersol 110, Emersol 120, Emersol 132, Emersol
140 and Emersol 150 are especially valuable. In each
case it is, of course, essential that the melting point he in
the above-described range, that the fatty compositions
be pharmaceutically and medically acceptable, and that
35 no undesirable taste be imparted to the preparations of
able ?avor of the iron composition in most instances
this invention by the fatty composition itself. With these
manifests itself in the phenomenon of aftertaste. Thus,
requirements in mind, any of the above-mentioned fatty
masking the ?avor of the iron compositions is only partly
or waxy compositions would be suitable for use in the
effective in solving the ?avor problem.
preparation of the instant invention.
According to the present invention, it has been found 40 The iron compositions may be used in proportions of
that fat insoluble iron compositions can be rendered sub
up to about 50% by weight of the mixture of iron com
stantially tasteless by coating these compositions with a
position and fatty composition with proportions of up to
fatty composition which is a solid at room temperature.
about 35% preferred.
The fatty composition used for coating the various iron
The process of coating the iron composition may be ac
compositions should have a melting point of at least 45 complished in a variety of ways so long as the product
45° C. in order that the preparation of the coated iron
compositions may be accomplished with facility and in
order to insure the stability of these coated iron composi
tions at ordinary temperatures.
It should be noted that when reference is made herein
to “iron compositions,” it is meant to include such solid
materials as reduced iron and other forms of iron com
obtained is the result of a chilling action upon a suspen
sion of the iron composition in a molten fatty composi—
tion.
Various chilling techniques are known. For example,
the hot suspension may be dropped into a cooled bath of
water Or other suitable known non-solvent for the sus~
‘ ' pension, whereby droplets of the suspension are caused
pounds which contain iron in an assimilable form and
to solidify. Another technique is the use of a spinning
are suitable for use in treating and preventing iron de—
disc type of apparatus. This is operated by causing the
?ciencies.
55 hot suspension to impinge upon the surface of a spinning
The coating process involves the preparation of a sus
disc, which divides the suspension into small globules and
pension of the particular iron composition having a par
scatters them into a chilling Zone, which serves for chill
ticle size of at least about 200 mesh, in a molten fatty
ing the suspension, such as by provision of a cooling
composition and the chilling of the resulting suspension
means therein. A particularly desirable and preferred
to produce solid spheroidal particles of the iron composi 60 means of accomplishing this result is the use of a spray
tion having a coating of the fatty composition. By the
chilling technique. For operation of this technique the
term “spheroidal,” it is means discrete rounded particles
suspension of the iron composition in the molten fatty
which may be of spherical or nearly spherical shape,
,
The solid iron compositions which may be used in
practicing this invention must, of course, be pharmaceuti
cally and medically acceptable for use in preventing and
treating iron de?ciencies. In addition, since the coatings
are produced by a process of chilling a suspension of the
composition is passed through heated lines to a heated noz
zle and thereupon sprayed into a chilling Zone or chamber
65 which is maintained at ambient or lower temperatures,
whereupon discrete coated particles of the preparation
solidify upon being sprayed into this chilling zone.
The product of vany of these chilling methods is a par
iron composition in a fatty composition, it is essential
ticulate mass in which the particles are individually
that the iron composition be substantially insoluble in the 70 steroidal in shape. These particles are found to be
fatty composition. With these requirements in mind, iron
homogeneous in appearance and to possess a uniform coat
3,035,985
4
3
ing of the fatty composition utilized in the preparation
Example 6
of the suspension.
The products of this invention which contain biologi
cally available iron are essentially tasteless and may be
readily formulated into various types of tablets and other
Emersol 150 containing about 82% by weight of stearic
acid, 15% palmitic acid, 2% myristic acid and 1% oleic
The procedure of Example 4 was followed except that
acid was substituted for Emersol 132 and a feed temper
ature of 93° C. was used. The product was found to be
pharmaceutical forms as desired. Because of the objec
tionable taste of the iron composition used, exempli?ed by
the disagreeable taste of reduced iron, ferrous sulfate, and
ferric pyrophosphate, for example, the products of this in~
substantially tasteless.
Example 7
vention are particularly useful in the form of chewable
tablets. In addition to the coated preparations of this
The process of Example 2 was followed except that
ferrous sulfate exsiccated (325 mesh) was substituted
invention, the formulated tablets may contain’ ?avoring
for reduced iron. The resulting product was found to
agents, lubricants,v coloring materials and the like as de
be substantially tasteless.
sired. However, the inclusion of a ?avoring agent in the
Example 8
tablets formulated from the preparations of this invention 15
is not'at allnecessary and might be dispensed with, if
A quantity of 150 g. of a fatty composition containing
desired, since the tablets would be otherwise substantially
about equal parts by weight of stearic and palmitic acid
tasteless.
was melted and maintained at a temperature of 75° C.
'
The instant invention will be better understood by refer~
and 50 g. of ‘ferrous sulfate exsiccated (325 mesh) was
ence to the following examples which are intended for 20 added with stirring. The heated mixture was continuous
purposes of illustration only and are not intended as in
ly stirred until a smooth, homogeneous suspension was
any way limiting the scope of this invention, which is ‘de
obtained. The suspension was passed through heated
?ned in the appended claims.
lines to an external mixing pneumatic nozzle maintained
at a temperature of 100° C. and sprayed through the
Example I
heated nozzle into a chilling chamber containing circu
A quantity of 150 g. of Emersol>132 containing about
lating air at 25° C. The resulting product was found to
49% by weight of stearic acid, 50% palrnitic acid and
1% myristic acid was melted and maintained at a tern-v
perature of 70° C. and 50 g. of reduced iron (about 200
mesh) was added with stirring. The heated mixture was. 30
be substantially tasteless.
