Note : Les descriptions sont présentées dans la langue officielle dans laquelle elles ont été soumises.
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CAPSULE SHAPED TABLETS
This invention relates to tablets and particularly
to film coated capsule shaped tablets.
Dispensing pharmaceutical products as powders and/
or granules contained in gelatin capsules has gained wide
acceptance in the pharmaceutical industry. Gore recently,
consumers of over-the-counter (OTC) drugs have also demon-
striated a preference for taking these OTC drugs as powders
or granules in a gelatin capsule. However, the recent
rash of cases of tampering with OTC drugs in gelatin
capsules has presented the pharmaceutical industry with a
serious problem. On the one hand, these powdered drugs in
a gelatin capsule are a highly acceptable dosage form and
yet there are distinct dangers inherent in this kind of a
dosage form, particularly for pharmaceutical products sold
OTC.
It has now been found that this dilemma can be
alleviated by forming a powdered and/or granular mix con-
twining one or more pharmaceutical agents into a tablet
having a true capsule shape live. having body and cap
portions in which the outside diameter of the cap portion
is greater than the outside diameter of the body) and when
preferably applying a film coating to the capsule shaped
tablet which simulates both the appearance and function of
the gelatin capsule.
It is accordingly an object of an aspect of the
present invention to provide a tamper proof pharmaceutical
dosage form having the simulated form and function of a
capsule.
It is an object of an aspect of the present invent
lion to provide a tamper proof dosage form in which a mix
of materials containing one or more pharmaceutically active
ingredients is formed into a capsule shaped tablet having
Atari capsule shape and preferably then coating the
I
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capsule shaped tablet with a film forming agent to Sims-
late the appearance and function of a gelatin capsule.
An aspect of the invention is as follows:
As an article of manufacture of pharmaceutical
dosage form comprising a capsule shaped tablet contain-
in at least one pharmaceutically active ingredient; said
capsule shaped tablet having a cap portion and a body
portion which are physically bound to each other to form
a unitary tablet; said cap portion having a larger out-
side diameter than said body portion whereby a lip informed at the juncture of said cap portion and said body
portion to give said tablet the appearance of a true
capsule.
Other and more detailed objects of this invent
lion will be apparent from the following description drawings and claims.
In the attached drawings 7 in which the same
numerals designate the same structure in the various views:
Fig. 1 is a top plan view of a film coated capsule
shaped tablet embodied in the present invention, part of
the coating being shown as removed to expose the under-
lying tablet.
Fig. 2 is a side elevation of the film coated
capsule shaped tablet shown in Fig. 1.
Fig. 3 is an end view of the film coated capsule
shaped tablet shown in Fig. 2 as viewed prom the right
side of Fig. 2.
Fig. 4 is a cross-sectional view of the coated
tablet shown in Fig. 2 taken along line 4-4.
Forming a tablet into a cylindrical dosage form
and providing this with a coating is known in the prior
art. Typical examples of tablets of this character are
shown in the Physicians Desk Reference, Thea Edition,
1980, pg. 434 see T~ERAGRAN tablets). These, however,
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do not have the appearance of a true capsule having a
cap and body portion nor do they simulate the function
of a gelatin capsule.
Referring to the drawings in which the same
parts in the various views have the same designation,
the film coated capsule shaped tablet is shown general-
lye at 1. This comprises a cap portion 3 and a body
portion 5. Film coated tablet 1 is formed by compress-
in a powdered or
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granular mixture containing pharmaceutical ingredients into
a capsule shaped tablet 7 shown in cross section in Fig. 4.
The profile of tablet 7 (albeit film coated) is
seen in Fig. 1 and comprises cap portion 3 which is physically
S bound to a body portion 5 to form a unitary tablet. The
outer diameter of cap portion 3 is greater than the outer
diameter of body portion 5 along a major portion of their
respective long ayes. Because of these dimensions, a lip 9
is formed at the juncture of cap portion 3 and body
portion 5. This gives the tablet the appearance of a true
capsule.
