Note: Descriptions are shown in the official language in which they were submitted.
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A PHARMACEUTICAL COMPOSITION, USE OF A PHARMACEUTICAL
COMPOSITION AND METHOD FOR TREATING THE SYMPTOMS OF EXCESS
ALCOHOL CONSUMPTION
FIELD OF THE INVENTION
10001] The
present invention relates generally to pharmaceutical compositions and methods
for treating the symptoms of alcohol cons-umption. More specifically, the
present invention may
preferably relate to compositions and methods for the treatment of the
symptoms of excessive
alcohol consumption with a combination of therapeutically effective arnounts
of an allcaloid, an
analgesic, an antiemetic, an electrolyte, an antidiantheal, an anti-foaming
agent, an anti-ulcer
agent, Opuntia ficus-indica and/or a fructose-containing product.
BACKGROUND OF THE' INVENTION
[0002]
Estimates of lost revenue due to reduced job productivity and absenteeism from
alcohol may be as high as $148 billion a year in the U.S. alone. Much of this
expense is related
to what is commonly referred to as "hang-overs" (i.e., symptoms of excessive
alcohol
consumption) in light to moderate
drinkers
(1-ittp://www.hopkinsmedicine.orgineuro1ogy neurosumervicenters
clinics/headache/conditions/
h2inaover headache.html). At least one report has found that 54% of all
workplace alcohol
issues (mainly hangover related) are caused by light drinkers and that 87% are
caused by light to
moderate drinkers (0 to 3 drinks / day for men; 0 to 1 drinks / day for
women).
[0003]
Based on various reports, the worldwide consumption of alcohol is rising. In
2010,
approximately 6.2 litres of pure alcohol was reported to be constune,c1 per
person at least 15 years
of age. In general, the greater the economic wealth of a country, the more
alcohol is consumed.
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As a rule, high-income countries have the highest alcohol per capita
consumption ("APC") and
the highest prevalence of heavy episodic or "binge" drinking ("HED") among
alcohol thinkers
(World Health Organizarion. Global status report on alcohol and health 2014,
accessible at
lity://vvww.who.int/substazwe abuse/publications/49hal aieohol report/an!),
HED iE defined
as the consumption of greater than 60 grams of pure alcohol (i.e., six or more
standard drinks in
most countries) on at least one single occasion at least monthly. The World
Health Organization
has also reported that the total APC (litres of pure alcohol) in the United
States will be from 7.5
to 9.9 anct in Canacia from 10.0 to t2.4 in the next 15 years (World !Icahn
Organization. Global
status report on alcohol and health 2014, accessible
at
hup://www.who.inr/substance abuse/publicationstiobal alcohol report/en/) and
the prevalence
of HED among current drinkers has also been estimated by the World Health
Organization
(World Health Organization. Global sratus report on alcohol and health 2014,
accessible at
hrtn://www.who.int/substance_abuse/publications/global_alcohol reporeen/) to
be between
20.0-29.9% in North America,
[0004] It has been reported that 10% of British males experience hangover-
related problems
at work at least monthly. It has also been estimated that 8% experience
hangover-related
problems at work in the United States, 4% for British females and 2% for
females in the United
States. The number of the population annually that experience hangovers in the
United States is
estimated to be half of those who experience hangovers in the United Kingdom.
[0005] Given the growing prevalence of HED and the estimates of lost
revenue and job
absenteeism clue to alcohol, there is a need to provide a composition that may
treat the symptoms
that often follow overconsumption of alcohol, By ameliorating the 'hang-over'
symptoms,
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individuals (i.e., social drinkers, stress / self-medicating drinkers, binge
drinkers, causal drinkers)
will be better able to perform their activities of daily living.
[00061 Commercially available products currently available and described in
the prior art
may comprise herbal remedies with unsubstantiated and pseudoscientific claims
of benefit.
[00071 It is an object of the present invention, therefore, to obviate
and/or mitigate one or
more of the aforementioned disadvantages and/or shortcomings associated with
the prior art, to
provide one of the aforementioned needs or advantages, and/or to achieve one
or more of the
aforementioned objects of the invention.
SUMMARY OF THE INVENTION
[0008] According to the present invention, there is disclosed a
pharmaceutical composition
for treating the symptoms associated with excess alcohol consumption in a
patient. The
pharmaceutical composition preferably, but need not necessarily, comprises
alone or in
combination, therapeutically effective amounts of one or more of an alkaloid,
an analgesic, an
antiemetic, an electrolyte, an antidiatTheal, an anti-foaming agent, an anti-
ulcer agent, Opuntia
ficus-indica and/or a fructose-containing product.
100091 AS may be known to persons skilled in the art, administering each of
the foregoing
medicinal ingredients separately (as is currently available) requires a large
volume of various
oral dosage forms (including the amount of fluids accompanying each medicinal
ingredient).
The combination of the different ingredients into a single oral dosage form
may preferably
improve patient compliance and therapeutic outcomes.
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10010]
Based preferably on the varying absorption times of the medicinal ingredients
and
potential synergistic drug-drug effects between the various ingredients of the
present invention,
there rnay be a synergy between the different medicinal ingredients such that
the cumulative
therapeutic effect on the hangover symptoms is greater than with each
medicinal ingredient used
indi vidually.
[0011]
According to the invention, there is preferably disclosed a pharmaceutical
composition for treating the symptoms associated with alcohol consuraption in
a patient. The
pharmaceutical composition includes a therapeutically effective amount of an
alkaloid, an
analgesic, an electrolyte, an antidiarrheal, an anti-foaming agent, an anti-
ulcer agent, Opuntia
fieus-indica, a fructose-containing product and pharmaceutically acceptable
excipients.
100121
According to the invention, the alkaloid of the pharmaceutical composition may
preferably include one or more alkaloids selected front the group consisting
of nicotine,
caffeine, morphine, quinine, theobromine, theacrine, theophylline, ephedrine,
and/or xanthine.
