U.S. patent application number 12/190114 was filed with the patent office on 2008-12-04 for odourless garlic supplement comprising an enteric coating and a deodorising layer.
This patent application is currently assigned to David Kannar. Invention is credited to David Kannar.
Application Number | 20080299181 12/190114 |
Document ID | / |
Family ID | 3820823 |
Filed Date | 2008-12-04 |
United States Patent
Application |
20080299181 |
Kind Code |
A1 |
Kannar; David |
December 4, 2008 |
ODOURLESS GARLIC SUPPLEMENT COMPRISING AN ENTERIC COATING AND A
DEODORISING LAYER
Abstract
A garlic supplement comprises one or more cores comprising
garlic and an enteric coating encasing the core(s) which is
insoluble at pH less than about 5 but soluble at a pH greater than
about 5. In one example, the enteric coating comprises a
deodorizer. In another example, an external coating is present over
the enteric coating and the external coating includes a
deodorizer.
Inventors: |
Kannar; David; (Belgrave
South, AU) |
Correspondence
Address: |
HAHN LOESER & PARKS, LLP
One GOJO Plaza, Suite 300
AKRON
OH
44311-1076
US
|
Assignee: |
Kannar; David
Belgrave South
AU
|
Family ID: |
3820823 |
Appl. No.: |
12/190114 |
Filed: |
August 12, 2008 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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10240855 |
Jan 21, 2003 |
7425342 |
|
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PCT/AU01/00390 |
Apr 6, 2001 |
|
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12190114 |
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Current U.S.
Class: |
424/439 ;
424/451; 424/456; 424/754 |
Current CPC
Class: |
A61P 9/12 20180101; A23V
2250/212 20130101; A61K 9/2886 20130101; A23L 33/105 20160801; A61P
7/02 20180101; A23V 2002/00 20130101; A23V 2002/00 20130101 |
Class at
Publication: |
424/439 ;
424/754; 424/451; 424/456 |
International
Class: |
A61K 9/00 20060101
A61K009/00; A61K 36/8962 20060101 A61K036/8962; A61K 9/48 20060101
A61K009/48 |
Foreign Application Data
Date |
Code |
Application Number |
Apr 6, 2000 |
AU |
PQ 6728 |
Claims
1. A garlic supplement comprising: (a) one or more cores comprising
garlic; and (b) an enteric coating encasing the core(s) which is
insoluble at pH less than about 5 but soluble at a pH greater than
about 5 and wherein the enteric coating comprises a deodorizer.
2. The garlic supplement according to claim 1 wherein the
deodorizer is selected from the group consisting of extracts,
aqueous extracts, natural flavours or oils derived from parsley
seed, Lamiaceae plants, green tea, and flavanoid containing plants
or synthetic versions thereof and mixtures thereof.
3. The garlic supplement according to claim 1 wherein the garlic is
in a form selected from the group consisting of fresh garlic, dry
powder, oils, macerates, extracts, aged extracts, steam distilled
oils and mixtures thereof.
4. The garlic supplement according to claim 3 wherein the garlic is
in the form of a dry powder.
5. The garlic supplement according to claim 1 wherein the core(s)
further comprise(s) one or more carriers selected from the group
consisting of binders, fillers, deodorizers and other
pharmaceutically acceptable excipients.
6. The garlic supplement according to claim 5 wherein the core
further comprises a deodorizer.
7. The garlic supplement according to claim 1 wherein the enteric
coating is selected from the group consisting cellulose,
methylcellulose, natural polymers, synthetic polymers, cross-linked
gelatin and mixtures thereof.
8. The garlic supplement according to claim 7 wherein the enteric
coating is selected from cellulose or methylcellulose or mixtures
thereof.
9. The garlic supplement according to claim 1 wherein the thickness
of the enteric-coating is not greater than about 0.5 mm.
10. The garlic supplement according to claim 1 wherein the
deodorizer is present in an amount from about 0.5 to about 1.0
weight % of the total weight of the garlic supplement.
11. The garlic supplement according to claim 10 wherein the
deodorizer is present in an amount from about 0.6 weight % of the
total weight of the garlic supplement.
12. The garlic supplement according to claim 1 which further
comprises an external coating applied over the enteric coating.
13. The garlic supplement according to claim 12 wherein the
deodorizer is incorporated in the external coating.
14. The garlic supplement according to claim 12 wherein the
external coating has a thickness in the range of from 0.001 mm to
1.500 mm.
15. The garlic supplement according to claim 12 wherein the
external coating comprises one or more coating agents selected from
the group consisting of microcrystalline waxes, carnauba wax,
polyvinylpyrroldidone, sugars and mixtures thereof.