The dimensions of tablet 7 may vary somewhat. In
general, however, the overall length will be in the range
ox from about 11 mm. to about 22 mm. with the preferred
length being from about 16 mm. to about 19 mm.
The outer end 11 of cap portion 3 and the outer
end 13 of body portion 5 will have curved profiles 50 as to
simulate a capsule. The radius of curvature of these end
portions may vary somewhat. Usually, however, the radius
of curvature of end 11 will be from about 2.8 mm to about
3.20 mm.; the radius of curvature for end 13 will also be
from about 2.8 mm to about 3.2 mm.
As indicated above, the outside diameter of cap
portion 3 will always be a little greater than the outer
diameter of body portion 5. Generally, the cap portion 3
will have a diameter of from about 5.3 mm to about 8.5 mm
and preferably from about 6.9 mm to about 7.6 mm; whereas,
the body portion 3 will have an outside diameter from about
5.1 mm to about 8.2 mm, the preferred diameter being from
about 6.6 mm to about 7.3 mm. For the most part, the
outside diameter of cap portion 3 will be from about 0.05 mm
to about 0.30 mm greater than the outside diameter of body
portion 5. This preferred difference is from about 0.125 mm
to about 0.210 my
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In preparing the capsule shaped tablets in accord
dance with the present invention, a granulation or other
compressible powdered material is compressed in an appear-
privately shaped die between appropriately shaped upper and
S lower die punches. These punches and dies are designed
to form a tablet having the configuration shown in Figs. 1
through 3. It is advisable during this compression process
to stop the die punch martins or edges of the upper and
lower tablet punches from coming in contact with each other
since this would tend to destroy the punches. The consequences
of this procedure i.e. halting the compression before the
die punch margins meet is to form a slightly elevated band 4
around the longitudinal equator of tablet 1.
The pharmaceutically active ingredients that may be
contained in the tablets of the present invention can be any
of a large variety of materials. The only limitation on
this material is that it is able to be incorporated into a
mixture that is capable of being tabulated. By way of
example of active pharmaceutical ingredients that may be
incorporated in the present tablets, there may be mentioned
analgesics, decongestants, antihistamines, antitussives,
antacids, gastric protestants, appetite suppressants,
bronchodilators, hematinics, sleep aids, sleep suppressors,
vitamins, laxatives, antibiotics, antispasmodic, etc. and
mixtures thereof. It is particularly useful in conjunction
with such therapeutically active materials as aspirin,
acetaminophen; combinations of aspirin and acetaminophen;
combinations of aspirin with buffers, combinations of acetamino-
pen, phenylpropanolamine HCl~chlorphaniramine Malta,
dextromethorphan Her; combinations ox aspirin and phenol-
ephrine Hal; combinations ox aspirin, acetaminophen,
salicylamide and caffeine; the combination of acetaminophen
and pyrilamine Malta; the combination of aspirin, phenol-
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propanolamine and chlorpheniramine Malta; caffeine vitamin combinations, etc.
In addition to the pharmaceutically active ingredients
described above, the tablets of the present invention may
also contain other conventional tablet additives and aids.
These include such ingredients as granulating agents,
fillers, lubricating agents, disintegrants, surface active
agents, coloring agents, flavoring agents, glidents, etc.
The capsule shaped tablets of the present invention
may be prepared in a variety of ways. The procedure
may follow one or a combination of several well established
methodologies such as:
(a) direct compression from primary powder mixtures
or from granules which are also prepared by dry compaction; or
(b) wet granulation utilizing a solution of a
powder binder which is mixed with the drug ingredient plus
excipients to produce agglomerates or granules. The granules
are subsequently dried and sized into a blend suitable for
compression.
In any event, the final formation of the compressed tablet
entails the use of well known tablet compressing machines
which, by utilizing steel punches and dies and the applique-
lion of high pressures, compress the powder mixture and/or
granulation into a tablet of a specific shape or design as,
for example, shown in Figs. 1 through 3.