[00131
According to the invention, the analgesic of the pharmaceutical composition
may
preferably include one Or more analgesics selected from the group consisting
of: acetaminophen,
n n
nn-qe:rni cl a 1 a nti nflammatorY drua. saliCYlates, acetic acid derivatives,
eno I i c acid
derivatives, anthranilic acid derivatives, select cyc1ooxyengase-2 inhibitors
and/or opioids.
10014)
According to the invention, the electrolyte of the pharmaceutical composition
may
preferably include one or more electrolytes selected from the group consisting
of: a sodium salt
and/or a potassium salt.
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100151
According to the invention, the antidiarrheal of the pharmaceutical
composition rnay
preferably include one or more antidia,nheals selected from the group
consisting of: a bulking
agent, an absorbent, an anti-inflammatory compound, an anticholinergic, and/or
an opioid.
[00161
According to the invention, the antifoaraing agent of the pharmaceutical
composition
may preferably include simethicone.
1001'71
According to the invention, the anti-ulcer agent of the pharmaceutical
composition
may preferably include one or more anti-ulcer agents selected from the group
consisting of: an
H2 receptor antagonist, antacids, proton pump inhibitors and/or antibiotics.
[0018]
According to the invention, the fructose-containing product of the
pharmaceutical
composition may preferably include one or more fructose-containing products
selected from the
group consisting of: a honey extract and/or a propolis extract.
[00191
According to the invention, the pharmaceutical composition may also preferably
include an antiemetic.
[0020]
According to the invention, the antiemetic of the pharmaceutical composition
may
preferably include one or more antiemetics selected from the group consisting
of: a 5-11T3
remptor antagonist, a (1Qpaming 41-11A-gonipt, a NKl receptor antagonist, an
antihistamine, a
cannabinoid, a benzodiazepine, an anticholinergic, a steroid,
trimethobenzamide, ginger, emetrol,
propofol, peppermint, muscimol, and/or ajwain.
[0021]
According to the invention, there is preferably disclosed a use of a
pharmaceutical
composition. The pharmaceutical composition may include a therapeutically
effective amount of
an alkaloid, an analgesic, an electrolyte, an anticliarrheal, an anti-foaming
agent, an anti-ulcer
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agent, Opuntia ficus-indica, a fructose-containing product. and
pharmaceutically acceptable
excipients for the treatment of symptoms associated with excess alcohol
consumption in a
patient.
10022] According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following alkaloids: nicotine, caffeine,
morphine, quinine,
theobromine, theacrine, theophylline, ephedrine, and/or xanthine.
[00231 According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following analgesics: acetaminophen, a non-
steroidal anti-
inflammatory drug, salicylates, acetic acid derivatives, enolic acid
derivatives, anthranilie acid
derivatives, select cyclooxyengase-2 inhibitors and/or apioids.
(00241 According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following electrolytes: a sodiurn salt
and/or a potassium
salt.
[0025] According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following antidiarrheals: a bulking agent,
an absorbent, an
anti-inflammatory compound, an anticholinergic, and/or an opioid.
[0026] According to the invention, the use may preferably include a
pharmaceutical
composition with the anti-foaming agent simethicone.
[0027] According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following anti-ulcer agents: an 1-12
receptor antagonist,
antacids, proton pump inhibitors and/or antibiotics.
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[0028] According to the invention, the use may preferably include a
pharmaceutical
composition with one or more of the following fructose-containing products: a
honey extract
and/or a propolis extract.
[00291 According to the invention, the use may preferably include a
pharmaceutical
composition with an antiemetic.
[0030] According to the invention, the use may preferably include a
pharmaceutical
composition with one of more of the following antiemetics: a 5-HT3 receptor
antagonist, a
dopamine antagonist, a NKI receptor antagonist, an antihistamine, a
cannabinoid, a
benzodiazepine, an anticholinergic, a steroid, trimethobenzamide, ginger,
emetrol, propofol,
peppermint, muscimol, and/or ajwain.
[00311 According to the invention, there is preferably disclosed a method
for treating the
symptoms associated with excess alcohol consumption in a patient that includes
administering to
the patient, in one or more doses at predetermined time intervals, a
pharmaceutical composition.
The pharmaceutical composition may include a therapeutically effective amount
of one or more
medicinal ingredients selected from the group consisting of: an alkaloid, an
analgesic, an
antiemetic, an electrolytes, an antidiarrheal, an anti-foaming agent, an anti-
ulcer agent, Opuntia
ficus-indica and/or a fructose-containing product.
[00321 According to the invention, the method may preferably include a
first dose
formulation and a second dose formulation. The first dose formulation
comprises a first set of a
therapeutically effective amount of the one or more medicinal ingredients and
a second dose
formulation comprises a second set of a therapeutically effective amount of
the one or more
medicinal ingredi ents.
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100331 According to the invention, the method may preferably include
administering the
Second dose formulation at a predetermined time after the first dose
formulation.
[0034] According to the invention, the method may preferably include a
third dose
formulation. The third dose formulation comprises a third set of a
therapeutically effective
amount of the one or more medicinal ingredients.
f00351 According to the invention, the method may preferably include
administering the
second dose formulation at a predetermined time after the second dose
formulation arid a third
dose formulation at a predetermined time after the second dose formulation.
10036] According to the invention, there is disclosed methods and uses of a
pharmaceutical
composition of the present invention comprising alone or in combination a
therapeutically
effective amount of one or more of an alkaloid, an analgesic, an antiemetic,
an electrolyte, an
antidiarrhcal, an anti-foaming agent, an anti-ulcer agent, Opuntia ficus-
indica and/or a fructose-
containing product for the treatment or amelioration of symptoms associated
with excess alcohol
consumption in a patient.
