U.S. patent application number 11/002025 was filed with the patent office on 2005-05-05 for edible pga coating composition.
This patent application is currently assigned to FMC Corporation. Invention is credited to Augello, Michael.
Application Number | 20050095272 11/002025 |
Document ID | / |
Family ID | 27752691 |
Filed Date | 2005-05-05 |
United States Patent
Application |
20050095272 |
Kind Code |
A1 |
Augello, Michael |
May 5, 2005 |
Edible PGA coating composition
Abstract
An edible, hardenable coating composition is disclosed which
comprises high levels of low viscosity propylene glycol alginate
and a surfactant, which may additionally contain a filler, a
pigment, and optionally a small amount of a secondary film former
and/or a strengthening polymer. The coating composition of the
present invention may be applied to pharmaceutical and veterinary
solid dosage forms, confectionery, seeds, animal feed, fertilizers,
pesticide tablets, and foods and provides an elegant prompt release
coating which does not retard the release of active ingredients
from the coated substrate.
Inventors: |
Augello, Michael; (Marlboro,
NJ) |
Correspondence
Address: |
WOODCOCK WASHBURN LLP
ONE LIBERTY PLACE, 46TH FLOOR
1650 MARKET STREET
PHILADELPHIA
PA
19103
US
|
Assignee: |
FMC Corporation
|
Family ID: |
27752691 |
Appl. No.: |
11/002025 |
Filed: |
December 2, 2004 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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11002025 |
Dec 2, 2004 |
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10077338 |
Feb 15, 2002 |
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10077338 |
Feb 15, 2002 |
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09994252 |
Nov 26, 2001 |
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6699315 |
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60284778 |
Apr 19, 2001 |
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60253406 |
Nov 28, 2000 |
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Current U.S.
Class: |
424/439 ;
106/162.8; 106/205.01; 106/205.6; 106/205.9 |
Current CPC
Class: |
C08L 2666/26 20130101;
A23V 2200/22 20130101; A23V 2250/5026 20130101; A23V 2250/1842
20130101; A23V 2200/22 20130101; A23V 2250/5026 20130101; A23V
2250/1842 20130101; A23V 2250/5114 20130101; A23V 2250/612
20130101; A23G 2200/00 20130101; C08L 71/02 20130101; A23V 2002/00
20130101; C08L 2666/02 20130101; A23P 20/105 20160801; A61K 9/2072
20130101; A23V 2002/00 20130101; C08L 5/00 20130101; C08L 1/284
20130101; C08L 3/02 20130101; A23V 2002/00 20130101; C09D 105/06
20130101; A23G 3/343 20130101; C09D 105/04 20130101; A23G 2200/00
20130101; A61K 9/282 20130101; C09D 105/04 20130101; A23G 3/343
20130101; C09D 105/06 20130101; A61K 9/286 20130101 |
Class at
Publication: |
424/439 ;
106/205.01; 106/205.6; 106/205.9; 106/162.8 |
International
Class: |
A61K 009/36; C09D
101/26 |
Claims
1. An edible, hardenable, prompt release coating composition
comprising 55% to 85% of propylene glycol alginate and up to 10% of
a surfactant, wherein the propylene glycol alginate is a primary
film former of the composition and such that a 1% aqueous solution
thereof has a viscosity in the range of about 1 to 500
mPa.multidot.s at 25.degree. C.
2. (canceled)
3. The coating composition of claim 1, wherein said surfactant is
lecithin.
4. The coating composition of claim 3, further comprising at least
one of a filler and a pigment.
5-12. (canceled)
13. A dry coating composition comprising a dry blend of the coating
composition of claim 1.
14. A wet coating composition comprising an aqueous dispersion of
the coating composition of claim 1.
15. (canceled)
16. The composition of claim 1 wherein the film forming polymer
consists of propylene glycol alginate.
17. An edible, hardenable, prompt release coating composition
comprising 55% to 90% of propylene glycol alginate and up to 10% of
a surfactant, wherein the propylene glycol alginate is the primary
film former of the composition and such that a 1% aqueous solution
thereof has a viscosity in the range of about 1 to 500
mPa.multidot.s at 25.degree. C.
Description
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation in part of U.S. patent
application Ser. No. 09/994,252, filed Nov. 26, 2001, which claims
the benefit of U.S. Provisional Application No. 60/284,778, filed
Apr. 19, 2001; U.S. Provisional Application No. 60/268,608, filed
Feb. 14, 2001; and U.S. Provisional Application No. 60/253,406,
filed Nov. 28, 2000.
