CA1223209A - Capsule shaped tablets - Google Patents

Abstract

ABSTRACT OF THE DISCLOSURE

A capsule shaped tablet containing a pharmaceutically active ingredient in which the tablet has a cap portion and a body portion physically bound to each other; the cap portion having a larger outside diameter than the body; the tablet may be provided with a coating of a film forming polymer to simulate a hard gelatin capsule dosage form.

Description

232~

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

12Z32~9 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, ~Z3~
-pa-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 ~Z232~

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 ~2232~

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-~23'~

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), 23Z(~

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

. .

~223;~

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.

~'~;23Z~)~

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 I=

~Z3Z~
g 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.

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.

~ZZ3Z~I~

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.

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 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.

~zz~

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.

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.

-SUE

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 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 -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 ~Z~3~

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 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~

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 ~Z;~32~

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.

Claims (22)

The embodiments of the invention in which an exclusive property or privilege is claimed are defined as follows:

1. As an article of manufacture a pharmaceutical dosage form comprising a capsule shaped tablet containing 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 outside diameter than said body portion whereby a lip is formed at the juncture of said cap portion and said body portion to give said tablet the appearance of a true capsule.

2. A capsule shaped tablet according to Claim 1 wherein said tablet is coated with a film forming polymer;
said polymeric film forming coating on said tablet being of sufficient thickness and character so as to simulate the appearance and function of a gelatin capsule.

3. An article of manufacture according to Claim 2 in which said tablet contains at least one analgesic as a pharmaceutically active ingredient.

4. An article of manufacture according to Claim 3 in which said tablet contains ASPIRIN? as a pharmaceutic-ally active ingredient.

5. An article of manufacture according to Claim 3 in which said tablet contains ASPIRIN? and a buffering agent as pharmaceutically active ingredients.

6. An article of manufacture according to Claim 3 in which said tablet contains acetaminophen as a pharma-ceutically active ingredient.

7. An article of manufacture according to Claim 3 in which said tablet contains a combination of ASPIRIN?
and acetaminophen as pharmaceutically active ingredients.

8. An article of manufacture according to Claim 3 in which said tablet contains a combination of acetamino-phen, phenylpropanolamine HCl, chlorpheniramine maleate and dextromethorphan HBr as pharmaceutically active ingredients.

9. An article of manufacture according to Claim 3 in which said tablet contains a combination of ASPIRIN?
and phenylephrine HCl as pharmaceutically active ingred-ients.

10. An article of manufacture according to Claim 3 in which said tablet contains a combination of ASPIRIN?, acetaminophen, salicylamide and caffeine as pharmaceutic-ally active ingredients.

11. An article of manufacture according to Claim 3 in which said tablet contains the combination of aceta-minophen and pyrilamine maleate as pharmaceutically active ingredients.

12. An article of manufacture according to Claim 3 in which said tablet contains the combination of ASPIRIN?, phenylpropanolamine and chlorpheniramine maleate as pharmaceutically active ingredients.

13. An article of manufacture according to Claim 2 in which said tablet contains caffeine as a pharmaceutically active ingredient.

14. An article of manufacture according to Claim 2 in which said tablet contains vitamin combinations.

15. An article of manufacture according to Claim 2 having an overall longitudinal dimension in the range of from about 11 mm to about 22 mm, the outer diameter of said cap portion being in the range of from about 5.3 mm to about 8.5 mm and the outside diameter of said body portion being in the range of from about 5.1 mm to about 8.2 mm.

16. An article of manufacture according to Claim 15 in which the thickness of said coating of film forming polymer is in the range of from about 0.0127 mm to about 0.127 mm.

17. An article of manufacture according to Claim 15 in which the thickness of said coating of said film forming polymer is in the range of from about 0.025 mm to about 0.075 mm.

18. An article of manufacture according to Claim 2 in which said film forming polymer is selected from the group consisting of hydroxypropyl methylcellulose, methylcellulose, ethylcellulose, PVP, cellulose acetate phthlate and mixtures thereof.

19. An article of manufacture according to Claim 18 in which the film forming polymer is hydroxypropyl methyl-cellulose.

20. An article of manufacture according to Claim 18 in which said film forming polymer is a combination of hydroxypropyl methylcellulose and ethylcellulose.

21. An article of manufacture according to Claim 18 wherein said film forming polymer is a combination of hydroxy-propyl methylcellulose and PVP.

22. An article of manufacture according to Claim 18 in which said film forming polymer is a combination of hydroxy-propyl methylcellulose, ethylcellulose and PVP.