100371 According to the invention, there is disclosed a method for treating
the symptoms
associated with excess alcohol consumption in a patient comprising
administering to the patient,
in one or more doses at predetermined time intervals, a pharmaceutical
composition comprising
alone or in combination a therapeutically effective amount of one or more of
an alkaloid, an
analgesic, an antiernetic, an electrolyte, an antidiarrheal, an anti-foaming,
an anti-ulcer agent,
Opuntia ficus-indica and/or a fructose-containing product.
[0038] Other advantages, features and characteristics of the present
invention, as well as
methods of operation and functions of the related elements of the system,
method, device and
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computer readable medium, and the combination of steps, pans and economics of
manufacture,
will becoine more apparent upon consideration of the following detailed
description and the
appended claims with reference to the accompanying drawings, the latter of
which are briefly
described hereinbel ow.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0039] The description that follows, and the embodiments described therein,
is provided by
way of illustration of an example, or examples, of particular embodiments of
the principles and
aspects of the present invention, These examples are provided for the purposes
of explanation,
and not of limitation, of those principles and of the invention.
[0040] It should also be appreciated that the present invention can be
implemented in
numerous ways, including as a use of the pharmaceutical composition or a
method for treating
symptoms associated with the overconsumption of alcohol or alcohol containing
beverages (e.g.
distilled alcoholic beverages (e.g. whiskey), brewed or fermented alcoholic
beverages (e.g. beer,
wine, etc.). It will be understood by a person skilled in the relevant art
that the term "alcohol" as
used herein refers to alcohol per se or anything containing alcohol that is
typically consumed by
users, In this specification, these implementations, or any other form that
the invention may
take, may be referred to as uses or methods, In general, the order of the
steps of the disclosed
methods may be altered within the scope of the invention,
100411 In this disclosure, a number of terms are used. The following
definitions of such
terms are provided.
[00421 As used herein, a person skilled in the relevant art may generally
understand the term
"comprising" to generally mean the presence of the stated features, integers,
steps, or
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components as referred to in the claims, but that it does not preclude the
presence or addition of
one or more other features, integers, steps, components or groups thereof.
[00431 As used herein, the skilled reader may generally understa,nd the
term "hang-over" to
generally mean the constellations of symptoms that typically develop following
alcohol
consumption. it will be understood that given variations in an individual's
physiology, physical
condition, etc. over time, the amount of alcohol that is required to induce
the symptoms of a
hangover may vary siertificantly between individuals and even for the same
individual. A person
skilled in the relevant art will understand that the amount of alcohol
consumed that ca.n be
defined as "excessive" (i.e., enough to induce a hangover) will vary between,
individuals and for
a given individual. The consumption of the amount of alcohol necessary for an
individual to
experience one or more of the symptoms associated with a hangover may be
referred to as
"overconsumption", overindulgence or the like.
[0044] Physiologic symptoms of a hangover may often be related to a
combination of
dehydration, metabolic changes, and dropping alcohol levels in the blood
stream. Hang-over
symptoms, may generally include, but are not limited to: fatigue, thirst and
dry mouth,
drowsiness and sleepiness, headache, nausea / upset stomach, diarrhea / gas /
intestinal bloating,
weakness, reduced alertness and concentration problems. These symptoms were
reported by at
least 75% of survey responders in Penning R. et al. Alcohol hangover symptoms
and their
contribution to the overall hangover severity. Alcohol. 2012; 47: 248-252.
[0045] As used herein, a person skilled in the relevant art may generally
understand the ten-n
"treatment to generally refer to an approach for obtaining beneficial or
desired results.
Beneficial ûr desired results can include, but are not limited to, prevention
OT prOphyla.xis,
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alleviation or amelioration of one Or more symptoms or conditions,
diminishment of the extent of
a disease, stabilized (i.e. not worsening) state of disease, preventing spread
of disease, delay or
slowing of disease progression, amelioration or palliation of the disease
state, and remission
(whether partial or total), whether detectable or undetectable, "Treatment"
can also mean
prolonging survival as compared to expected survival if not receiving
treatment.
[0046] As used herein, a person skilled in the relevant art may generally
understand the term
"therapeutically effective amount" to be an amount sufficient to effect
treatment when
administered to a subject in need of treatment. In the case of the embodiments
of the present
invention, a therapeutically effective amount can include, but is not limited
to, an amount that
eliminates or reduces the effects of the hang Over.
[00471 It will be understood by a person skilled in the relevant art that
the compositions of
the present invention can be formulated into pharmaceutical compositions for
administration in a
manner customary for administration of such materials using standard
pharmaceutical
formulation chemistries and methodologies, all of which are readily available
to a person skilled
in the relevant art. It will also be understood by a person skilled in the
relevant art that such
phaxmaceutical compositions may include one or more excipients, carriers,
stabilizers or other
pharmaceutically inactive compounds, such as, but not limited to, wetting or
emulsifying agents,
p1-1 buffering substances and the like. Pharmaceutically acceptable salts can
also be included
therein. A thorough discussion of pharmaceutically acceptable excipients,
vehicles ancl auxiliary
substances is available in Remington's. Pharmaceutical Sciences (Mack Pub. Co.
N.J. 1991),
incorporated herein by reference. Such pharmaceutical compositions can be
prepared as
injectable or oral preparations. The embodiments of the present invention may
be administered
by injection, including, but not limited to, intramuscular, intravenous,
subcutaneous, peritoneal,
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transderrnie or nasal injection. The therapeutically effective doses may vary
according to body
weight and the timing and duration of administration wili be determined by
specific clinical
research protocols.
[0048] It
will be understood by a person skilled in the relevant art that the term
"dose" refers
to the measured quantity of an agent, preferably a therapeutic agent, to be
taken at one time to
have a desired therapeutic effect(s). Preferably, "dose" as used herein means
a specified quantity
of a pharmaceutical or therapeutic agent provided in one or more
administration, It will be
farther understood that a "dosage unit" or "dosage form" as used herein means
a form in which
the active agent is provided. It will be understood that any known dosage form
may be
employed with the present invpntinn Th
rnay inc1iiç1. solid dosage forms. liquid domge
forms, gel dosage fonns, etc. The term "effective dose" or "effective dosage"
is defined as an
amount sufficient to achieve or at least partially achieve the desired effect.