FIELD OF INVENTION
[0002] This invention relates to edible, hardenable prompt release
coating compositions comprising a film forming amount of low
viscosity propylene glycol alginate that serves as the principle,
primary or sole film former of the coating composition. The
coatings of the present invention can be applied to pharmaceutical,
including neutraceutical, and veterinary solid dosage forms, such
solid substrates such as seeds, animal feed, fertilizers, pesticide
tablets and granules, and also to confectionery and foods. They are
readily dispersed in aqueous media, and, when applied as a coating,
provide high lustre coatings which do not retard or extend release
of active ingredient from a coated substrate.
BACKGROUND OF THE INVENTION
[0003] It is a common practice to coat pharmaceutical and
veterinary tablets to obtain several advantages. Among these are to
improve the surface characteristics of tablets to make them easier
to swallow, to reduce the absorption of water or moisture which can
potentially degrade the active ingredient or promote some other
undesirable change in the tablet structure, and simply to make a
more elegant appearing tablet.
[0004] Another very important function of a pharmaceutical or
veterinary tablet coating is to improve the integrity of the tablet
itself. Uncoated tablets are often subject to being abraded or
chipped, causing a loss of active ingredient in the process. More
dramatically, they may break into two or more pieces. One measure
of a useful coating is its ability to prevent any of these physical
degradations of tablet structure. The effectiveness of a coating
material to prevent abrading, chipping, or breakage of the tablet
is determined by friability testing.
[0005] Confectionery and foods may be coated with a formulation to
preserve the confection or food from deteriorating by contact with
the oxygen and the moisture in the atmosphere. Coatings also can
provide improved appearance and desirable organoleptic properties
to the food as well as preventing loss of flavor.
[0006] Seeds may be coated to preserve the viability of the seeds
by protecting against moisture. They may also be coated as a means
for increasing particle size to facilitate mechanical planting. A
dye can be included in the coating formulation to identify the
seeds as to quality, type, or some other designation. Frequently, a
pesticide, e.g., a fungicide, is incorporated into the coating
formulation to protect both the seed itself and the seedling that
results from germination of the seed. In all cases, this coating
must not decrease the viability of the seeds or interfere with
germination when the seeds are planted in the soil.
[0007] Animal feed may be coated to improve its flowability,
appearance and its resistance to powdering or dusting. In such
applications, the coating may be formulated to include vitamins,
hormones, antibiotics, or the like, to benefit the livestock which
will consume the feed.
[0008] Fertilizers, in either granular or tableted forms, may be
coated to retain the integrity of the form and, especially, to
protect the fertilizer from moisture which can cause agglomeration
during storage, which could make rapid, even application to the
soil difficult or inconvenient.
[0009] Coating of tableted pesticide formulations serves to
maintain the integrity of the tablets or granules until they are
placed in water where they rapidly disintegrate, forming a solution
or slurry to be applied to the soil or plants. A second, and
equally important, function of the coatings on tablets containing
pesticides is to prevent human contact with the pesticide, thereby
increasing safety for those handling and applying the
pesticide.
[0010] In the preparation of a coating formulation to be sprayed,
the film former is usually dissolved or dispersed in a solvent, for
example, water, along with the other ingredients of the
formulation. In aqueous systems, since many polymers require
significant time to become fully hydrated, the coating formulation
must frequently be prepared in advance of the time it is to be
applied to the tablets. A common procedure is to prepare these
coating formulations the day preceding the coating operation in
order to assure adequate hydration of the polymers used in
them.
[0011] A particular disadvantage of coatings based primarily on
HPMC is that the coating may harden over time and therefore
increase tablet disintegration times. An increase in disintegration
time delays the bioavailability of the active ingredient at least
in proportion to the increase in disintegration time. Many other
agents commonly used in coating compositions are also known to
delay release of pharmaceutical agents, such as enteric coatings
which use polymeric film forming materials which are insoluble in
water, or gastric fluid, some of these being specifically selected
to by-pass both the stomach and small intestine and provide colonic
release.
[0012] The coatings of this invention meet U.S. Pharmacopoeia
standards for rapid or immediate dissolution (U.S.P. monograph 23)
of active ingredients from tablets or other solid dosage forms
coated with them. They provide prompt release or dissolution
consistent with the release rates which is normally obtained with
the uncoated tablets or other substrates. Thus, they do not
adversely impact or retard release of active ingredients from a
substrate coated with them. Further, the coatings of this invention
are readily dispersed and rapidly hydrated in aqueous media for
application to a coating substrate, and provide elegant coatings
which have all the benefits of coatings now in commercial use
without the drawbacks that are common to them.