16. The garlic supplement according to claim 1 wherein the garlic
supplement is in a form selected from the group consisting of a
tablet cross-linked capsule, gelatin capsule, suspensions,
emulsions, enteral feeds, functional foods or micro-particles.
17. The garlic supplement according to claim 16 wherein the core(s)
is in a form selected from the group consisting of liquids, solids,
fluids, gels and mixtures thereof.
18. A garlic supplement comprising: (a) one or more cores
comprising garlic; and (b) an enteric coating encasing the core(s)
which is insoluble at pH less than about 5 but soluble at a pH
greater than about 5; and (c) an external coating over the enteric
coating wherein the external coating comprises a deodorizer.
19. The garlic supplement according to claim 18 wherein the enteric
coating further comprises a deodorizer.
20. The garlic supplement according to claim 18 wherein the
deodorizer is selected from the group consisting of extracts,
aqueous extracts, natural flavours or oils derived from parsley
seed, Lamiaceae plants, green tea, and flavanoid containing plants
or synthetic versions thereof and mixtures thereof.
Description
CROSS REFERENCES TO RELATED APPLICATIONS
[0001] This invention is a divisional of copending U.S. application
Ser. No. 10/240,855, filed Oct. 4, 2002, which is the National
Stage of International Application No. PCT/AU01/00390, filed Apr.
6, 2001, which claims priority from Australian Application No. PQ
6728, filed Apr. 6, 2000.
FIELD OF THE INVENTION
[0002] This invention relates to an improved garlic supplement with
reduced breath odor effects.
BACKGROUND OF THE INVENTION
[0003] In this specification, where a document, act or item of
knowledge is referred to or discussed, this reference or discussion
is not an admission that the document, act or item of knowledge or
any combination thereof was at the priority date: [0004] (i) part
of common general knowledge; or [0005] (ii) known to be relevant to
an attempt to solve any problem with which this specification is
concerned.
[0006] Garlic is utilized in many food cultures for its distinctive
flavor. It has also been of interest in medicine for many years and
has recently recaptured the interest of the public and of modern
Western medical science. This is primarily because of garlic's
relatively high sulfur content, historic antibacterial use and
reported protective effects on the cardiovascular system.
[0007] During the last decade epidemiological, in vivo and in vitro
studies, have suggested important cardioprotective properties
associated with an increase of garlic in the diet including: [0008]
a) reduction of blood cholesterol levels which may assist in
treating hypercholesterolaemia which is a major risk factor for
heart disease; [0009] b) increase of antioxidant activity which
assists in reduction of atherosclerosis and lowering of blood
viscosity; [0010] c) decrease in blood pressure and hardening of
the aorta; [0011] d) potential protection against breast cancer;
[0012] e) inhibition of blood clotting and reduction in platelet
aggregation; [0013] f) reduction in blood glucose levels; and
[0014] g) protection against ventricular tachycardia, and
fibrillation during ischaemia and reperfusion.
[0015] As a result of the recognition of these health benefits,
garlic supplements have become popular in the market. These
supplements are available as garlic powders, oil macerates, steam
distilled oils and aged garlic extracts. Fresh garlic and dried
powders are typically used in food preparation and as spices but
may also be presented as tablets. Steam distilled oils and aged
extracts are used in tablets, soft gelatin capsules or liquids.
Actives and Dosage
[0016] When a garlic bulb is crushed, allinase found in vacuoles
reacts with S-alk(en)ylcysteine sulfoxide within the cell, forming
sulfenic acids which spontaneously convert to thiosulfinates
including allicin. The thiosulfinates further degrade to vinyl
dithins and ajoenes within 24 hours. The thiosulfinate allicin
accounts for approximately 70% of the total thiosulfinates produced
and is thought to be the principle bioactive compound responsible
for the health promoting benefits of garlic.
[0017] Most of the cardio-protective and antibacterial effects of
garlic seem to be derived from allicin, its metabolites and to a
lesser extent the dialkyl sulfides. The ajoenes have been shown to
be powerful inhibitors of platelet aggregation. The most
conclusively shown beneficial effect is a reduction of low density
lipoprotein and total cholesterol, although the results published
to date are variable and inconsistent. Recent evidence suggests
that this variation may be due to variability arising from dose
formulation causing inconsistent allicin release. These results
could be interpreted to mean that the therapeutic efficacy of
garlic is dose dependant, relying upon the quantity of allicin
released.
[0018] As studies have not conclusively shown which phytochemical
components are responsible for which beneficial effects provided by
garlic, many garlic supplements are currently available on the
market such as garlic powders, oil macerates steam distilled oils
and aged garlic extracts. Each dose form varies in the
phytochemical content because of the different methods of
preparation. Even though still relatively inconsistent, the most
reproducible cardiovascular benefits seem to be derived from use of
fresh garlic and of carefully dried garlic powders.