Example 9
A quantity of 450 g. of Emersol 132 was melted by
heatingto a temperature of 75° C. To the resulting
continuously stirred until a smooth, homogeneous suspen
sion was obtained. The suspension was passed through
heated melt was added 450 g. of ferric pyrophosphate
heated lines to an external mixing pneumatic nozzle main
- soluble (about 200 mesh) with constant stirring. The
tained at a temperature of 100° C. and sprayed through
mixture was stirred until a smooth, homogeneous sus
the heated nozzle into a chilling chamber containing cir-v 35 pension was obtained. The suspension Was passed
culating air at 25 ° C. The resulting product was found
through heated lines to a spinning disc maintained at
to be'substantially tasteless.
>
100° C. and atomized into a chilling chamber containing
circulating air at 23° C. The resulting product was found
Example 2
to be substantially tasteless.
A quantity of 500 g. of Emersol 132 was melted by 40
Example 10
heating to a temperature of 70° C. To the resulting heat
A quantity of 450g. of Emersol 120 containing about
ed melt was added 500 g. of reduced iron (about 200
41% by Weight of stearic acid, 51% palmitic acid, 2%
mesh) with constant stirring. The mixture was stirred
myristic acid and 6% oleic acid was melted by heating to
until a smooth, homogeneous suspension was obtained.
The suspension was passed through heated lines to a spin4 45 a temperature of 75° C. To the resulting heated melt
was added 450 g. of ferric pyrophosphate soluble (about
ning disc maintained at 100° C. and atomized into a chill
200 mesh) with constant stirring. The mixture was
ing chamber containing circulating air at 23° C. The re
stirred until a smooth, homogeneous suspension was ob
sulting product was found to be substantially tasteless.
t-ained. The suspension was passed through heated vlines
Example 3
50 to‘ an external mixing pneumatic nozzle maintained at a
temperature of 100" C. and sprayed ‘through the heated
The procedure of Example 2 was followed except that '
'
nozzle
into a chilling chamber containing circulating air
Emersolv 140 containing about 27% by weight of stearic
at 25° C.
acid, 70% palmitic acid, 1% myristic acid and 2% oleic
acid was substituted for Emersol 132. The product was
found to be substantially tasteless.
Example 4
The resulting product was found to be sub
stantially tasteless.
55
~
'
Example 11
__ The procedure of Example 10 was followed except that
Emersol 110 containing about 39% by weight of stearic
A quantity of 120 g. of Emersol 132 was melted and
acid, 48% palmitic acid, 2% myristic acid, 10% oleic
maintained at a temperature of 83° C. and 60 g. of fer 60 acid and 1% linoleic acid was substituted for Emersol
120. The product was found to be substantially tasteless.
rous sulfate exsiccated (325 mesh) was added with stir
ring. The heated mixture was continuously stirred until
Example 12
a smooth, homogeneous suspension was obtained. The
suspension Was passed through heated lines to an external
a A quantity of 120 g. of Emersol 132 was melted and
mixing pneumatic nozzle maintained at a temperature of 65 maintained at a temperature of 70° ‘C. and 60 g. of fer
100° C. and sprayed through the heated nozzle into a
rous gluccnate (about 200 mesh) was added with stir
chilling chamber containing circulating air at 23° C. The
ring. -The heated mixture was continuously stirred until
resulting product was found to be substantially tasteless.
a smooth, homogeneous suspension was obtained. The
Example 5 '
suspension was passed through heated lines to an ex
70 ternal mixing pneumatic nozzle maintained at a tempera
ture of 100° C. and sprayed through the heated nozzle
The procedure of Example 4 Was followed except that
into a chilling chamber containing circulating air at
75 g. of Emersol 132 and 75 g. of ferrous sulfate exsic
. 25° C.. The resulting product was found to be substan
cated (325 mesh) were used. As in the preceding ex
tially tasteless.
amples the resulting product was found to be substantially
tasteless.
'
75 Various changes and modi?cations of the invention can
3,035,985
6
be made, and to the extent that such variations incorpo
rate the spirit of the instant invention, they are intended
to be included within :the scope of the appended claims.
What is claimed is:
l. A chewable tablet preparation comprising a phar
maceutically and medically acceptable iron composition
and, as ‘a coating for particles thereof, a pharmaceutically
and medically ‘acceptable fatty composition having a melt
ing point of ‘at least 45 ° C. and comprised essentially of a
mixture of saturated fatty acids having from 14 to 18 10
carbon ‘atoms, said preparation being palatable when
chewed.
2. The preparation of claim 1 wherein ‘the fatty com
position is comprised of a mixture of saturated fatty
acids having from 14 ‘to 18 carbon atoms and up to about 15
11% by weight of an unsaturated ‘fatty acid selected from
the group consisting of oleic ‘acid, linoleic acid and mix
tures thereof.
3. The preparation of claim 1 wherein the fatty com
position is essentially a mixture of stearic acid and pal
mitic acid.
4. The ‘preparation of claim 1 wherein the fatty com
position is essentially a mixture of about equal parts
by weight of stearic acid ‘and palmitic acid.
References Cited in the ?le of this patent
FOREIGN PATENTS
285,091
543,309
Great Britain ____ .._i__i_.._ June 10, 1929
Great Britain _________ __ Feb. 19, 1942
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