SUMMARY OF THE INVENTION
[0013] It has been found that these and other advantages may be
achieved in accordance with the present invention by a coating
composition which comprises a low viscosity propylene glycol
alginate as the principle or only film-forming component of the
coating composition, preferably in combination with a surface
active agent. The coating composition of the present invention
utilizes as the primary film former a low viscosity propylene
glycol alginate (PGA), a 1% aqueous solution of which has a
viscosity in the range of about 1 to 500 mPa.multidot.s at
25.degree. C. The PGA preferably is used in combination a surface
active agent, and optionally such additional ingredients as a
filler, a coloring agent, or combination of these, and may also
contain a small amount of a secondary film former and/or a
strengthening polymer as an additional ingredient. More
specifically, the present invention provides a prompt release,
edible, hardenable PGA coating composition, as well as dry coatings
and aqueous dispersions thereof and solid dosage forms coated
therewith.
DETAILED DESCRIPTION OF THE INVENTION
[0014] For purposes of this application, the term "edible" is
intended to mean food or pharmaceutical grade materials which are
approved by regulatory authorities for use in pharmaceutical or
food applications. The term "hardenable," used to describe the
coating compositions of this invention, is intended to include only
those coating compositions that are capable of being dried from an
aqueous solution or dispersion thereof into a solid coating which
resists abrasive forces, i.e. a hardened coating, as distinguished
from those "enrobing" coatings on confections which set up into a
soft coating that can be handled and packaged but which do not
resist abrasive forces significantly. The terms "immediate,"
"rapid," or "prompt," as applied to dissolution rates or times for
the coating compositions of this invention or tablets coated with
the compositions of this invention, mean that the coatings of this
invention meet U.S. Pharmacopoeia standards (U.S.P. monograph 23)
for rapid or immediate dissolution of active ingredients from
tablets or other solid dosage forms coated with them. Thus, they
provide prompt release or dissolution consistent with the release
rates which is normally obtained with the uncoated tablets or other
substrate. They do not, when placed in water or ingested, adversely
impact or retard release or dissolution of tablets or other dosage
forms coated with them. Coatings made in accordance with the
present invention are substantially or completely disintegrated
and/or dissolved within less than 10 minutes after being ingested
or placed in aqueous media. These definitions are intended to apply
throughout this application unless a contrary meaning is clearly
indicated.
[0015] Propylene glycol alginate provides important film-forming
characteristics required to provide an elegant coating which is
particularly useful in, for example, coating pharmaceutical and
veterinary tablets, caplets, granules, and spheres which contain
active ingredients which require release promptly after being
placed in aqueous media or ingested.
[0016] Propylene glycol alginate by itself is known to be a film
forming hydrocolloid when an aqueous dispersion thereof is spread
on a surface and allowed to dry. However, the film has heretofore
been considered to be too weak for satisfactory coatings. However,
when a low viscosity propylene glycol alginate is utilized in high
concentrations in combination with a suitable surface active agent,
elegant, high performance coating formulations are provided which
may readily be applied as an aqueous suspension to coating
substrates. The propylene glycol alginate used in the present
invention is a low viscosity propylene glycol alginate which, when
present at 1% in water at 25.degree. C. produces a aqueous solution
having a viscosity in the range of about 1 to 500 mPa.multidot.s.
It has been found that PGA having a viscosity substantially above
about 500 mPa.multidot.s is difficult to formulate into suitable
coatings, requires numerous additives to produce satisfactory
coatings, and tend to be too viscous for practical application to
materials to be coated. Low viscosity propylene glycol alginate is
commercially available as Profoam.RTM. from Pronova and as Duckloid
SLF-3 from Kibun. The low viscosity propylene glycol alginate is
employed in the coating compositions at about 55% to about 100% by
dry weight of the composition, more specifically at about 55% to
about 85% by dry weight of the composition. In another embodiment
of the invention, the low viscosity propylene glycol alginate is
employed in the coating compositions at about 91% to about 100% by
dry weight of the composition.
[0017] Surfactants which are either anionic or nonionic may be used
beneficially in the edible, hardenable coating compositions of the
present invention. Useful surfactants may be, for example, sodium
lauryl sulfate, hydroxylated soy lecithin (lecithin), polysorbates,
and block copolymers of propylene oxide and ethylene oxide. Such
surface active agents may be employed at up to about 10% by dry
weight of the composition. Surfactants such as lecithin assist in
redispersion of the dry composition and improving flowability of
the coating composition during application, assuring a smooth even
coating.
