U.S. patent application number 17/344790 was filed with the patent office on 2021-10-07 for tablets with improved friability.
This patent application is currently assigned to TOWER LABORATORIES LTD. The applicant listed for this patent is TOWER LABORATORIES LTD. Invention is credited to Freddy Acosta, Mevin Corcino, Allen Rau, Donald Stadolnik.
Application Number | 20210308059 17/344790 |
Document ID | / |
Family ID | 1000005642320 |
Filed Date | 2021-10-07 |
United States Patent
Application |
20210308059 |
Kind Code |
A1 |
Rau; Allen ; et al. |
October 7, 2021 |
TABLETS WITH IMPROVED FRIABILITY
Abstract
Tablets are prepared with friability reducing agents to yield
tablets that are more resistant to breakage or crumbling, but with
satisfactory hardness. The friability reducing agents include low
molecular weight polyethylene glycol as well as similar agents
exhibiting at least three percent (3%) hydroxide moieties and a
water solubility of at least eighty percent (80%) (w/w %) in room
temperature water. The tablets may comprise an active agent and
excipient of almost any type, and about 0.1-about 0.5% by weight
friability reducing agent. They exhibit a hardness of at least
eighty percent (80%) of the same tablet prepared without the
friability reducing agent.
Inventors: |
Rau; Allen; (Cincinnati,
OH) ; Stadolnik; Donald; (Centerbrook, CT) ;
Corcino; Mevin; (Centerbrook, CT) ; Acosta;
Freddy; (Centerbrook, CT) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
TOWER LABORATORIES LTD |
Centerbrook |
CT |
US |
|
|
Assignee: |
TOWER LABORATORIES LTD
Centerbrook
CT
|
Family ID: |
1000005642320 |
Appl. No.: |
17/344790 |
Filed: |
June 10, 2021 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
13867308 |
Apr 22, 2013 |
11058642 |
|
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17344790 |
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Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61K 9/2013 20130101;
A01N 25/00 20130101; A61K 9/2031 20130101; A61Q 11/00 20130101 |
International
Class: |
A61K 9/20 20060101
A61K009/20; A01N 25/00 20060101 A01N025/00; A61Q 11/00 20060101
A61Q011/00 |
Claims
1-10. (canceled)
11. A tablet exhibiting reduced friability, said tablet comprising:
A) An active agent; B) an excipient compatible with said active
agent; and C) an agent to reduce friability, wherein said agent to
reduce friability is a polyethylene glycol of molecular weight of
200-1000, present in amounts of about 0.1%-about 5.0% by weight of
the tablet, wherein said tablet comprising said friability reducing
agent exhibits a hardness of at least eighty percent (80%) of the
hardness exhibited by said tablet prepared in the absence of said
friability reducing agent.
12. The tablet of claim 11, wherein said active agent is selected
from the group consisting of a flavor, an aroma, a medication, a
nutritional product, a bleach, a detergent, an herbicide, an
insecticide or bactericide
13. The tablet of claim 11, wherein said tablet comprises an
effervescent couple which combine to release carbon dioxide when
the tablet is moistened.
14. The tablet of claim 11 wherein said active agent is a
medication.
15. The tablet of claim 13, wherein said medication is selected
from the group consisting of a pharmaceutical preparation available
with a prescription, an over-the-counter product, a gastric acid
neutralizer, a laxative, and an anti-flatulent.
16. The tablet of claim 11, wherein said friability reducing agent
is comprised of polyethylene glycol 400.
17. The tablet of claim 11, wherein said excipient is a stabilizer,
lubricant, a binder, a disintegrant, or a coating.
18. The tablet of claim 11, wherein said active agent comprises a
nutritional product.
19. The tablet of claim 11, wherein said tablet is intended for
consumption by an animal.
20. The tablet of claim 19, wherein said animal is a mammal.
21. The tablet of claim 20, wherein said mammal is a human.
22. A tablet exhibiting reduced friability, said tablet comprising:
A) An active agent; B) an excipient compatible with said
medication; and C) an agent to reduce friability, wherein said
agent to reduce friability is glycerin, present in amounts of about
0.1%-about 5.0% by weight of the tablet, wherein said tablet
comprising said friability reducing agent exhibits a hardness of at
least eighty percent (80%) of the hardness exhibited by said tablet
prepared in the absence of said friability reducing agent.