[0019] Therefore, in order to reproduce the historic health
benefits of garlic demonstrated in epidemiological studies and
maximize therapeutic activity of garlic, the finished product not
only needs to be representative of fresh garlic but contain
adequate amounts of active phytochemicals, in particular allicin,
because efficacy seems dose dependant.
[0020] Another factor affecting the efficacy of garlic supplements
is the fact that allinase's activity is known to be completely
inhibited by the acidic conditions of the stomach. However, the
watery alkaline activity in the small intestine does not inhibit
allinase activity enabling allicin, other thiosulfinates and/or
thiosulfinate metabolites, to be metabolised and transported across
the gut mucosa into the portal vein, to reach the liver and
cardiovascular system. If allicin and the other thiosulfinates can
reach the small intestine they are then able to provide beneficial
effects including benefiting the cardiovascular system. Therefore,
the garlic supplement should protect allinase from stomach
acid.
Garlic Odor
[0021] Unfortunately, the consumption of garlic often produces the
unsociable `garlic breath` and general garlic odor. This limits
consumption and deprives the public of a therapeutically valuable
food, or dietary supplement well recognized for its health
promoting benefits. Like many other plant remedies, garlic is a
complex mix of biological and phytochemical components, of which
the bioactive sulfur compounds have drawn the most attention.
[0022] Although allicin is thought to be the principle active
compound responsible for providing most of the pharmacological
activity of garlic, its metabolic processing by the body to
mercaptans is responsible for the characteristic "garlic odor".
Allicin is also thought to be responsible for the odor of garlic
released in the buccal cavity and upper gastrointestinal tract
after consumption. As a result, increasing the dosage of allicin in
garlic supplements may cause an increase in garlic odor on the
breath.
[0023] Some manufacturers have developed formulations to minimize
this odor. Odor reducing strategies for garlic supplements have
previously included addition of charcoal, titanium dioxide, milk
sugar, potato starch, gallic acid or other substances with little
success. Odor minimized garlic extracts may also be produced by
aging or denaturation of allinase activity. However, minimization
of odor may also eliminate many of garlic's active pharmacological
compounds and therefore eliminate some of the beneficial effects,
for example, aging or denaturation of allinase activity inhibits
allicin producing potential. In fact, these deodorized garlic
supplements have demonstrated very low efficacy levels.
[0024] Parsley has been used in an attempt to reduce the odor of
garlic preparations and tablets by mixing the parsley with the
garlic in the tablet matrix. The action of parsley is thought to be
accomplished by the addition of chlorophyll. The "odor blocking"
potency of parsley and chlorophyll has not been previously studied
but addition of other strong-smelling volatile oils from thyme,
peppermint or other Lamiaceae species is thought to mask the strong
garlic odor. Green tea extract, standardized to contain polyphenols
(catechins), has been tested for deodorizing properties, and found
more effective than synthetic deodorants against mercaptan (cause
of garlic odor), ammonia, trimethylamine and cigarette smells.
Whilst these deodorizing agents do mask the garlic odor to some
extent, there is still some odor remaining at a level which many
people find objectionable.
[0025] Some manufacturers have used an enteric coating to mask the
odor of garlic supplements. This has the double advantage of
protecting the allinase from the stomach acids until the supplement
reaches the small intestine. Whilst enteric coatings have been the
most successful method at reducing garlic odor, it has been found
that when garlic tablets are consumed daily, an objectionable
garlic odor is noticeable in some people after the second day.
[0026] While the potential benefits of garlic have been recognized,
and many attempts made to provide garlic supplements in a variety
of forms including tablets, the odor of garlic has limited the
success of these supplements. The previous attempts to in some way
alleviate the odors caused by consumption of garlic have not been
very successful. There is thus a need for an improved garlic
supplement or food to provide beneficial effects for humans and to
further reduce the smell of the garlic associated with a high
allicin producing garlic powder while maintaining efficacy.
SUMMARY OF THE INVENTION
[0027] It has been found that if a garlic supplement has both an
enteric coating and a deodorizer then the objectionable garlic odor
was considerably reduced. Further, the garlic odor did not return
when the garlic supplements were consumed daily for more than two
days.
[0028] The word `supplement` as used in this description refers to
all forms of supplying pharmaceuticals or nutrients orally or
enterally. For example, tablets, capsules, oral suspensions,
children's formulations, enteral feeds and functional foods.
[0029] Accordingly, there is provided a garlic supplement
comprising: [0030] (a) one or more cores comprising garlic; [0031]
(b) an enteric coating encasing the core(s) which is insoluble at
pH less than about 5 but soluble at a pH greater than about 5; and
[0032] (c) a deodorizer applied external of the core(s).