[0018] In addition to PGA and a surface active agent, the balance
of the composition may comprise certain adjuvants which are
commonly utilized in coating compositions, including fillers and/or
pigments for colored coatings, and may include a minor amount of
secondary film former such as carrageenan or HPMC and/or a
strengthening polymer such as hydroxyethylcellulose.
[0019] Fillers suitable for use in the compositions of the
invention include, for example, calcium carbonate, dicalcium
phosphate and carbohydrates, such as starch, maltodextrin, lactose,
mannitol and other sugars, croscarmellose sodium, or
microcrystalline cellulose Of these, maltodextrin has been found
beneficial at about 10% to about 30% by dry weight of the
composition, but the other fillers may be used at these levels.
[0020] Coloring agents and opacifiers may be used in these coating
compositions or added to a suspension thereof, including aluminum
lakes, insoluble pigments, water-soluble dyes, titanium dioxide,
and talc. Such coloring agents may be suitably employed at about 5%
to about 15% by dry weight of the composition. In general such
coloring agents may be utilized in addition to or in lieu of a
filler. As further illustrated in the examples below, the combined
amount of filler and coloring agent may suitably be in the range of
about 10% to about 40% by dry weight of the composition.
[0021] It is also contemplated that certain other additives may be
included in or added to the compositions of this invention.
Depending on the amount of PGA present in the specific formulation,
it may be desirable to include a secondary film former such as
carrageenan and/or a strengthening polymer such as
hydroxyethylcellulose. While such additional additives are
generally not required, they may be utilized if desired at about 3%
to about 12% by dry weight of the composition. A small amount
stearic acid or a salt or ester thereof, and/or a conventional
plasticizer may also be included at these levels to increase gloss
elasticity of the coating. Suitable plasticizers include, for
example, polyethylene glycol, triacetin, dibutyl sebacate.
propylene glycol, sorbitol, glycerin, and triethyl citrate.
[0022] A coating formulation of this invention may be sold as a dry
powder formulation or as a ready-to-use dispersion in water. For
aqueous dispersions it is preferred that these be prepared under
aseptic conditions. Heating the water to an elevated temperature,
for example, 85.degree. C., prior to preparation of the dispersion
has shown that bacteria, mold, and yeast growth are prevented for
at least 48 hours on agar pour plates. Therefore, if the containers
for the dispersion are properly sanitized and then kept closed
after being filled until the dispersion is used, there is little
likelihood of bacteria, mold, or yeast growing in the dispersion.
Alternatively, if a formulation is to be sold as an aqueous
dispersion to be stored for a period of time, a preservative may be
added. A combination of methyl paraben and propyl has been found to
be useful in this regard.
[0023] On a dry weight percentage basis, one embodiment of the
composition of this invention comprises from 60% to 85% of said
propylene glycol alginate, 2% to 10% lecithin, and 10% to 30%
maltodextrin. A second embodiment comprises from about 60% to 85%
of propylene glycol alginate, 2% to 10% lecithin, and 5% to 15%
pigment. Either embodiment may further comprise from 3% to about
12% by dry weight of the composition of a secondary film forming
polymer such as carrageenan or a strengthening polymer such as
hydroxyethylcellulose. Preservatives, such as methyl paraben at
0.75% to 1.50% and/or propyl paraben at 0.075% to 0.15% may also be
present in the formulation.
[0024] The viscosity of the hydrated formulation can be important.
It ideally should be low enough to be pumped to a spray unit
continuously and then sprayed evenly in a useful pattern onto the
substrate being coated. A useful concentration of the dry
ingredients in water on a weight percentage basis, therefore, may
be about 6% to about 15%, advantageously 6.5% to 11%, preferably
about 8% to about 11%. To assure uniformity of the coating
composition, it may be preferable to maintain agitation of the
aqueous dispersion during the entire period of its being sprayed
onto the pharmaceutical or veterinary solid dosage forms,
confectionery, seeds, animal feed, fertilizer, pesticide tablets,
or food.
[0025] The preferred edible, hardenable, prompt release coating
formulations of this invention may generally be prepared and used
according to a simple procedure. Propylene glycol alginate and
other dry ingredients, including, as appropriate for the desired
composition, a surface active agent, a filler, a secondary polymer,
and/or preservatives, are dry blended together to a form dry
coating composition. Addition of edible coloring agents, for
example, a water-soluble dye or a pigment, may precede the
hydration step required to prepare the final coating formulation.