Description
BACKGROUND OF THE INVENTION
Background of the Technology
[0001] To those versed in the art and science of tableting, the
term friability describes a tablet's propensity to crumble. When a
tablet formulation displays high friability, it crumbles easily.
This is not a good thing. Highly friable tablets are difficult to
convey during production and are hard to package and transport.
Consumers, reasonably, expect their tablet products to be unbroken
and whole.
[0002] This invention is based on the inclusion of lower molecular
weight polyethylene glycol (low MW PEG) in tablet formulations.
These PEGs are liquid at room temperature (melting points below
about 35.degree. C.). They have average molecular weights of about
200 to 800. We have discovered that low molecular weight PEG has
the surprising benefit of dramatically improving the friability of
tablet formulations.
Background of the Prior Art
[0003] This performance is not known in the art. In fact, the major
manufacturer of PEG, Dow Chemical Company, teaches away from using
low MW PEG for tableting in their sales literature (reference
dow-answer.custhelp.com: Carbowax.TM. Sentry.TM. PEGS & MPEGS
for Pharmaceuticals; answer id 3561, Carbowax.TM. Sentry.TM.
Polyethylene Glycols for Cosmetics and Personal Care (answer id
3541) and Carbowax.TM. Sentry.TM. Polyethylene Glycols (form no
118-01790-1011 AMS)). Searches of the United States and European
patent literature do not yield results that teach the inclusion of
low MW PEG in tablet formulations, let alone for its ability to
improve tablet friability.
[0004] Polyethylene glycol (PEG) is a polymer frequently used in
tablet formulations. Higher molecular weight PEG is commonly used a
binder and/or as a lubricant. Typically, PEG with average molecular
weight 8000 (INCI nomenclature PEG-180, trade name: Carbowax.TM.
8000) is used for this function. PEGs with slightly lower MW (down
to about MW 4000) are also known to be used for this function. The
higher molecular weight PEGs are solid at room temperature and have
melting points around 50-60.degree. C. Numerous citations of these
materials being used for these functions can be found in the
art.
[0005] Dow Chemical Company's publication "Carbowax.TM. Sentry.TM.
Polyethylene Glycols" (form no. 118-01790-1011 AMS, page 8,
obtained from the dow.com website) indicates that materials with
slightly lower molecular weight, "MW 1450 and higher" can be used
as processing aids for granulations. This reference however goes on
to state that "high MW materials such as PEG 8000 preferred" for
this purpose.
[0006] There are references in the patent art to PEGs with slightly
lower molecular weights being used as granulation aids. U.S. Pat.
No. 5,403,593 teaches PEGs with molecular weight as low as about
3000 (Col. 5, line 19 and claim 3) for this purpose. Although no
clear reason or data is presented in the patent, claim 2 includes
PEG with "average molecular weight of at least 900" as part of a
granulating medium. As noted at column 2, line 64, "the
compositions of the invention are prepared by a melt granulation
process, in the substantial absence of added liquid solvents".
Examples 1 and 2 note that tablets made from inventive granulations
have low friability (column 9, line 51; column 10, line 47).
However, it is not possible for one skilled in the art to infer
that this performance can be caused by low MW PEG, as the example
compositions only contain PEG 8000.
[0007] U.S. Patent Publication No. 2011/0112160, at claim 6,
describes a tablet with an excipient comprising PEG with MW in the
range of 400 to 20,000. None of the examples of this application
include PEGs with MW lower than 4000. Although the application
states that acceptable friability can be achieved (P0023, P0051)
using this technology, no data is given that would allow someone
skilled in the art to learn low MW PEG's ability to affect this
property. In fact, P0053 explicitly states that PEG 4000 is
preferred.
[0008] U.S. Patent Publication No. 2011/0135738 is similar to the
above application. It names the same inventors and has the same
assignee. Like the previous application, the use of PEG 400 in a
tablet is recited (claim 2). Also like the above application, there
is no teaching that would enable one skilled in the art to use low
molecular PEG as a friability improver. Again, PEG-4000 is
explicitly taught as the preferred material (P0053).