[0033] Preferably, the garlic supplement or food will be in the
form of a tablet, cross linked capsule or gelatin capsule. The
garlic may be formed into micro-particles and the enteric-coated
micro-particles can then be used in a range of pharmaceutical and
food dose forms including hard gelatin capsules, oral suspensions,
children's formulations, enteral feeds and functional foods.
[0034] The core(s) may in any form including fluid, liquid, solid,
gel or mixtures thereof. The core(s) may further comprise carriers
suitable for garlic supplements. Such carriers will be known to
those skilled in the art. The carrier may be composed of a variety
of different binders, fillers, deodorizers, other pharmaceutically
acceptable excipients or mixtures thereof.
[0035] In order to maximize therapeutic activity of the garlic
supplement, the garlic used in the supplement not only needs to be
representative of fresh garlic but also needs to contain adequate
amounts of pro-active phytochemicals in particular allicin and
allinase to optimize allicin and other thiosulfinates producing
potential. The garlic may be in any form selected from fresh
garlic, dry powder, oils, macerates, extracts, aged extracts, steam
distilled oils or mixtures thereof. Such therapeutic activity is
maximized by using specialized dehydration techniques and/or
specific strains of garlic. Persons skilled in the art will be
aware of such dehydration techniques and strains of garlic. One
form of garlic which can be used in the supplement is garlic powder
although other forms may be possible. Typically, the garlic powder
is produced by dehydrating garlic cloves or garlic parts and then
crushing the dried garlic to form a powder.
[0036] The enteric coating may be selected from the group
consisting of cellulose, methylcellulose, natural polymers,
synthetic polymers, cross-linked gelatin and mixtures thereof.
Preferably, the enteric coating will be cellulose or
methylcellulose or a similar substance designed to delay release of
the active ingredients. Coating agents are used to protect the
tablet core and garlic from the inhibiting effect of the stomach
acids. Polymers with pH dependant solubility properties (enteric
coatings) have been found to be most useful for this application.
Cross-linking of gelatin in the hard or soft gelatin capsule is
understood to impart the same biological effect. It is also
possible to place the garlic core in a capsule which has been
enterically coated or cross linked. Each of these methods will
delay the release of the garlic powder until the small
intestine.
[0037] The enteric coating typically has a maximum thickness of up
to 0.5 mm or, if the garlic tablet or capsule is for administration
to humans, the coating will normally need to comply with USP 2000
standards for delayed release dose forms.
[0038] The deodorizer may be either incorporated within the enteric
coating or applied as an external coating over the enteric coating.
Where the deodorizer is incorporated as an external coating over
the enteric coating, this external coating has a thickness in the
range of 0.001 mm to 1.500 mm. Typically, when the deodorizer is
incorporated into the enteric coating, the weight ratio of
deodorizer to the remainder of the enteric coating is in the range
of from 0.5 to 1.0%. Preferably, the weight ratio of deodoriser to
the remainder of the enteric coating is about 0.6%.
[0039] The deodoriser is selected from the group consisting of
extracts, aqueous extracts, natural flavours or oils derived from
parsley seed, Lamiaceae plants, green tea, and flavanoid containing
plants or synthetic versions thereof and mixtures thereof. Those
skilled in the art will also understand that it is possible to use
a variety of other products or combinations of products as a
deodorizer. Typically the deodorizer will be incorporated into an
additional surface coating such as carnauba wax,
polyvinylpyrroldidone, or a sugar, which surface coating may then
be applied to the tablet or capsule to form a coating or external
layer on the tablet or capsule. Typically the thickness of this
outer coating will be from about 0.001 mm to about 1.500 mm. The
weight ratio of the deodorizer to the coating as a whole can vary
significantly depending on the amount of deodorizer desired for
inclusion in the supplement.
[0040] It is possible to vary where the deodorizer is located in
the supplement. For example, as an alternative, the deodorizer may
be incorporated only in the enteric coating; or as a further
alternative, the deodorizer may be incorporated in the enteric
coating and also in the surface coating. Typically, the deodorizer
may be present in amount in the range of 0.5 to 1.0% by weight of
the total garlic supplement. Preferably, the amount of deodorizer
is about 0.6% by weight of the total garlic supplement.
[0041] According to a second aspect of the invention, there is
provided a method for preparing a garlic supplement comprising the
steps: [0042] (a) forming one or more cores comprising garlic;
[0043] (b) encasing the core(s) with an enteric coating which is
insoluble at pH less than about 5 but soluble at a pH greater than
about 5; and [0044] (c) applying an external coating over the
enteric coating wherein the external coating comprises a
deodorizer.