This dry mixture is then added slowly to the vortex of stirred,
purified water. Stirring of this mixture is continued for a
sufficient period to allow all of the components to be fully
hydrated. If a colored coating material is required a water soluble
dye or a pigment may also be added, preferably as a dispersion or
solution, to the hydrated coating composition. Optionally
surfactants, and/or plasticizers may also be added at this stage of
the process.
[0026] In the hydration step, a simple propeller mixer provides
adequate agitation for rapid hydration. The period of hydration may
be as short as 0.5 hours. It may, and preferably should, be longer,
but more than 3 hours is not believed to be necessary. Hydration
can take place at room temperature or at elevated temperatures as
high as 65.5.degree. C. (150.degree. F.), preferably at a
temperature about 48.9.degree. C. (120.degree. F.). The time
required for full hydration and the viscosity of the dispersion are
both considerably reduced when the dispersion is prepared at an
elevated temperature, but coating dispersions prepared at ambient
temperature only require an increase in hydration time and a slight
reduction in solids content to perform completely satisfactorily.
As previously stated, these formulations may be prepared on the day
preceding the coating operation, if that is more convenient;
however, a period of mixing will be required to overcome any
thixotropic behavior of a formulation which sets up during
overnight storage. Unlike coating formulations based primarily on
hydroxyalkyl ethers of cellulose, for example, HPMC, constant
stirring of the propylene glycol alginate-based formulations of
this invention does not need to be continued throughout the coating
procedure, but mixing may continue, if preferred.
[0027] Any commercial spray coater may be used to apply the
coating. Examples of useful coaters are Vector High Coaters
manufactured by Vector Corporation and Accela-Coat manufactured by
Thomas Engineering. Equipment variables which one skilled in the
art can manipulate to provide an elegant coating based on propylene
glycol alginate, include inlet temperature, outlet temperature, air
flow, speed of rotation of the coating pan, and the rate at which
the coating formulation is pumped to the coater. It is important
that the inlet and outlet temperatures be controlled so that they
are high enough to efficiently dry the coating to prevent the
tumbling action of the already-coated tablets from damaging the
newly-applied coating before more coating is applied to the same
tablets.
[0028] The level of coating applied to pharmaceutical or veterinary
dosage forms is preferably between about 0.5% to about 4% by weight
of the uncoated dosage form, more preferably about 2% to about
3.5%, by weight of the uncoated dosage form. This level of coating
will provide an elegant, serviceable coating to a wide variety of
dosage forms. To apply a heavier coating to tablets would not be
economical, and it might adversely affect disintegration of the
tablets or other properties. Too light a coating would not provide
optimal properties normally expected from a coating.
[0029] For confections the coating level should be about 5% to
about 10% by weight of the uncoated confection. Seed coatings
should be in the range of about 3% to about 6% by weight of the
uncoated seeds. Fertilizers and pesticide tablets and granules
benefit from coating of 1% to about 3%, by weight of the uncoated
granules or tablets.
[0030] The coatings of the present invention may be applied
successfully to tablets having wide variety of active ingredients
incorporated therein. For example, it has been reported that
multivitamin tablets are difficult to coat because of the
lipophilic surface properties of the vitamins. Similarly, ibuprofen
is a challenging active ingredient to coat. Tablets comprising both
of these difficult-to-coat active ingredients may be readily coated
with the coating compositions of this invention, providing elegant
tablets. Additionally, the coating have been applied to tablets
which have been debased with letters or a logo without bridging
which would hide, or even obliterate, the debossed design.
[0031] Storage of coated tablets under ambient temperature and
humidity and 40.degree. C. and 75% relative humidity for one to
three months has demonstrated that no significant degradation has
occurred. These tablets have disintegrated within the same length
of time as the same batch of newly coated tablets did, and in each
case provided dissolution rates and times substantially equal to
those of the uncoated tablets used as a substrate for coating. This
is an additional unexpected benefit of the coatings based on
propylene glycol alginate
[0032] All components of the formulation are typically
pharmaceutically acceptable, edible food grade materials.
[0033] The following examples, in which percentages are weight
percent, are provided to demonstrate the method of preparation and
application of these elegant coatings, but they are not intended to
be limiting as to amounts and the type of optional ingredients or
the specific method of application of the tablet coating described
herein.