[0009] U.S. Patent Publication No. 2011/0136883 (same assignee as
above two (2) references, one common inventor) speaks directly to
use of PEG-400 in tablet formulations. This reference is not
predictive of the instant invention. While Example 4 (Table 2)
teaches the use of PEG 400 at five percent (5%), the test results
shown in Table 4 do not exhibit the dramatic decrease in friability
discovered in our invention. The Application's data shows a drop in
friability (0.10% without PEG 400, 0.05% with it) and a decrease in
hardness (140-220 N without PEG-400, 110-130 with it). Tablets
prepared according to our invention do not exhibit the loss in
hardness. More importantly, our discovery is that low MW PEG has a
much greater impact on friability at much lower levels than taught
here. In fact, we are not even able to make acceptable tablets when
PEG 400 is utilized at five percent (5%).
[0010] U.S. Patent Publication No. 2011/0262497 (same inventor and
assignee as immediate above application) mentions the use of liquid
polyethylene glycols as a possible excipient at P0029. However
there is no teaching anywhere in this application as to the
benefits and/or functions of doing so.
[0011] U.S. Pat. No. 4,093,710 is directed to the preparation of
powders or granules of small size, smaller than 20 mesh (a higher
mesh number means a smaller sized particle). This patent refers to
the use of a surfactant for use in the granulating solution
employed. The surfactant may be polyethylene glycol of PEG 400PEG
9000, as well as other surfactants such as sodium lauryl sulfate.
PEG 1540 is identified as the preferred surfactant. As this patent
is directed to the preparation of free flowing, rapidly dissolving
powders or small granules, friability and related properties are
not discussed.
SUMMARY OF THE INVENTION
[0012] We have discovered that low molecular polyethylene glycols
can dramatically improve the friability of tablet formulations when
incorporated at surprisingly low levels. In particular,
polyethylene glycols in the range of about PEG 200 to about PEG
1000 give superior performance and improvement in friability,
without a significant loss in hardness or other properties, when
formulating tablets in otherwise customary fashion. The level of
incorporation of low molecular weight and similar compounds at low
weight percentage gives improvements that are particularly
surprising. In fact, at weight levels of the overall tablet weight
at about 0.1-about 5.0%, striking improvements in friability are
observed. At higher levels, above about five percent (5.0% w/weight
of the tablet) an unacceptable loss of hardness is observed.
Hardness of a tablet is impacted by a wide variety of factors, one
of which is the character of the central or active agent of the
tablet, as well as the excipients included therewith. As a result,
an absolute standard or range for hardness of the tablets of the
invention is difficult to establish. The tablets of this invention
have reduced friability and exhibit at least eighty percent (80%)
of the hardness the same tablet would exhibit in the absence of the
agent to reduce friability. The hardness exhibited by the tablets
of this invention may be 85, 90, 95 or even 100% of the hardness of
the same tablet made without the friability reducing agent.
[0013] While polyethylene glycol of the molecular weight PEG
200-PEG 1000 is the preferred friability improvement agent of this
invention, other similar compounds are effective in improving
friability (resistance to crumbling) without sacrificing other
desirable properties. In addition to polyethylene glycol, other
glycols, such as polypropylene glycol and methoxypolyethylene
glycol at relatively low molecular weights (PPG 425-about PPG 1000;
MPEG 350-about MPEG 1000) are also effective in improving tablet
friability at less than about five percent (5.0%) by weight. Other
high hydroxide content materials that are at least partially water
soluble, like glycerin and Tween.RTM. 80 are also effective in this
role.
[0014] The invention therefor is focused not on powders or
granules, but on tablets (tablet diameter is typically at least 3/4
inch diameter), and in particular, tablets of low friability,
tablets that exhibit a resistance to crumbling or breakage or
chipping. The tablets require an active agent of some sort--the
agent that is being delivered to the consumer in the tablet dosage.
This might be a flavor, an aroma, a medication (e.g.,
pharmaceutical prescription or OTC, a gastric acid neutralizer, a
laxative, an anti-flatulent, etc.) a nutritional product, a bleach,
a detergent, an herbicide or insecticide or bactericide, or any
other agent that is to be consumed or used. In preferred
embodiments, the tablet may comprise more than one active
agent.