The term
"therapeutically effective close" is defined as an amount sufficient to cure
or at least partially
arrest the disease and its complications in a patient already suffering from
the disease.
[00491 It
will be understood by a person skilled in the relevant art that the term
"administering" means providing a therapeutically active agent or composition
to a subject, and
includes, but is not limited to, administering by a medical professional and
self-administering.
100501 It
will be understood by a person skilled in the relevant art that a
"pharmaceutical
agent" or "therapeutic agent" as used herein means a substance that provides a
therapeutic effect
when administered to a subject. "Pharmaceutical composition" means a mixture
of substances
suitable for administering to an individual that includes one or more
pharmaceutical or
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therapeutically effective agents. The terms "active pharmaceutical ingredient"
shall be
understood to refer to a substance in a pharmaceutical composition that
provides a desired effect.
[0051) The treatment of the symptoms of excess alcohol consumption in
accordance with the
present invention and as hereinafter defined for the purposes of this
invention is directed to the
relief of the symptoms associated with the overindulgence of alcohol,
including but n.ot limited
to: fatigue, weakness, alertness, drowsiness, dehydration, headache, diarrhea,
gas / intestinal
bloating, and/or heartburn. One or more of the foregoing symptoms may be
caused at least in
part by the production of inflammatory mediators and/or blood alcohol
concentration. In a
preferred embodiment of tne presem invention, an agent ur aguniz wliich can
treat a range of
symptoms is recommended. Since no single active ingredient is presently
capable of treating the
multiple symptoms of excess alcohol consumption, a composition such as is
described in the
present invention is recommended.
[0521 Preferred embodiments of the present invention treat the one or more
symptoms of an
alcohol-induced hang-over, including, headache, nausea, gastroesophageal acid
reflux, and
somnolence.
[0053] Preferably, the pharmaceutical compositions of the present invention
may be
provided with different active ingredients, different strengths and/or
different formulations.
Preferably, the pharmaceutical composition of the present invention comprises
a therapeutically
effective amount of an alkaloid. A person skilled in the relevant art would
understand the term
"alkaloid" to refer to any of a class of nitrogenous organic compounds that
h.ave pronounced
physiological actions on humans. Alkaloids preferable include a large class of
organic, nitrogen
-
containing ring compounds of vegetable or synthesized origin, some of which
are liquid but most
CA 02919586 2016-02-01
of which are solid, that have a bitter taste, that are usually water-insoluble
and alcohol-soluble,
that combine with acids without the loss of a water molecule to form water-
soluble
hydrochlorides, hydrobromides, or the like, and that usually exhibit
pharmacological action, as
nicotine, caffeine, morphine, quinine, theobromine, theacrine, theophylline,
ephedrine, and
xanthine. Persons skilled in the art will appreciate that alkaloids may
include true alkaloids,
protoalkaloids, polyarnine alkaloids, peptide and cyclopeptide alkaloids,
and/or
pseudoal kalkoids
10054] Preferably, the alkaloid of the present invention may have central
nervous stimulating
effects, preferably for the treatment of symptoms including fatigue, weakness,
alertness and/or
drowsiness. Persons skilled in the art will understand that alcohol,
considered a depressant drug,
may supress the central nervous system (causing, for example, decreased rate
of breathing,
decreased heart rate, loss of consciousness, etc.). Persons skilled in the art
will also readily
appreciate that, following consumption, alkaloids such as caffeine act as
central nervous system
and metabolic stimulants. In accordance with one or more preferred embodiments
of the
invention, the pharmaceutical composition may preferably comprise an alkaloid
with a stimulant
effect including at least one of caffeine, theobromine or theophylline.
Pharmaceutical
compositions of the present invention may preferably comprise alkaloids such
as caffeine, in
amounts from about 0 to 200 mg per dose and preferably from about 0 to 120 mg
per dose. In
some alternate compositions of the present invention, persons skilled in the
art will appreciate
that sympathomirnetic drugs such as pseudoephedrine may be used for treating
the symptoms of
fatigue, weakness, alertness and/or drowsiness.
[00551 Preferably, the pharmaceutical composition of the present invention
may also
comprise a therapeutically effective amount of one or more analgesics. A
person skilled in the
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relevant art would understand the term "analgesic" to refer to any member of
the group of drugs
used to achieve analgesia, relief from pain, acting on the peripheral and/or
central nervous
systems. Analgesics include acetaminophen, non-steroidal anti-inflammatory
drugs ("NSAIDs";
including propionic acid derivatives such as ibuprofen, dexibuprofen,
naproxen, fenoprofen,
ketoprofen, dexketoprofen, flurbiprofen, oxaprozin, and/or loxoprofen;
salicylates; acetic acid
derivatives; enolic acid derivatives; anthranilic ac id derivatives; and/or
selective
cyclooxygenase-2 inhibitors), and opioid drugs such as morphine and oxycodone.
Preferably,
acetylsalicylic Acid and other NSAIDs, including but not limited to ibuprofen
and naproxen,
may preferably, but need not necessarily, be included in the pharmaceutical
composition for the
treatment of symptoms including pain and/or headache, Persons skilled in the
art will
under$tand that one or more symptoms of excess alcohol consumption may be
related to the
increased synthesis of prostaglandins and that nonselective and/or selective
inhibitors of the
enzyme cyclooxygenase preferably inhibit the formation of prostaglandins -
among other
biologic effects. In preferred embodiments of the invention, therapeutically
effective amounts of
NSAIDs, such as ibuprofen, may be present in the composition preferably from
about 0 to 400
mg per dose. While in a preferred embodiment of the present invention, the
composition
contains ibuprofen, persons skilled in the art win appreciate that alternative
NSAIDs, such as
naproxen or celecoxib or other short or long acting NSAIDs may be used in
accordance with the
present invention.