[0045] According to a third aspect of the invention, there is
provided a method for preparing a garlic supplement comprising the
steps: [0046] (a) forming one or more core comprising garlic; and
[0047] (b) encasing the core(s) with an enteric coating which is
insoluble at pH less than about 5 but soluble at a pH greater than
about 5 and wherein the enteric coating comprises a deodorizer.
[0048] According to a fourth aspect of the invention, there is
provided a method for reducing blood cholesterol in patients having
high blood cholesterol comprising the step of administering a
garlic supplement comprising: [0049] (a) one or more cores
comprising garlic; [0050] (b) an enteric coating encasing the
core(s) which is insoluble at pH less than about 5 but soluble at a
pH greater than about 5; and [0051] (c) a deodorizer applied
external of the core(s).
[0052] According to a fifth aspect of the invention, there is
provided a method for providing reproducible clinical benefits
associated with garlic for therapeutic or prophylactic treatment to
patients having conditions which benefit from administration of
garlic comprising: [0053] (a) one or more cores comprising garlic;
[0054] (b) an enteric coating encasing the core(s) which is
insoluble at pH less than about 5 but soluble at a pH greater than
about 5; and [0055] (c) a deodorizer applied external of the
core(s).
DETAILED DESCRIPTION OF THE INVENTION
[0056] The garlic powder is in tablet form. It will be readily
understood by those skilled in the art that garlic powder can be
put in tablet form in a number of different ways. It will be
understood that a variety of different binders, fillers and a
number of other excipients can be used. An enteric coating is then
applied to the tablet by usual methods.
[0057] When the tablet formed as detailed above, is swallowed, the
tablet moves down the digestive tract to the stomach. As the tablet
moves along the upper alimentary tract the outer surface coating
(if present) or the enteric coating begins to dissolve and releases
deodorizer into the upper alimentary tract. The tablet enters the
stomach and further deodorizer is released. The tablet or capsule
then passes into the alkaline small intestine, and at this point
the enteric coating completely dissolves and allicin produced by
the garlic is released. Accordingly, irrespective of whether the
deodorizer is contained in a surface coating on the outside of the
enteric coating or within the enteric coating itself, or both, a
portion of the deodorizer will be released in the upper gut. This
is preferred as parts of the deodorizer may react with the garlic
released in the lower gut, in particular the allicin, and reduce
the potential of the beneficial effects of garlic being provided to
the recipient of the tablet or capsule.
[0058] Whilst not wishing to be limited by theories, it is
postulated that the deodorizer `dissolved`, absorbed, held or
metabolized in the upper gut may act locally in the mouth, throat
and stomach to reduce garlic odor produced by exhaled garlic
derived volatile metabolites. The deodorizer may act to alleviate
the odor through either or both of the following two mechanisms:
[0059] (a) by deodorizing, that is, the process of adsorbing or
reacting with an aromatic substance to render it involatile or
non-aromatic, for example, by reacting with any odorous sulfur or
garlic derived compound rising from the lower gut or lungs into the
buccal cavity; or [0060] (b) by masking, that is, superimposition
of a dominant aroma on an undesirable odor so that the undesirable
odor was not recognizable.
[0061] Accordingly, the enteric coating ensures that all the garlic
(and hence allicin) is not released until the small intestine,
where it will be most effective. If there is deodorizer in the
remaining enteric coating it will also be dissolved at this stage.
Any such deodorizer and the garlic will then be digested in the
lower gut. At this time the allinase in the garlic powder
enzymatically forms sulfenic acids from the S-alk(en)ylcysteine
sulfoxides. The sulfenic acids spontaneously convert to
thiosulfinates including allicin. Allicin and it's metabolites and
other phytochemicals in the garlic are absorbed through the lining
of the intestine into the portal vein and/or lymph eventually
reaching the arteries, tissue and organs. Non digestible garlic
carbohydrates may also remain in the small intestine and act to
stimulate beneficial intestinal bacteria including bifidobacteria
and lactabacillus and also act broadly as a pre-biotic compound.
Once in circulation the allicin, its metabolites and other
phytochemicals can provide therapeutic benefits to the human
recipient.
[0062] The garlic supplement thus provides adequate allicin to the
person to produce the beneficial therapeutic effects whilst
minimizing the odor of the garlic.
EXAMPLES
[0063] The invention will now be further illustrated and explained
by reference to the following non-limiting examples.
Preparation of a Garlic Supplement
[0064] Enteric coated garlic tablets with mint are made using the
following method.