EXAMPLE 1
[0034] In a Patterson-Kelly twin shell blender were placed 250
grams of low viscosity propylene glycol alginate (Profoam,
Pronova/FMC Corporation) and 10 grams of hydroxylated soy lecithin
(Precept 8120, Central Soya). After the dry components had been
thoroughly blended, the blend was added slowly to the vortex of
3450 grams deionized water which was stirred with a Lightnin'
mixer. The suspension was stirred for 3 hours at ambient
temperature to fully hydrate the composition. To this dispersion
was added 40 grams of Chroma-Kote red liquid dispersion (Crompton
and Knowles). A 24" Acella Comp-U-Coat coater was charged with 12
Kg of ibuprofen caplets. The coater was operated at an inlet
temperature of 40-55.degree. C., an outlet temperature of
35-39.degree. C., and 8-9 rpm. During the spraying, which required
85 minutes, a 2-3% by weight coating, based on the weight of the
caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as Example 1 of
Table 1, below.
EXAMPLES 2 and 3
[0035] In a Patterson-Kelly twin shell blender were placed 292
grams of low viscosity propylene glycol alginate (Profoam,
Pronova/FMC Corporation) and 45 grams of hydroxyethylcellulose 250
L, 22.5 grains of hydroxylated soy lecithin (Precept 8120, Central
Soya), 45 grams of maltodextrin M1 80 (Maltrin M1 80, GPC) and 45
grams of Color Blend Pigment (Croma-tone, Warner Jenkinson). After
the dry components had been thoroughly blended, the blend was added
slowly to the vortex of 5175 grains deionized water which was
stirred with a Lightnin' mixer. The suspension was stirred for 2
hours at ambient temperature to fully hydrate the composition. To
this dispersion was added 40 grams of Chroma-Kote red liquid
dispersion (Crompton and Knowles). A 24" Acella Comp-U-Coat coater
was charged with 12 Kg of ibuprofen caplets. The coater was
operated at an inlet temperature of 53-55.degree. C., an outlet
temperature of 32-39.degree. C., and 8-11 rpm. During the spraying,
which required 63-69 minutes, a 3% by weight coating, based on the
weight of the caplets, was applied. The composition of the coating
and the physical properties of the coated caplets are shown as
Example 2 and 3 of Table 1, below.
EXAMPLE 4
[0036] In a Patterson-Kelly twin shell blender were placed 65 grams
of low viscosity propylene glycol alginate (Profoam, Pronova/FMC
Corporation), 22.5 Crams of hydroxylated soy lecithin (Precept
8120, Central Soya), and 45 grams of maltodextrin M1 80 (Maltrin M1
80, GPC). After the dry components had been thoroughly blended, the
blend was added slowly to the vortex of 1150 grams deionized water
which was stirred with a Lightnin' mixer. The suspension was
stirred for 2 hours at ambient temperature to fully hydrate the
composition. A Vector LDCD 15" coater was charged with 2 Kg of
chlorpheniramine 4 mg tablets. The coater was operated at an inlet
temperature of 74-83.degree. C., an outlet temperature of
34-39.degree. C., and 13-16 rpm. During the spraying, which
required 67 minutes, a 3% by weight coating, based on the weight of
the caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as Example 4 of
Table 1, below.
EXAMPLE 5
[0037] In a Patterson-Kelly twin shell blender were placed 270
grams of low viscosity propylene glycol alginate (Profoam,
Pronova/FMC Corporation), 11.25 grams of hydroxylated soy lecithin
(Precept 8120, Central Soya), and 135 grains of maltodextrin M180
(Maltrin M180, GPC), and 33.75 grams of Pigment Blend (Chroma-tone,
Warner Jenkinson). After the dry components had been thoroughly
blended, the blend was added slowly to the vortex of 5175 grams
deionized water which was stirred with a Lightnin' mixer. The
suspension was stirred for 2 hours at ambient temperature to fully
hydrate the composition. A Vector LDCD 15" coater was charged with
2 Kg of acetaminophen 500 mg caplets. The coater was operated at an
inlet temperature of 52-54.degree. C., an outlet temperature of
32-37.degree. C., and 8-10 rpm. During the spraying, which required
63 minutes, a 3% by weight coating, based on the weight of the
caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as Example 5 of
Table 1, below.