[0015] Typically, the tablet will also include an excipient of some
type, to aid in delivery of the desired active agent. Excipients
are widely known, and can be selected from any chemical class that
does not impact the desired physical properties of the tablet. Many
excipients are stabilizers and add bulk to the tablet, and may
function as binders, such as saccharides and polysaccharides, sugar
alcohols such as sorbitol or xylitol, dicalcium phosphate,
microcrystalline cellulose, various proteins and synthetic
polymers. Other excipients commonly employed in the tablet art are
lubricants, coatings and disintegrants, all of which are compatible
with the friability reducing agents of the invention. Many
excipients are featured in the examples set forth below, but are
not so limited, and excipients as would be recognized as commonly
useful in the preparation of tablets by those of skill in that art
may be generally useful in the invention. The tablet need not
effervesce or otherwise demonstrate active properties other than
dissolution on wetting, but in one embodiment, the tablet does
comprise a dry effervescent couple (typically, an organic acid like
citric, fumaric or malic acid together with a carbonate or
bicarbonate such as sodium or potassium bicarbonate) that will
generate carbon dioxide when the tablet is wetted, or preferably
immersed, such as a drink or bathing formulation.
[0016] Thus, the invention is focused in terms of the properties of
the additive to reduce friability, but otherwise generally
inclusive of the components and purposes to which tablets are
commonly put. The tablet generally includes an active agent of some
type, and an excipient chosen to be compatible with that active
agent. The excipient may improve shape, appearance, flavor, texture
or other features of the tablet. A wide variety of optional agents,
depending on the ultimate utility of the tablet, may be
incorporated. These include flavorants, colorants, aromatic agents,
dispersants, preservatives, lubricants, etc. The tablets of the
invention further comprise an agent to reduce friability upon
tableting, present in amounts of about 0.1-about 5.0 percent by
weight of a compound having a solubility in room temperature water
of at least eighty percent (80%) (w/w%) and is comprised of at
least three percent (3%) by weight --OH moieties, and wherein said
tablet with said friability reducing agent exhibits a hardness of
at least eighty percent (80%) of the hardness of that same tablet
prepared in the absence of said additive.
SPECIFIC EXAMPLES OF THE INVENTION
[0017] The following examples demonstrate this performance. The
examples are provided for purposes of demonstration only, and are
not intended to limit the invention in any way. Other active agents
and excipients, as well as other agents effective in reducing
friability, within the broad parameters set forth above, will occur
to those of skill in the art.
Example 1: Denture Cleanser Tablet
[0018] The following base denture cleanser formula was prepared by
blending the indicated ingredients (Table 1) using conventional
powder mixing equipment.
TABLE-US-00001 TABLE 1 Material % w/w Sodium Bicarbonate 25.0
Citric Acid 20.0 Sodium Carbonate 15.0 Potassium Monopersulfate
10.0 Sodium Perborate Monohydrate 10.0 Maltodextrin 9.5 Sodium
Sulfate 8.7 Sodium Lauryl Sulfoacetate 0.7 PEG 8000 0.7 Flavor Oil
0.3 Sodium Benzoate 0.1 Total 100.0
[0019] Formulations that demonstrate the invention were prepared by
adding the indicated amount of PEG 400. The formulas were balanced
to one hundred percent (100%) by reducing the amount of sodium
sulfate.
[0020] Tablets were compressed using 7/8'' round tooling on a
Stokes F press. Compression force was adjusted to give the hardest
possible tablet (limit set by capability of the press or by the
appearance of tablet capping). Data is shown in Table 2.
[0021] Hardness was measured using a Schuleuniger-4M tablet
hardness tester.
[0022] Friability was measured in a manner similar to that
described in the USP-NF, Chapter <1216>. The USP-NF method
was modified in that the number of tablet used and the method of
calculation were changed as indicated here. Ten (10) tablets were
placed in an Erweka TA friability apparatus. The tablets were
tumbled at 25 rpm for the indicated number of minutes. The
percentage of unbroken tablets is reported.
[0023] Dissolution time was measured by placing a tablet in 125 ml
of water at 25.degree. C. The time needed for essentially complete
dissolution is reported.