TABLE-US-00001 Ingredient Amount Cellulose gum modified NF 7.50 kg
Peppermint extract on micro-crystalline cellulose 36.00 kg Garlic
powder capable of producing 10,000 ppm allicin 924.00 kg
Microcrystalline cellulose, Silicified 400.50 kg Natural peppermint
flavor 36.00 kg Silicon dioxide, MS 4.50 kg Stearic acid, acid
powder 45.00 kg Carboxymethyl Starch 46.50 kg Shellac 20% with
Methylcellulose 215.30 kg Aqueous Peppermint Extract 14.5 L
Manufacturing Directions
[0065] 1.5 kg of peppermint extract is mixed with 4.50 kg of
silicon dioxide in a sealed container until uniformly blended (Part
A). The remaining peppermint extract (34.50 kg) is then passed
through a Sweco separator with 20 mesh screen in a 55 gallon
stainless steel drum (Part B). Part A and B are then mixed together
in the drum for 10 minutes=Part C.
[0066] 36.00 kg of natural peppermint flavor and 45.00 kg of
stearic acid powder are then passed through a Sweco separator
equipped with a 30 mesh screen directly into a 55 gallon stainless
steel drum then mixed for 10 minutes=Part D.
[0067] 924.00 kg of garlic powder is passed through a Sweco
separator equipped with a 20 mesh screen and then blended for 10
minutes=Part E.
[0068] 46.50 kg of carboxymethyl starch, 7.50 kg cellulose gum, and
400.50 kg silicified microcrystalline cellulose are passed through
a Sweco separator equipped with a 20 mesh screen then blended for
15 minutes=Part F.
[0069] Mix parts C to F and blend.
Tableting Instructions
[0070] The blended mixture is loaded into a Gemini tablet press and
2 to 6 tons of pressure is applied. Target weight of each tablet is
625 mg. Target tablet hardness is 25 scu. Target tablet gauge is
0.265 inches.
Coating Instructions
[0071] Set inlet air temperature dial to 93.degree. C. Set
mistchecker atomization air at 160 SLPM on each gun. Set
mistchecker pattern air (total volume) to 240 SLPM on each gun.
[0072] Turn on exhaust fan. Load each pan with approximately
600,000 tablets and set guns 10 to 12 inches from tablet bed. Jog
coating pan until exhaust temperature is 115.degree. F. to
120.degree. F. and adjust pan speed to 6 r.p.m. Pre-mix shellac 20%
with methylcellulose and aqueous mint extract to give a
conveniently sprayable product then apply 45 litres of the solution
at 480 ml/min. Cool tablets until exhaust temperature is
100.degree. F. (38.degree. C.). Apply 40 to 50 gm of carnauba
wax.
Example One
[0073] Allyl mercaptan and diallyl disulfide are among the
malodorous constituents of garlic breath. The purpose of this
example is to quantitatively determine and compare the amounts of
allyl mercaptan and diallyl disulfide present in garlic breath,
over a 24 hour period, resulting from the consumption of garlic
tablets according to the invention compared with an equivalent
portion of fresh garlic.
Method
[0074] A comparative assay of garlic breath odor was performed on
two subjects with two garlic tablets according to the invention and
2 cloves of fresh garlic (positive control). The subject's breath
was collected at time 0 (prior to consumption of tablets or fresh
garlic) and then at 0.5, 1, 2, 4, 8, and 24 hours. The tablets were
swallowed whole and washed down with water. The fresh garlic was
homogenized in 100 mL of water and swallowed, being washed down
with another volume of water.
[0075] Breath of the test subjects was exhaled into 3.0 L-Tedlar
bags. A PDMS (polydimethylsiloxane) SPME (Solid Phase
Microextraction) fibre was introduced to the inflated bag via a gas
tight septa. Volatile components of the subjects breath were
absorbed onto the surface of the SPME fibre for 30 minutes. The
fibre was removed and thermally desorbed onto a GC Column (BPX5 1
.mu.m film, 0.5 mm.times.50 m) with an inlet temperature of
260.degree. C. in splitless mode. The GC oven was set at an initial
temperature of 45.degree. C. for 6 mins to allow focussing of the
desorbed compounds.
[0076] To attain maximum sensitivity the mass spectrometer was set
in SIM (selected ion monitoring) mode whereby only ions significant
to the compounds allyl mercaptan and diallyl disulfide are scanned,
thus enhancing the response for these compounds. For allyl
mercaptan the ions 39, 45, 47, 59, 69, and 74 m/z, were selected in
the elution time range. 4.6-15.0 mins. For diallyl disulfide the
ions 81, 105, 113, 146 m/z were selected in the elution time range
15.0-23.5 mins. A major ion for both allyl mercaptan and diallyl
disulfide is 41 m/z, however was not included in the SIM ions as
its common occurrence in human breath negates any gain in
selectivity. The peak areas of allyl mercaptan and diallyl
disulfide are measured and calculated to mass units by reference to
external calibration standard curves.