EXAMPLE 6
[0038] In a Patterson-Kelly twin shell blender were placed 247.5
grams of low viscosity propylene glycol alginate (Profoam,
Pronova/FMC Corporation), 22.5 grams of hydroxylated soy lecithin
(Precept 8120, Central Soya), and 112.5 grams of maltodextrin M1 80
(Maltrin M1 80, GPC), 22.5 grams sodium iota carrageenan (FMC
Corporation), and 33.75 grams of Pigment (Whittaker, Clarke &
Daniels). After the dry components had been thoroughly blended, the
blend was added slowly to the vortex of 5175 grams deionized water
which was stirred with a Lightnin' mixer. The suspension was
stirred for 4 hours at ambient temperature to fully hydrate the
composition. A 24" Accela Comp-U-Coat coater was charged with 2 Kg
of acetaminophen 500 mg caplets. The coater was operated at an
inlet temperature of 52-53 OC, an outlet temperature of
33-35.degree. C., and 9-12 rpm. During the spraying, which required
4 hours, a 3% by weight coating, based on the weight of the
caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as Example 6 of
Table 1, below.
1 TABLE 1 Example 1 2 3 4 5 6 Ingredients (% by dry weight)
PGA.sup.1 83.3 65 65 65 60 55 Lecithin.sup.2 3.3 5 7 5 2.5 5
Maltodextrin.sup.3 -- 10 18 30 30 25 Pigment 13.4 10 10 -- 7.5 10
HEC.sup.4 -- 10 -- -- -- -- Iota carrageenan -- -- -- -- -- 5
Caplet Ingredients Acetaminophen X X Ibuprofen X X X
Chlorpheniramine X Coating Weight 3 3 3 3 3 3 (%) Friability (10 0%
0% 0% 0% 0% 0% minutes) Appearance 5 5 5 5 5 5 (shine).sup.5
Initial Dissolution (% @ Time) 15 minutes NT.sup.6 31 34 89 NT NT
30 minutes 69 71 100 45 minutes 92 91 60 minutes 99 99
.sup.1Polypropylene glycol alginate (Profoam .RTM., Pronova/FMC
Corporation) .sup.2Hydroxylated soy lecithin, Central Soya
.sup.3Maltodextrin, Maltrin M180 .sup.4Hydroxyethylcellulose 250L
.sup.55 = excellent; 4 = acceptable; 3 = marginal; 2 = poor; 1 =
Not acceptable .sup.6Not tested
EXAMPLE 7
[0039] In a Patterson-Kelly twin shell blender were placed 90 grams
of low viscosity propylene glycol alginate (Duckloid SLF-3, Kibun)
and 10.00 grams of (Red Iron Oxide, hydrophillic, WCD). After the
dry components had been thoroughly blended, the blend was stirred
with a Lightnin' mixer. The suspension was stirred for 4.5 hrs. at
an ambient temperature to fully hydrate the composition. A 15"
vector LDCS loader was charged with 1.9 kilograms of Acetaminophen
500 milligram caplets. The coater was operated at an inlet
temperature of 74-75.degree. C. An outlet temperature of
34-35.degree. C. and 14-16 RPM. During the spraying, which required
55 minutes, a 3% by weight coating, based on the weight of the
caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as example 7 of
Table 2 below.
EXAMPLE 8
[0040] In a Patterson-Kelly twin shell blender were placed 80 grams
of low viscosity propylene glycol alginate (Duckloid SLF-3, Kibun),
17 grams of polyethylene glycol 8000 (PEG 8000, Union Carbide) and
3.00 grams of Maltodextrin-180 (Maltrin-M-180, Grain Processing
Corporation). After the dry components had been thoroughly blended,
the blend was added slowly to the vortex of 900.0 grams deionized
water which was stirred with a Lightnin' Mixer. The suspension was
stirred for 1 hour at an ambient temperature to fully hydrate the
composition. A 15" Vector LDCS coater was charged with 2.0
kilograms of Acetometaphin. A 15" Vector LDCS coater was charged
with 2.0 kilograms of Acetaminophen 500 milligram caplets. The
coater was operated at an inlet temperature of 73-78.degree. C., an
outlet temperature of 34-39.degree. C., and 13 RPM. During the
spraying, which required 57 minutes, a 3% by weight coating, based
on the weight of the caplets, was applied. The composition of the
coating and physical properties of the coated caplets are shown as
Example 8 of Table 2, below.
EXAMPLE 9
[0041] In a Patterson-Kelly twin shell blender were placed 80.82
grams of low viscosity propylene glycol alginate (Duckloid SLF-3,
Kibun), 10.1 grams of Lactose Anhydrous (Sheffield Corporation) and
9.1 grams of Blue Pigment Blend (Chromatone, Warner Jenkinson).