As indicated above, a feature of the present invention
is to coat the capsule shaped tablet with a film forming
polymeric substance which will simulate the appearance and
function of a gelatin capsule. A number of film forming
materials are known in this art which will serve this purpose.
By way of example, the following may be mentioned: methyl-
cellulose, hydroxypropyl methyl cellulose, PUP (Pavane),
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ethyl cellulose (Ethocel 10 CUPS), EUDRAGIT E 30D, ~.UDRAGIT L 30D,
*PHARMACOAT 606 6CPS, OPADRY, COTERIE, cellulose acetate
phthlate. However, the film forming polymers of choice
are hydroxypropyl methyl cellulose 5-15 cups, PHARM~COAT
6 CUPS (Shunts Co.) alone or in combination with ethyl-
cellulose 10 CUPS and PUP.
The thickness of the coating of film forming polymer
that is applied to the capsule shaped tablet of this invent
lion may vary. The only essential limit is that it be able
to simulate the appearance and function of a gelatin capsule.
In the case where quick absorption of the active pharmacy-
tidal agents contained in the tablet is desired, this will
be taken into account in determining the thickness of the
film coating. Visually, the thickness ox the polymer coating
on the capsule shaped tablet will be within the range of
from about .0127 mm to about 0.127 mm with the preferred
range being from about .025 mm to about .075 mm.
The coating of film forming polymer may be applied
to the capsule shaped tablets according to the present
invention in a number of ways. Visually, it will be applied
using a solution or suspension of the film forming polymer
in a solvent. Generally, the film forming polymer will be
present in said solvent or suspending medium in the range
of from about 4% to about 15% by weight based on the total
weight of the coating solution or composition. This may
vary with the nature of the solvent system employed. In
non-aqueous systems, the film forming polymer may be present
at a level in the range of from about I to about 6% on
the same weight basis with the preferred level being from
about 4.5% to about 5%. In the case of aqueous solvent
systems, the polymer will usually constitute between about
I to about 15~ by weight based on the total weight of the
coating solution or composition.
* Hydroxypxopyl methyl cellulose viscosity 6 CUPS
. .
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A variety of solvents or solvent systems may be
employed as the carrier for the film forming polymer
during the coating operation. These may be aqueous or
organic solvent systems. By way of example, the following may
be mentioned water; isopropyl alcohol plus ethylene
chloride; methanol plus ethylene chloride, etc.
In applying the film forming polymer coating to
the capsule shaped tablets in accordance with this invent
lion, any Go the known techniques may be employed. The
film coating may be performed using any one of several
types of equipment such as conventional coating pan,
Accela-Cota, Hackett or Wurster air suspension column.
All these equipment should have an exhaust system to remove
dust and solvent or water vapors to facilitate quick
drying.
Spray guns or other suitable atomizing equipment
may be introduced into the coating pans and rigidly fixed
in a desired position to provide spray patterns conducive
to rapid and uniform coverage of the tablet bed. Normally,
heated or cold drying air is introduced o'er the tablet
bed in a continuous or alternate fashion with a spray
cycle to expedite drying of the solution.
The coating solution may be sprayed by using
pneumatic or hydraulic spray pump system in a continuously
or intermittent spray-dry cycle which is controlled by the
use of timers, punch tapes or solenoid valves. The type
of spray application usually depends on the drying efficiency
of the coating pan.
In most cases, the coating material is sprayed
until the tablets are uniformly coated and the desired
increase in weight is achieved to impart the required coat-
in properties and appearance to the tablet core.
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Many different types of coatings may be applied
such as enteric; slow release or rapidly dissolving type
for fast acting tablets.
The polymeric film coating applied to the capsule
shaped tablets according to the present invention is
designated as 6 in the drawings and is best seen in Figs.
1 and 4. In Fig. 1, the cage of the film coating 6 is
seen; a portion of this coating having been broken away
to expose the underlying tablet 7. In Fig. 4 film
coating 6 is shown in cross section. The relative
thickness of coating 6 is somewhat exaggerated so that
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The following Examples are given to further thus-
irate the present invention. It is to be understood, however,
that this invention is not limited thereto.