TABLE-US-00002 TABLE 2 Friability (% whole tablets) PEG 400 Weight
Hardness Thickness 2 4 6 8 10 Dissolution concentration (g) (kp)
(mm) min min min min min Time (sec) .sup. 0% 2.69 7.8 3.96 70 10 0
0 0 83 0.1% 2.70 8.2 3.95 100 85 40 15 5 82 0.6% 2.69 9.0 3.82 100
100 100 100 100 103 1.0% 2.65 8.5 3.85 100 100 100 100 100 145 5.0%
2.80 4.6 4.21 100 100 100 100 100 71
[0024] This data clearly shows the effect of PEG 400 on the denture
cleanser composition. Below five percent (5%) PEG 400, friability
is unexpectedly and dramatically improved while hardness and
dissolution time are not significantly affected. At five percent
(5%) though, the tablet's hardness is decreased to an unacceptable
level.
Example 2: Alternate Molecular Weight PEGs
[0025] The effect of different molecular weight PEGs was
investigated. The PEGs listed in Table 3 were evaluated using the
formula shown in Table 1. 0.6% PEG was used in each trial. The
formulas were balanced to 100% by reducing sodium sulfate. Data is
shown below.
TABLE-US-00003 TABLE 3 Friability (% Whole Tablets) Weight Hardness
Thickness 2 4 6 8 10 Dissolution PEG MW (g) (kp) (mm) min min min
min min Time (sec) None (control) 2.69 7.8 3.96 70 10 0 0 0 83 200
2.66 8.1 3.92 100 100 100 100 100 72 400 2.69 9.0 3.82 100 100 100
100 100 103 600 2.69 7.5 3.94 100 100 100 100 100 145 1000 2.71 7.4
3.98 100 85 30 0 0 82 1450 2.62 6.6 3.90 60 20 5 0 0 73
Clearly, the friability benefit of the invention is maximized when
using PEGs with MW between 200 and 1,000. The drop in performance
at MW 1450 is surprising.
Example 3: Alternate Materials Similar in Structure to PEG
[0026] Materials with chemical structures somewhat similar to PEG
were tested to assess their performance in reducing tablet
friability. That is, we assessed hydrophilic materials that are
ethoxylated or propoxylated. A range of chain length materials were
investigated. For comparison purposes, we also looked at a
hydrophobic material (mineral oil) and glycerin (as a very short
chain, high hydroxyl content material). These assessments were
conducted using the denture cleanser formulation shown in Table
1.
[0027] Data from these experiments are presented in Table 4:
TABLE-US-00004 TABLE 4 Friability (% Whole Tablets) Material added
Weight Hardness 2 4 6 8 10 (0.6% formula) Structure (g) (kp) min
min min min min No additive -- 2.69 7.8 70 10 0 0 0 PEG 400
H--(O--CH.sub.2--CH.sub.2).sub.8--OH 2.69 9.0 100 100 100 100 100
Polypropylene glycol H--(O--CH(CH.sub.3)CH.sub.2).sub.4--OH 2.64
8.0 100 100 100 100 100 250 (PPG-4) Polypropylene glycol
H--(O--CH(CH.sub.3)--CH.sub.2).sub.9--OH 2.67 7.5 100 80 55 30 0
425 (PPG-9) Polypropylene glycol
H--(O--CH(CH.sub.3)--CH.sub.2).sub.10--OH 2.65 6.5 100 70 30 10 0
700 (PPG-10) Polypropylene glycol
H--(O--CH(CH.sub.3)--CH.sub.2).sub.26--OH 2.67 3.7 20 0 0 0 0 2000
(PPG-26) Methoxypolyethylene
CH.sub.3--(O--CH.sub.2--CH.sub.2).sub.6--OH 2.66 6.4 100 100 100
100 100 glycol 350 (MPEG-6) Methoxypolyethylene
CH.sub.3--(O--CH.sub.2--CH.sub.2).sub.10--OH 2.66 6.4 100 100 100
100 100 glycol 550 (MPEG-10) Tween 80 (Polysorbate 80) ##STR00001##
2.69 5.6 100 100 90 95 85 Mineral Oil C.sub.nH.sub.2n+2 n=12-40
2.65 7.4 90 60 30 0 0 Glycerin OH--CH.sub.2--C(OH)--CH.sub.2--OH
2.65 9.5 100 100 100 100 100 ##STR00002##
[0028] In an attempt to understand what chemical properties of the
tested materials are critical to improving friability, we looked at
some of the physical properties of the tested materials. Table 5
provides these comparisons:
TABLE-US-00005 TABLE 5 Friablilty Appearance at Room Material