After the dry components had been thoroughly blended, the blend was
added slowly to the vortex of 1011.0 grams deionized water which
was stirred with a Lightnin' Mixer. The suspension was stirred for
1 hour and 45 minutes to fully hydrate the composition. A 15"
Vector LDCD was charged with 2.0 Kilograms of Ibuprofen 200
milligram caplets. The coater was operated at an inlet temperature
of 66-72.degree. C., an outlet temperature of 32-35.degree. C. and
12-16 RPM. During the spraying, which required 1 hour and 2
minutes, a 3% by weight coating, based on the weight of the
caplets, was applied. The composition of the coating and the
physical properties of the coated caplets are shown as Example 9 of
Table 2, below.
EXAMPLE 10
[0042] In a Patterson-Kelly twin shell blender were placed 65.0
grams of low viscosity propylene glycol alginate (Duckloid SLF-3,
Kibun) and 35.0 grams of Polyethylene glycol 8000 (PEG 8000, Union
Carbide). After the components had been thoroughly blended, the
blend was added slowly to the vortex of 1011.0 grams deionized
water which was stirred with a Lightnin' Mixer. The suspension was
stirred for 1 hour at an ambient temperature to fully hydrate the
composition. A 15" Vector LDCD coater was charged with 1.9
kilograms of acetaminophen 500 milligram caplets. The coater was
operated at an inlet temperature of 73-78.degree. C., an outlet
temperature of 32-35.degree. C. and 12-17 RPM. During the spraying,
which required 54 minutes, a 3% by weight coating, based on the
weight of the caplets, was applied. The composition of the coating
and the physical properties of the coated caplets are shown by
Example 10 of Table 2, below.
EXAMPLE 11
[0043] In a Patterson-Kelly twin shell blender were placed 85.0
grams of low viscosity propylene glycol alginate (Duckloid SLF-3,
Kibun), 5.00 grams of Lactose Anhydrous (Sheffield Corporation) and
10.0 grams of Yellow Lake Blend (Warner Jenkinson). After the dry
components had been thoroughly blended, the blend was added slowly
to the vortex of 1011.0 grams deionized water which was stirred
with a Lightnin' Mixer. The suspension was stirred for 1 hour to
fully hydrate the composition. A 15" Vector LDCD was charged with
1.9 kilograms of Acetaminophen 500 milligram caplets. The coater
was operated at an inlet temperature of 77-80.degree. C., an outlet
temperature of 33-36.degree. C. and 13-17 RPM. During the spraying,
which required 53 minutes, a 3% by weight coating, based on the
weight of the caplets, was applied. The composition of the coating
and the physical properties of the coated caplets are shown as
Example 11 of Table 2, below.
2 TABLE 2 Example 7 8 9 10 11 Ingredients (% by dry weight)
PGA.sup.1 90.0 80 80.82 65.0 85 Maltodextrin.sup.2 -- 3.0 -- -- --
Pigment.sup.3 10.0 -- 9.1 -- 10.0 PEG 8000.sup.4 -- 17.0 -- 35.0 --
Lactose -- -- 10.1 -- 5.0 Anhydrous.sup.5 Caplet Ingredients
Acetaminophen X X X X Ibuprofen X Coating Weight 3 3 3 3 3 (%)
Friability (10 0% 0% 0% 0% 0% minutes) Appearance 5 5 5 5 5
(shine).sup.6 Initial Dissolution (% @ Time) 10 minutes 87.0% 86%
N/A N/A N/A 15 minutes N/A N/A 50.0% N/A N/A 20 minutes 99.0% 97.0
N/A N/A N/A 30 minutes 101.0% 99.0% 84.0% N/A N/A 45 minutes N/A
N/A 96.0% N/A N/A 60 minutes N/A N/A 99.0% N/A N/A
.sup.1Polypropylene glycol alginate (Duckloid SLF-3,
Kibun)(Spectrum Chem, USP/NF) .sup.2Maltodextrin, Maltrin M180
.sup.3Pigment (Whittaker Clarke & Daniels, Warner Jenkinson)
.sup.4Polyethylene Glycol 8000 (Union Carbide) .sup.5Lactose
Anhydrous (Sheffield) .sup.65 = excellent; 4 = acceptable; 3 =
marginal; 2 = poor; 1 = Not acceptable
* * * * *