EXAMPLE 1
Uncoated Capsule Shaped Buffered Aspirin
Tablets (Tablet Cores PUP 873C-01-74)
A batch (46,285) two-layer buffered aspirin tablets
is prepared as hollows:
Dosage Unit
amity. Item % Total
mg/tab No. _ Ingredients Layer Tab
Mayer I (aspirin
granulation)__ _
324.000 1. Aspirin 80 mesh 84.749 35.982
1557.348 2. Starch, corn 15.001 6.369
3. Sodium laurel
0.956 sulfate, pros. buffered 0.250 0.106
382.30-4 Libya (42.457)
Layer II (buffer
granulation
225.000 4. Magnesium carbonate 24.987
200.000 I Calcium carbonate 22.211
6. Starch, corn (as 10%
25.000 starch paste 4.995 2.776
2548.000 7. Starch, corn 9.590 5.331
2.500 8. Castor oil, hydrogenated 0.500 0.278
powder
9. Water, deionized
500.000 100.000 (55.583)
30%82.804 98.04-0
Procedure:
Layer I (Granulation)
Granulated without further modification.
Layer II (Granulation)
351. Blend 4 & 5 and granulate with 6, aiding additional
water as required.
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2. Pass wet mass through Tornado Mill (5/16"
screen) dry in fluid bed dryer.
3. Pass dry granulation through Oscillator (10 mesh
screen, 0.059" opening).
4. Add 7 & 8, blend well.
Granulations for Layers I and II are fed sequentially
into a tablet die provided with a lower tablet punch. The
granulations are then compressed by an upper tablet punch
to form a two-layer tablet. The tablet die and tablet
punches are tooled to form a capsule shaped tablet shown in
Figs. 1 to 3 of the drawings. The specifications for this
tablet are as follows:
Punch: Cap. 281" x .750" x .060"
Weight: 882.804 my. CORES
Thickness: 0.255" + 0.005"
Hardness: 14-16 SCUM (Heberlein)
Disintegration: US Basket Asp., Water
37C - 35-45 sec.
EXAMPLE 2
Film Coated Capsule Shaped Buffered Aspirin
Tablets
A batch of tablets (11,330) prepared according to
Example 1 above were film coated using the composition and
process described below.
sty
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Dosage Unit % ox %
Amt. Item Film Total
grab No. Ingredients Coating Tab
882.804 Part I Tablets
from Example 1 (98.0357)
Part II Film Coating
(216.623)* 10. Ethylene chloride *
11. Hydroxypropyl methyl-
cellulose E-15
10 11.931 Premium 67.452 1.3249
~111.714)~ 12. Methanol *
1.326 13. "Plasticizer
Blend" *** 7.497 0.1473
4.381 14. Opaspray~- Yellow
K-1-2184 contain-
in 36.72% solids
in AYE alcohol*) 24.768 0.4865
15. "Polishing Wax"
(Carnauba Wax
200-050 powder) 0.283 0.0056
17.688 100.000 1.9643
-900.~92 100.0000
* does not add to tablet weight
Dosage Unit of %
Amt. Item Film total
mq/tab No. Ingredients Coating Tax
***"Plasticizer Blend"
Composition
0-707 Propylene glycol 3.9971 0.0785
0.266 Mineral oil, 55-65
SWISS 1.5038 0.0296
0.353 Tweet 80 1 9957 0.0392
1.326 7.4966 0.1473
Preparation:
1. Blend propylene glycol with Tweet 80 in a stain-
less steel container using lightening mixer.
2. Add mineral oil 55-65 SUP to the above blend and
mix well.
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Part II - Film Coating
Preparation:
1. Disperse item 11 in item 10 (2.454 kilos) using
tightening mixer, then add item 12 (1.266 Gyms) to make clear
solution.
2. Add items 13 and 14 (135.2 Gym), mix well to
make homogeneous color suspension.
Application:
1. Place tablets in coating pan with baffles and
exhaust. Heat to 42-45 C.