[00561 In some preferable enabodiments, a therapeutically effective amount of
acetaminophen is included in the composition as an alternative, or in
addition, to NSAIDs for the
treatment of symptoms including pain and/or headache, Similar to NSAIDs,
acetaminophen has
been reported to inhibit cyclooxygenase leading to an inhibition in the
formation of
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prostaglandins. In addition, acetaminophen provides analgesic and antipyretic
properties
comparable to acetylsalicylic acid and other NSAIDs. In some embodiments of
the present
invention, the composition may preferably comprise acetaminophen from about 0
to 500 mg per
dose,
T00571
Preferably, the pharmaceutical composition of the present invention comprises
a
therapeutically effective amount of one or more antiemetic. A person skilled
in the relevant art
would understand the term "antiemetic" to refer to a drug that is effective
against vomiting and
nausea and may include 5-1-1T3 receptor antagonists (e.g., dolasetron,
granisetron, ondansetron,
etc.), dopamine antagonists (e.g., domperidone, olanzapine, metoclopramide,
etc.), NK1 receptor
antagonists (e.g., aprepitant), antihistamines (e.g., cyclizine,
diphenhydramine, dimenhydrinate,
etc.), cannabinoids (e.g., cannabis, sativex, etc.), benzodiazepines (e.g.,
midazolam, lorazepam,
etc.), a,ntichol inergies (e.g., hyosci ne), steroids (e.g., dexamethaso ne),
trimethobenzami de,
ginger, emetrol, propofol, peppermint, muscimol, and ajwain, In preferred
embodiments, the
composition may comprise a therapeutically effective amount of dimenhydrinate
alone or in
combination with an electrolyte (e.g., sodium chloride or other electrolytes
known to persons
skilled in the art) to provide an antiemetic effect in persons who have
consumed excessive
amounts of alcohol. Symptoms such as nausea may be treated by including one or
both of
dimenhydrinate and/or an electrolyte in a preferred embodiment of the
composition. It will be
understood by a person skilled in the relevant art that alcohol is metabolized
into acetaldehyde
by liver enzyme alcohol dehydrogenase and that high concentrations of
acetaldehyde in the body
can cause nausea and vomiting. Moreover, excess alcohol consumption may
decrease
antidiuretic hormone ("ADH") levels in the body leading to dehydration and
potential electrolyte
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imbalances. The antiemetie effect of dimenhydrinatc may be due to antagonism
of the H1-
receptor in the vestibular system in the brain.
[0058] In
S ome embniiimpritc nf thc.. pre.sent invention. the composition comprises
dimenhydrinate from about 0 TO 100 mg per dose and preferably from about 0 to
25 mg per dose.
Persons skilled in the art will appreciate that other antierneties, such as
prochlorperazine and
ondansetron may be used in the composition instead of dimen.hydrinate.
[0059]
Preferably, the pharmaceutical composition of the present invention comprises
a
therapeutically effective amount of one or more electrolytes. A person skilled
in the relevant art
would understand the term "electrolyte" to refer to a substance that produces
an electrically
conducting solution when dissolved in a polar solvent, such as water,
Dissolved electrolytes
separate into cations and anions, which disperse uniformly through the
solvent. An electrolyte,
preferably but need not necessarily comprising soditun and potassium salts
(e.g., sodium
chloride), preferably replenish electrolyte levels in the body to restore
balance and/or prevent
imbalances. In some embodiments of the present invention, an electrolyte may
be present in the
composition from about 0 to 50 mg per dose and preferably from about 0 to 25
mg per dose.
[0060]
Preferably, the pharinaceutical composition of the present invention comprises
a
therapeutically effective amount of one or more antidiarrheal. A person
skilled in the relevant art
would understand the term "antidiarrheal" to refer to any medication which
provides
symptomatic relief for diarrhea, including but not limited to, bulking agents
(e.g.,
methylcellulose, plant fibres, etc.), absorbents, anti-inflarnmatory compounds
(e.g., bismuth
subsalicylate), anticholinergics, and/or opioids (e.g., loperamide). In
some preferred
embodiments, the composition further comprises a therapeutically effective
amount of
CA 02919586 2016-02-01
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loperamide for the treatment of symptoms including diarrhea. Persons .skilled
in the relevant art
rnay understand that excessive consumption of alcohol (acute or chronic) may
alter
gastrointestinal motility, including increasing colonic propulsive motility.
Such changes in
gastrointestinal function may, for example, contribute to diarrhea following
the acme
overconsumption of alcohol and chronic alcohol consumption. In addition, the
consumption of
alcohol may reduce the ability of the intestinal cells to absorb water,
resulting in higher volumes
of fluid in the intestinal tract. Persons skilled in the relevant art may
appreciate that loperamide,
an opioid-receptor agonist, decreases the activity of the myenteric plexus of
the large intestine
which in turn decreases the tone of the longitudinal and circular smooth
muscles of the intestinal
wall. This may effectively increase the amount of time substances retnain in
the intestine,
allowing for more water to be absorbed out of fecal matter (e.g., as the body
metabolizes the
alcohol in the system). In some embodiments of the present inveruion,
loperamide may be
present in the composition from about 0 to 16 mg per dose and preferably from
about 0 to 4 mg
per dose.
[0061i Preferably, the pharmaceutical composition of the present invention
comprises a
therapeutically effective amount of one or more anti-foaming agent. A person
skilled in the
relevant art would understand the term "anti-foaming agent" to refer to a
chemical additive that
reduces and hinders the formation of foam, such as simethicone. Some
embodiments of the
pharmaceutical composition may preferably, but need not necessarily, further
comprise a
therapeutically effective amount of simethicone, an anti-foaming agent, for
the treatment of
symptoms including intestinal bloating and/or discomfort or pain caused by
excessive gas in the
stomach or intestines. Persons of skill in the relevant art may appreciate
that such symptoms can
be caused by excessive alcohol consumption. Simethicone may increase the rate
at which
CA 02919586 2016-02-01
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formed gas exits the body by decreasing the surface tension of gaseous
bubbles, causing them to
combine into larger bubbles in the gastrointestinal tract and stomach that can
be passed more
easily. In accordance with some embodiments of the present invention,
simethicone may be
present in the composition from about 0 to 500 mg per dose and most preferably
from about 0 to
125 mg per dose.