improvement Solubility in Water (w/w %) Temperature PEG 200 Yes
100% Clear viscous liquid PEG 400 Yes 100% Clear viscous liquid PEG
600 Yes 100% Clear viscous liquid PEG 1000 Somewhat 80% Soft,
Opaque white solid PEG 1450 No 72% Soft, Opaque white solid MPEG
350 Yes 100% Clear viscous liquid MPEG 550 Yes 100% Clear viscous
liquid PPG 250 Yes 100% Clear viscous liquid PPG 425 Yes Soluble at
room temperature, but Clear viscous liquid insoluble at higher
temperatures PPG 700 Somewhat Soluble to slightly soluble at Clear
viscous liquid room temperature PPG 2000 No 0% Clear viscous liquid
Tween 80 Yes 100% Clear viscous liquid (yellow) Mineral Oil No 0%
Clear viscous liquid Glycerin Yes 100% Clear viscous liquid
[0029] Examining these data, it appears that agents which are at
least somewhat soluble in water at room temperature exhibit the
inventive effect. It will be evident that the friability reducing
agents of this invention are physically and chemically compatible
with each other. Accordingly, they may be used in combination and
in mixtures. Given the desirability of limiting the amount of the
friability reducing agent present in the tablet in general, the
Examples herein focus on one agent or another, but multiple agents
could be used together, provided the weight limits are observed,
and any reduction in hardness is controlled
Example 4: Acids Other than Citric Acid
[0030] Denture cleanser tablets formulated according to Table 1,
with PEG 400 at included at the indicated level were produced with
acids other than citric acid. This was done to ascertain if the
inventive effect is limited to products based only on citric acid.
Table 6 displays the results of this experiment:
TABLE-US-00006 TABLE 6 Friability (% Whole Tablets) PEG 400 Weight
Hardness 2 4 6 8 10 Acid level (%) (g) (kp) min min min min min
Citric Acid 0 2.69 7.77 70 10 0 0 0 Citric Acid 0.6 2.69 8.96 100
100 100 100 100 Fumaric Acid 0 2.61 5.09 25 0 0 0 0 Fumaric Acid
0.6 2.60 5.80 100 100 95 90 85 Malic Acid 0 n/a n/a -- -- -- -- --
Malic Acid 0.6 2.39 5.28 100 100 100 100 100 Sodium Bisulfate 0
2.66 6.56 10 0 0 0 0 Sodium Bisulfate 0.6 2.70 5.99 85 40 10 0
0
[0031] The above data clearly show the benefits of including PEG
400 in the formulation. Most notably, and surprisingly, tablets
made with malic acid could not be produced without inclusion of the
low molecular weight PEG.
[0032] Product formulations other than denture tablets were also
studied. Examples follow.
Example 5: Vitamin C Drink Tablet
[0033] An effervescent Vitamin C tablet (designed to dissolve in
water before ingesting) was developed using the composition shown
in Table 7. The formula was prepared by blending the indicated
ingredients using conventional powder mixing equipment.
TABLE-US-00007 TABLE 7 Material % w/w Ascorbic Acid 33.4 Citric
Acid 33.4 Sodium Bicarbonate 8.3 Potassium Bicarbonate 8.3 Sorbitol
8.6 Maltodextrin 2.0 Flavor Oil 0.2 Sucralose 0.4 PEG 8000 4.4
Sodium Benzoate 1.0 Total 100.0
[0034] Formulations that demonstrate the invention were prepared by
adding the indicated amount of PEG 400. The formulas were balanced
to one hundred percent (100%) by reducing the amount of
sorbitol.
[0035] Three (3) gram tablets were compressed using 7/8'' round
tooling on a Stokes F press. Compression force was adjusted to give
the hardest possible tablet (limit set by capability of the press
or by appearance of tablet capping).
[0036] These tablets were evaluated by the same methods discussed
above. Data are shown in Table 8.