BRIEF DESCRIPTION OF THE SEVERAL VIEWS OF THE DRAWINGS
Results
[0077] FIG. 1 is a chart showing the results obtained for diallyl
sulfide in breath from coated garlic tables according to the
invention and from fresh garlic.
[0078] FIG. 2 is a chart showing the results obtained for allyl
mercaptan in breath from coated garlic tables according to the
invention and from fresh garlic.
[0079] FIG. 3 is a chart showing the results obtained for diallyl
disulfide in breath from control tablets (enteric) and garlic
tablets according to the invention (enteric/mint).
[0080] FIG. 4 is a chart showing the results obtained for diallyl
disulfide in breath from control tablets (enteric) and garlic
tablets according to the invention (enteric/mint) expressed in peak
areas.
[0081] FIG. 5 is a chart showing the results obtained for compound
RT-7.64 in breath from control tablets (enteric) and garlic tablets
according to the invention (enteric/mint).
[0082] FIG. 6 is a chart showing the results obtained for compound
RT 8.01 in breath from control tablets (enteric) and garlic tablets
according to the invention (enteric/mint).
[0083] FIG. 7 is a chart showing the results obtained for diallyl
disulfide in breath from fresh garlic and fresh garlic with
peppermint extract.
[0084] FIG. 8 is a chart showing the results obtained for allyl
mercaptan in breath from fresh garlic and fresh garlic with
peppermint extract.
[0085] Allyl mercaptan present in subject breath in the test period
following consumption of enteric/mint coated garlic tablets is
markedly lower than the levels detected in fresh garlic breath.
Diallyl disulfide exhibits two maximia at 30 minutes and at 4 hours
for the fresh garlic indicating release from the stomach and
subsequent release through the blood from the intestine. Diallyl
disulfide is present in very low levels in breath from the
enteric/mint coated tablets until 4-8 hours at which time it is
released into the blood via the intestine. The level of diallyl
disulfide is however significantly lower than levels detected in
fresh garlic breath.
[0086] The signal to noise ratio has been determined from the
calibration standards data. Diallyl disulfide peaks are confidently
integrated to 3 ng/L and are detectable to 0.3 ng/L. Allyl
mercaptan peaks are confidently integrated to 6 ng/L and detectable
to 0.6 ng/L. Peaks included in the results which have values lower
than the integration limits are presented as indicative data
only.
Conclusions
[0087] Humans can detect odors where there is above 2 ng/L of the
compound present. Since the tablets according to the invention do
not produce either of the tested compounds at a level above 2 ng/L,
example one illustrates that garlic tablets according to the
invention have substantially reduced the garlic odor.
Example Two
[0088] This example compares odor constituents of subject breath
during consumption period of garlic tablets without mint extract in
the enteric coating (control) and garlic tablets containing mint
extract in the enteric coating according to the invention. In
addition, this example compares the influence of peppermint extract
alone on subject breath odor components after consumption of fresh
garlic homogenate. The aim of this study was to confirm that the
deodorizing effect of the invention was not simply due to either
the enteric coating or mint extract alone.
Method
[0089] Comparison of Breath from Consumption of Control Enteric
Coated Tablets and Garlic Tablets According to the Invention.
[0090] A comparative assay of garlic breath odor was performed on
one subject consuming two garlic tablets (either control or garlic
tablets according to the invention) for three days. The subject's
breath was collected at time 0 (prior to consumption of tablets)
and then at 4, 8, 24, 26, 28, 32, 48, 50, and 54 hours. The tablets
were swallowed whole and washed down with water each morning after
the first breath sample for the day was collected. The fresh garlic
is homogenized in 100 mL of water and swallowed, being washed down
with another volume of water.
Comparison of Breath from Consumption of Garlic Homogenate with and
without Added Peppermint Extract
[0091] For the control sample two cloves of fresh garlic were
homogenised in 100 mL of water and swallowed, being washed down
with another volume of water. For the test sample 20-30 mgs (3
drops) of peppermint oil were added to a homogenate of 2 garlic
cloves and 100 mL of water. This sample was imbibed as above.
Subject breath was collected for analysis at time 0, 0.5, 1, 2, 4,
8, and 24 hours.
Analytical Methodology
[0092] Breath of the test subjects was exhaled into 3.0 L Tedlar
bags. A PDMS (Polydimethylsiloxane) SPME (Solid Phase
Microextraction) fibre was introduced to the inflated bag via a gas
tight septa. Volatile components of the subjects breath were
absorbed onto the surface of the SPME-fibre for 30 minutes. The
fibre was removed and thermally desorbed onto a GC Column (BPX5 1
Mm m film, 0.5 mm.times.50 m) with an inlet temperature of
260.degree. C. in splitless mode. The GC oven was set at an initial
temperature of 45.degree. C. for 6 mins to allow focussing of the
desorbed compounds.