[0()621
Preferably, the pharmaceutical composition of the present invention comprises
a
therapeutically effective amount of one or more anti-ulcer agent. A person
skilled in the relevant
art would understand the term "anti-ulcer agent" to refer to a class of drugs
used to treat ulcers in
the stomach and the upper part of the small intestine and may include acid
reducing medication
(e.g., 1-I2 receptor antagonists such as ranitidine and farnotidine, antacids,
proton pump
inhibitors) and/or when H. pylori infection is present., autibiutics (e.g.,
clarithromycin, metronidazole). In accordance with a preferred embodiment of
the present
invention, the composition preferably, but need not necessarily, further
comprises a
therapeutically effective amount of an anti-ulcer agent, such as ranitidine,
for the treatment of
symptoms related to stomach acid production. Certain alcoholic beverages
(e.g., beer and wine)
have been reported to be strong stimulants of gastric acid secretion and
gastrin release, In
addition, alcohol has also been reported to be a trigger for acid reflux
(i.e., stomach acid coming
up from the stomach into the esophagus). Occasional reflux may cause
heartburn, but chronic
reflux has been reported to result in reflux esophagitis, gastroesophageal
reflux disease and
sometimes Barrett esophagus. Ranitidine, a competitive, reversible inhibitor
of the action of
histamine at the histamine H2 receptors found in gastric parietal cells,
decreases gastric acid
secretion and gastric volume, as well as hydrogen ion concentration. In
accordance with some
embodiments of the present invention, ranitidine may be present in the
composition preferably
CA 02919586 2016-02-01
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=from about 0 to 150 mg per dose. Persons skilled in the art will appreciate
that alternative I-12
receptor antagonists (e.g., famotidine) or the class of proton pump inhibitors
(e.g., omeprazole,
lansoprazole, esomeprazole, etc,) may also be used in accordance with the
present invention.
[00631 In accordance with the present invention, the composition is
preferably taken with
water or other electrolyte containing beverage for th.e treatment of symptoms
including
dehydration. Alcohol has been reported to cause the body to increase urinary
output (i.e., a
diuretic). As aforesaid, alcohol may promote urine production by inhibiting
the release of ADI-1
or vasopressin. Reduced levels of ADH may prevent the kidneys from reabsorbing
water and
thereby increase urine production. Dehydration in combination with sweating,
vomiting and
diarrhea can result in additional fluid loss and electrolyte imbalances.
Persons skilled in the art
may appreciate that the ingestion of water or other electrolyte containing
beverage will
preferably contribute to the restoration of hydration and electrolyte balance.
Preferably, 1000 ml
of water or other electrolyte containing beverage is consumed along with the
composition.
0064] In preferred embodiments of the present invention, the pharmaceutical
composition
may preferably, but need not necessarily, contain a therapeutically effective
amount of Opuntia
ficus-indica to lessen the severity of the hangover symptoms. It has been
reported that the
symptoms of excessive constunption of alcohol may be related at least in part
to inflammation.
O. ficus-indica has been observed to inhibit the production of inflammatory
mediators,
potentially lessening the severity of the symptoms associated with excessive
alcohol
consumption. In accordance with the present invention, compositions comprising
O. ficus-inclica
are preferably ingested prior to the first alcoholic drink. In this way, such
compositions may
preferably serve as a preventative to reduce hangover symptoms associated with
overconsumption of alcohol. In accordance with some embodiments of the present
invention, O.
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ficus-indica may be present in the composition preferably from about 0 to 1600
IU per dose and
most preferably from about 0 TO 1600 IU per dose.
[0065] In accordance with some embodiments o tne present invention, the
composition may
include a therapeutically effective amount of a fructose-containing food
product (e.g., honey
extract). Tt has been reported that fructose-containing foods (e.g., honey)
may decrease blood
alcohol concentration. In accordance with the present invention, compositions
containing honey
extract may preferably, but need not necessarily, be ingested during a morning
application to
decrease the intensity of the symptoms associated with excess alcohol
consumption by reducing
blood alcohol concentration. In accordance with some embodiments of -the
present invention,
fructose-containing foods (e.g., honey extract, propolis extract) may he
present in the
composition from about 0 to 1000 mg per close and most preferably from about 0
to 25 mg per
dose.
[00661 The pharmaceutical composition is preferably, but need not
necessarily, ingested in a
multi-step or inulti-dose application. In a preferable embodiment of the
present invention,
formulations of the composition of the present invention may be administered
in various two or
three step regimens. A preferred embodiment involves a first regimen which may
comprise the
administration of a first dose of a formulation of the composition prior to or
during the episode
of alcohol consumption (e.g., before the onset of hangover symptoms) and one
or more
subsequent doses of a formulation of the composition following the episode of
alcohol
consumption (e.g., during or following the onset of hangover symptoms).¨ the
"Before and
After" regimen.
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[00671 More preferably, a further preferred embodiment involves a second
regimen which
may comprise the administration of a first dose of a formulation of the
composition following the
episode of alcohol consumption (e.g., during or following the onset of
hangover symptoms) and
one or more subsequent doses of a formulation of the composition at a
predetermined time after
the first close ¨ including, but not limited to, 4-24 hours, 12 hours, 8
hours, 6 hours, or 4 hours
after administration of the first dose. In accordance with preferred
embodiments of the present
invention, the formulation of the composition used for the first dose may be
the same or different
than the formulation of the composition used fol. the second dose.