2. Film coating solution is sprayed through a
spray gun while drying until all of the solution is sprayed.
3. Tablets are cooled to room temperature in the
coating pan with exhaust.
Polishing:
Polish tablets by sprinkling item 15 in pan, mix
5 minutes.
Specifications for the coated tablets prepared in
accordance with this Example are as follows:
Weight: 900.492 my.
Thickness: 0.262" + 0.005"
Disintegration: US Basket Asp., Water 37 C I min.
EXAMPLE 3
Film Coating Capsule Shaped Tablets Using
Aqueous Film Coating
Capsule shaped tablets prepared in accordance with
Example 1 are film coated with the coating composition
described below. The coating procedure is essentially the
procedure given in Example 2.
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Aqueous Film Coating - 12.5% Solids: Of 3096-18
Ingredients Gms/6000 gyms % w/w
1. Water Do 3200 53.334
2. Methuselah E-5 premium * 480 8.000
S 3. PUP 93 1.550
4. Sodium laurel sulfate 20 0.333
5. Water Do 2050 34.167
6. Propylene glycol 80 1.333
7. Mineral oil - light 2 0.033
8. Tweet 80 5 0.083
9. Color gone. C&W blue 70 1.167
6000 100.000
Add 1 gym Anti foam A emulsion if required to prevent foaming
Process for preparing Aqueous Film Coating Of
3096-18
Dissolve 3 4 in hot water - item 1
Add 2 while water is hot - hydrate completely
Add item 5 - cool to room temperature
Mix 7, 8 and 9 together - mix well
Add to coating solution
Mix well - slowly to avoid foam
EXAMPLE 4
-
Film Coating Capsule Shaped Buffered Aspirin
Tablet with Three Way Polymer Rapid Release Film
Coating System
__ .
Capsule shaped tablets prepared in accordance with
Example 1 are film coated with the composition described below.
The coating procedure is essentially the procedure given in
Example 2.
* Methyl cellulose
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Formula Of 1822-36
Ingredients % w/w
Ethylene chloride
Methuselah 15 cups* 1.50
Ethocel 10 cups 1.50
PUP 1.50
Methanol 30.00
Sodium laurel sulfite
Magnesium carbonate
Propylene glycol 0.75
Mineral oil, Lotte
Tweet 80 0.25
Opaspray Yellow K-1-2184 2.75
100. 00
EXAMPLE 5
Uncoated Capsule Shaped Acetaminophen
Tablets (Formula Of 3096-36)
An acetaminophen mixture was prepared having the
following formula:
Ingredients tabulate
Acetaminophen powder
PUP 5.00
Corn starch 50.55
Starkey acid 2.00
Total tablet wt. 557.55
This mixture was used to prepare uncoated capsule shaped
acetaminophen tablets using essentially the same tabulating
procedure described in Example 1. The specifications for
these tablets are as follows:
* Methyl cellulose
3~2Z3Z~9
Thickness: cap portion 0.253"; body portion
0.231"
Hardness: ~18 to 22 SCUM
Disintegration: less than 10 minutes
S Friability 0~22~
EXAMPLE 6
Aqueous Film Coated Capsule Shaped
Acetaminophen Tablets (Formula Of 3096-41
The uncoated tablets prepared in accordance with
Example 5 are film coated using the following coating
composition:
Ingredients mg/tablet
Uncoated core tablet
above toe 3096-36)557.550
PUP 2.041
Hydroxylpropylmethyl-
cellulose, 5 cps10.883
Propylene glycol 1.496
Arlacel~- 20 0.812
Tweet - 20 0.612
Mineral oil, Lotte
Color, soluble Dow
Total tablet wt. 574.278
The coating procedure is essentially thaw described in
Example 2. These tablets have the following specifications:
Thickness: cap portion ~0.255"; body portion
0.233
Disintegration: less than 12 minutes
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Although the invention has been described with
reference to specific forms thereof, it will be understood
that many changes and modifications may be made without
departing from the spirit of this invention.