TABLE-US-00008 TABLE 8 Friability (% Whole Tablets) PEG 400 Weight
Hardness Thickness 2 4 6 8 10 concentration (g) (kp) (mm) min min
min min min Comments 0 2.95 5.4 5.03 50 0 0 0 0 -- 0.1% 2.99 6.1
5.06 100 95 60 25 5 -- 0.6% 2.92 6.7 4.92 100 100 100 100 100 --
1.0% 2.78 3.7 5.05 100 100 100 100 100 -- 5.0% -- -- -- -- -- -- --
-- Tablets could not be pressed due to punch face sticking and
sidewall scoring
[0037] Again, the addition of a small amount of PEG 400 provides
the unexpected result of highly improved friability without harm to
other properties.
Example 6: Beverage Tablet
[0038] An effervescent tablet designed to form a lemon/lime
beverage when dissolved in water was formulated as shown in Table
9:
TABLE-US-00009 TABLE 9 Material % w/w Citric Acid 54.6 Sodium
Bicarbonate 21.2 Sorbitol 17.7 Lemon/Lime Flavor Oil 0.9 Acesulfame
K 0.4 Aspartame 1.0 PEG 8000 2.7 Sodium Benzoate 1.5 Total
100.0
[0039] Formulations that demonstrate the invention were prepared by
adding the indicated amount of PEG 400. The formulas were balanced
to one hundred percent (100%) by reducing the amount of
sorbitol.
[0040] 3.3 gram tablets were compressed using 7/8'' round tooling
on a Stokes F press. As above, compression force was adjusted to
give the hardest possible tablet (limit set by capability of the
press or by appearance of tablet capping).
[0041] These tablets were evaluated by the same methods discussed
above. Data are shown in Table 10.
TABLE-US-00010 TABLE 10 Friability (% Whole Tablets) PEG 400 Weight
Hardness Thickness 2 4 6 8 10 concentration (g) (kp) (mm) min min
min min min 0 3.27 7.1 5.60 100 75 35 0 0 0.6% 3.27 7.7 5.55 100
100 100 100 100
[0042] Again, the dramatic effect of low molecular weight PEG
addition was demonstrated.
[0043] It may be noted that all of the formulations in the above
examples are effervescent. That is, they contain one or more
organic acids and one or more carbonate salts. In the presence of
water the acid and the carbonate salt react to release carbon
dioxide, creating a bubbling action that is appealing to consumers
and that disperses formula ingredients. Many examples of
effervescent products (developed for many reasons) can be found in
the art. Given that effervescent formulations are somewhat
specialized, our inventive technology was also checked in a
non-effervescent formulation.
Example 7: Candy Tablet
[0044] A tart, sugar based candy tablet was developed according to
the formula shown in Table 11. This tablet can be dissolved in the
mouth as a lozenge.
TABLE-US-00011 TABLE 11 Material % w/w Dextrose 44.7 Maltodextrin
44.4 Citric Acid 10.0 Lemon/Lime Flavor Oil 0.3 PEG 8000 0.5 Sodium
Benzoate 0.1 Total 100.0
[0045] Formulations that demonstrate the invention were prepared by
adding the indicated amount of PEG 400. The formulas were balanced
to one hundred percent (100%) by reducing the amount of
maltodextrin.
[0046] 2.5 gram tablets were compressed using 7/8'' round tooling
on a Stokes F press. As above, compression force was adjusted to
give the hardest possible tablet (limit set by capability of the
press or by appearance of tablet capping).
[0047] These tablets were evaluated by the same methods discussed
above. Data are shown in Table 12.
TABLE-US-00012 TABLE 12 Friability (% Whole Tablets) PEG 400 Weight
Hardness Thickness 2 4 6 8 10 concentration (g) (kp) (mm) min min
min min min Comments 0 2.38 5.8 4.66 40 0 0 0 0 -- 0.1% 2.37 4.7
4.58 70 35 5 0 0 -- 0.6% 2.40 6.0 4.61 100 100 100 85 75 -- 1.0% --
-- -- -- -- -- -- -- Flow issues. Tablets were not pressed
[0048] These data clearly demonstrate the benefits of the invention
in a non-effervescent formulation.
[0049] While the present invention has been disclosed with
references to certain embodiments, numerous modification,
alterations, and changes to the described embodiments are possible
without departing from the sphere and scope of the present
invention, as defined in the appended claims. Accordingly, it is
intended that the present invention not be limited to the described
embodiments, but that it has the full scope defined by the language
of the following claims, and equivalents thereof.
* * * * *