100681 In accordance with embodiments of the present invention, the multi-
step application
may comprise a three step regimen. A first regimen may comprise the
administration of a first
dose of a formulation of the composition prior to or during the episode of
alcohol consumption
(e.g., before the onset of hangover symptoms), a second dose of a formulation
of the composition
following the episode of alcohol consumption (e.g., during or following the
onset of hangover
symptoms) and a third dose of a formulation of the composition at a
predetermined time after the
second dose ¨ including, but not limited to, 4-24 hours, 12 hours, 8 hours, 6
hours, or 4 hours
after administration of the second close. ln accordance with preferred
embodiments of the
present invention, the formulation of the composition used for the first dose
may be the same or
different than the formulation of the composition used for the second and/or
third dose.
Similarly, the formulation of the composition used for the second dose may be
the same or
different than the formulation of the composition used for the third dose.
[00691 In some embodiments of the invention, preventative treatments (e.g.,
Opuntia Ficus
Indica, which may prevent, or reduce the severity of, hangover symptoms if
administered in
CA 02919586 2016-02-01
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advance of the episode of alcohol consumption) may be combined with symptom-
directed
treatments (e.gõ acetaminophen and/or ibuprofen for pain relief).
[0070] An alternative embodiment of the present invention may comprise a
single-step
administration of the composition before, during or after the onset of
hangover symptoms.
[0071] The following examples set out various dose regimens using a variety
of formulations
of the pharmaceutical composition, in accordance with the present invention,
for the prevention
of hangover symptoms and/or the reduction or elimination of symptoms following
the onset of a
h angover.
[0072] Example 1
Night Before Morning After
Caffeine = 0 mg 80 mg
Ibuprofen 200 mg 200 mg
Acetaminophen 0 mg 325 mg
Dimenhydrinate 25 mg 0 mg
Ranitidine 75 mg 75 mg
Simethicone 0 mg 125 mg
Loperamicle 2 mg 2 mg
NaCl 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica 1000 IU .800 IU
100731 A first regular snength 2-step dosage (e.g., night before and
morning after) regimen
may preferably, but need not necessarily, comprise the administration of
formulations of the
composition in an oral dosage form (e,gõ a soluble powder, liquid, tablet, or
capsule). In the
present example, the formulation used for the first dose (i.e., Night Before)
preferably does not
CA 02919586 2016-02-01
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c,ornprise caffeine to reduce the probability that the user experiences
insomnolence. The first
dose may preferably, but need not necessarily, also comprise a higher strength
of Opuntia Ficus
indica to increase the probability of preventing, or reducing the severity of,
hangover symptoms.
In addition, the first dose also includes dimenhydrinate for treating the
symptoms of nausea, but
is not included in the second dose as dimenhyclrinate may cause drowsiness.
101)741 Example 2
Night Before Morning After
Caffeine 0 mg 1.00 mg
ibuprofen 200 nig 200 mg
Acetaminophen 0 mg 0 mg
Dimenhychiliate 0 mg 0 mg
Ranitidine 75 mg 75 mg
Simethicone 0 mg 125 rag
Loperami de 2 mg 2 mg
NaC1 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica 1000 ILI 800 IU .
100751 A second regular strength 2-step dosage (e.g., night before and
morning after)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the composition in an oral dosage form (e.g., a soluble powder, liquid, LJ1t
tn. 4.; apSuk). In the
present example, neither formulation includes acetaminophen.
(00761 Example 3
Night Before Morning After
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Caffeine = 0 mg 120 mg
Ibuprofen 400 mg 400 mg
Acetaminophen 0 mg 500 mg
Dimenhydri nate 25 mg 0 mg
Ranitidine 150 mg 150 mg
Simethi cone 0 mg 125 mg
Loperamide 2 mg 2 mg
NaC1 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica 1600 IU 1000 TU
[00771 A first extra strength 2-step dosage (e.g., night before and morning
after) regimen
may preferably, but need not necessarily, comprise the administration of
formulations of the
composition in an oral dosage form (e.g., a soluble powder, liquid, tablet or
capsule). The extra
strength formulations preferably, but need not necessarily, comprise greater
amounts of one or
more medicinal ingredients as compared to the regular strength formulations.
[0078] Example 4
Night Before Morning After
Caffeine 0 mg 120 mg
Ibuprofen 400 mg 400 mg
Acetaminophen 0 mg 0 mg
Dimenhydrinate 0 mg 0 mg
Rani ti dine 150 ing 150 mg
Simethicone 0 mg 125 mg
Loperarnide 2 mg 2 mg
NaCI 0 mg 25 mg
Honey Extract 25 mg 0 mg
CA 02919586 2016-02-01
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Opuntia Ficus Indica 1600 IU 1000 IU
[00791 A second extra strength 2-step dosage (e.g., night before and
morning after) regimen
cotnposition may preferably, but need not necessarily, comprise the
administration of
formulations of the composition in an oral dosage form (e.g., a soluble
powder, liquid, tablet or
capsule). In the present example, neither formulation includes acetaminophen.
100801 Example 5
Morning After =Morning After
+6 hrs
Caffeine 80 mg 80 mg
Ibuprofen 200 mg 200 mg
Acetaminophen 325 mg 500 mg
Dimenhydrinate 0 mg 0 mg
Ranitidi ne 75 mg 75 mg
Simethicone 125 mg 125 mg
L op eramide 2 mg 2 mg
1\11aCI 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica. 1000 IU 800 IU
[00811 A third normal strength 2-step dosage (e.g., morning oiler and
morning after + 6
hours) regimen may preferably, but need not necessarily, comprise the
administration of
formulations of the composition in an oral dosage form (e.g., a soluble
powder, liquid, tablet or
capsule), In the present example, both formulations contain caffeine and the
formulation used
CA 02919586 2016-02-01
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for the second dose contains a greater amount of acetaminophen than the
formulation used for
the first dose as it may provide greater pain relief.