[0093] To attain maximum sensitivity the mass spectrometer was set
in SIM (selected ion monitoring) mode, whereby only ions
significant to the compounds allyl mercaptan and diallyl disulfide
are scanned, thus enhancing the response for these compounds. For
allyl mercaptan the ions 39, 45, 47, 59, 69, 74, and 88 m/z were
selected in the elution time range 4.6-15.0 mins. For diallyl
disulfide the ions 81, 105, 113, 146 m/z were selected in the
elution time range 15.0-23.5 mins. The mass ion for both allyl
mercaptan and diallyl disulfide is 41 m/z. It could not be included
in the SIM ions as it is ubiquitous in human breath. The peak areas
of allyl mercaptan and diallyl disulfide are measured and
calculated to mass units by reference to external calibration
standard curves.
Results
[0094] Comparison of Breath from Consumption of Control Enteric
Coated Tablets and Garlic Tablets According to the Invention.
[0095] FIG. 3 shows the results obtained for diallyl disulfide in
breath from control tablets (enteric) and garlic tablets according
to the invention (enteric/mint).
[0096] FIG. 4 shows the results obtained for diallyl disulfide in
breath from control tablets (enteric) and garlic tablets according
to the invention (enteric/mint) expressed in peak areas.
[0097] The SIM conditions used are specifically targeted at allyl
mercaptan and diallyl disulfide. It is likely that the major ions
present in the fragmentation patterns of these two compounds are
present in the mass spectra of other related garlic odor compounds.
In the comparative assay of enteric coated tablets levels of allyl
mercaptan and diallyl disulfide were too low to explain the strong
breath odor and sulfurous flavors which were intermittently present
during this and other trials. However at least two other peaks
occurring either side of allyl mercaptan exhibited trends
correlating to the observed episodes of garlic breath. These occur
at retention times of 7.64 and 8.01 minutes. Comparative trends of
these two compounds are compared in charts 5 & 6.
[0098] FIG. 5 shows the results obtained for compound RT-7.64 in
breath from control tablets (enteric) and garlic tablets according
to the invention (enteric/mint).
[0099] FIG. 6 shows the results obtained for compound RT 8.01 in
breath from control tablets (enteric) and garlic tablets according
to the invention (enteric/mint).
[0100] FIGS. 5 & 6 clearly identify the that peaks RT 7.64
& RT 8.01 varied according to the tablet consumed. After 50
hours peak RT 7.64 increases substantially but only in the control
tablet. Analysis of breath after garlic tablets according to the
invention did not show a similar increase in peak 7.64. Similarly
after 30 hours peak RT 8.01 was only present after consumption of
the control garlic tablet without aqueous mint extract in the
enteric coat.
[0101] FIGS. 3 to 6 clearly demonstrate that the garlic tablets
according to the invention continue to inhibit the release of
objectionable sulfur compounds for a longer period than the Control
enteric coated tablets. Since tablets according to the invention do
not produce either of the tested compounds at a level above 2 ng/L,
example two illustrates that tablets according to the invention
substantially reduced garlic odor. These results also illustrate
that inclusion of aqueous extract in the external enteric coat
dramatically reduces garlic breath odour compared to an identical
tablet with only the enteric coating.
Comparison of Breath from Consumption of Garlic Homogenate with and
without Added Peppermint Extract
[0102] To determine if the odor reducing effect of the current
invention was simply due to addition of peppermint, a garlic
homogenate equivalent to the amount of garlic contained in the
tablet was consumed.
[0103] FIG. 7 shows the results obtained for diallyl disulfide in
breath from fresh garlic and fresh garlic with peppermint
extract.
[0104] FIG. 8 shows the results obtained for allyl mercaptan in
breath from fresh garlic and fresh garlic with peppermint
extract.
[0105] FIGS. 7 and 8 clearly show that whilst the peppermint
extract when included at many times the level incorporated into the
enteric coating does reduce the release of diallyl sulfide, it does
not have any odor reductive effects in relation to allyl
mercaptan.
CONCLUSION
[0106] Example 2 clearly demonstrates that the standard enteric
coating alone and the peppermint extract alone do not effectively
reduce garlic odor over extended periods of time. However, when an
enteric coating is applied to the garlic tablet which contains
peppermint extract, if a user consumes the garlic tablets daily
then garlic odor is effectively reduced for a more than two
days.
[0107] The word `comprising` and forms of the word `comprising` as
used in this description and in the claims does not limit the
invention claimed to exclude any variants or additions.
[0108] Modifications and improvements to the invention will be
readily apparent to those skilled in the art. Such modifications
and improvements are intended to be within the scope of this
invention.
* * * * *