[0082] Example 6
Morning After Morning After
+6 hrs
Caffeine 100 mg 80 mg
Ibuprofen 200 mg 200 mg
Acetaminophen 0 mg 325 mg
Dimenhydrinate 0 mg .25 mg
Ranitid ine 75 mg 75 mg
Si methicone 125 mg 125 mg
Loperamicle 2 mg 2 mg
NaC1 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica 1000 IU 800 ILI
[0083] A fourth normal strength 2-step dosage (e.g., morning and morning
after t 6 hours)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the cUlnpOSitiOn in an oral dosage form (e.g., a soluble powder, liquid,
tablet or capsule.), In the
present example, the formulation used for the first dose contains a greater
amount of caffeine
than the formulation used for the second dose. In addition, the formulation
for the second dose
contains acetaminophen. The "Morning After" (alternately, "first dose")
formulation preferably
provides relief of the hangover symptoms (e.g., fatigue, weakness, alertness,
drowsiness,
dehydration, headache, diarrhea, gas, intestinal bloating, and heartburn), The
"Morning After"
formulation also comprises an electrolyte, NaC1, to reduce nausea symptoms.
After a certain
CA 02919586 2016-02-01
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time interval (approximately 6 hours and noted as "Morning After + 6 hours",
alternately,
"second dose"), a second dose is administered to prolong and/or enhance the
effectiveness of the
composition in eliminating and/or reducing the severity of one or more
hangover symptoms.
Caffeine is reduced in the second dose to preferably provide alertness while
limiting potential
caffeine side effects. The second dose comprises acetaminophen to preferably
improve the
effectiveness of headache and pain relief jointly and synergistically with
ibuprofen, while being
administered at a predetermined time interval to prevent and/or minimize the
possible
metabolism interaction between high doses of alcohol and high doses of
acetaminophen. The
second dose, instead of the first dose, also comprises dimenhydrinate TO
preferably reduce and/or
eliminate fatigue-related symptoms and to prioritize the alertness effects
from the caffeine in the
first dose while reducing nausea symptoms, Opuntia Ficus Indica and honey
extract are reduced
and/or eliminated in the second dose preferably to maintain the consumption
dose for size and
mass of the patient.
[0084] Example 7
Morning After Morning After
+6 hrs
Caffeine 120 mg 120 mg
Ibuprofen 400 ing 400 mg
Acetaminophen 325 mg 500 mg
Dimenhydrinate 0 mg 0 mg
Raniti dine 150 mg 150 mg
S imethicoae 125 mg 125 mg
Loperamide 2 mg 2 mg
NaCl 0 mg 25 rag
Honey Extract 25 mg 0 mg
CA 02919586 2016-02-01
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Opuntia Ficus Indica 1600 TU 1000 ILI
[00851 A third extra strength 2-step dosage (e.g., morning and morning
after + 6 hours)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the composition in an oral dosage form (e.g., a soluble powder, liquid, tablet
or capsule). The
extra strength formulations preferably, but need not necessarily, comprise
greater amounts of one
or more medicinal ingredients as compared to the regular strength
formu[ations.
[0086] Example 8
Morning After Morning After
+6 hrs
Caffeine 140 mg 120 mg
Ibuprofen 400 mg 400 mg
Acetaminophen 0 mg 500 mg
Dimenhydri nate 0 mg 25 mg
Ranitidine 150 mg 150 mg
Simethicone = 125 mg 125 mg
Loperarnide 2 rng 2 mg
NaC1 0 mg 25 mg
Honey Extract 25 mg 0 mg
Opuntia Ficus Indica 1600 IU 1000 ILI
[00871 A fourth extra strength 2-step dosage (cg., morning anti iiiuming
aft& i 6 hou1'3)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the composition in an oral dosage form (e.g., a soluble powder, liquid, tablet
or capsule). In the
present example, the formulation used for the second dose includes
acetaminophen and
CA 02919586 2016-02-01
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dirnenhydrinate. The "Morning After" (a)ternately, "first dose") formulation
preferably provides
relief of the hangover symptoms (e.g., fatigue, weakness, alertness,
drowsiness, dehydration,
headache, diarrhea, gas, intestinal bloating, and heartburn). The first dose
preferably comprises
an electrolyte, NaCl, to reduce nausea symptoms. After the first dose, a
second dose is
preferably administered to enhance and/or prolong the effect of the first dose
in eliminating
and/or reducing the severity of the hangover symptoms. The amount. of caffeine
in the second
dose is reduced to preferably provide alertness while limiting caffeine side
effects. The second
close comprises acetaminophen to preferably improve the effectiveness of
headache and pain
relief jointly and synergistically with ibuprofen, while being administered at
a predetermined
time interval to prevent and/or minimize the possible metabolisrn interaction
between 1411 doses
of alcohol and high doses of acetaminophen. The second close, instead of the
first dose, also
comprises dirnenhydrinate to preferably reduce and/or eliminate fatigue-
related symptoms and to
prioritize the alertness effects from the caffeine in the first dose while
reducing nausea
symptoms, C.)puntia Ficus Indica and honey extract are red.uced and/or
eliminated in the second
dose preferably to maintain the constunption dose for size and mass of the
patient.
[0088] Example 9
Night Before Morning After Morning After
+6 hrs
Caffeine 0 mg 80 mg 80 mg
Ibuprofen 200 mg 200 mg = 200
mg
Acetaminophen 0 mg 325 mg 325 mg
Dimenhydrinate 25 mg 0 mg 0 mg
Raniticline 75 mg 75 mg 75 mg
S i me thicone 0 m.g 125 mg 125 mg
Loperamide 2 mg 2 mg 2 mg
CA 02919586 2016-02-01
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NaC1 0 mg 25 mg 25 mg
Honey Extract 25 mg 10 mg 0 mg
Opuntia Ficus Indica 1000 IU 800 IU 0 IU
[00891 A first normal strength 3-step dosage (e.g., night, morning =and
morning after -I- 6
hours) regimen may preferably, but need not necessarily, comprise the
administration of
formulations of the composition in an oral dosage form (e.g;., a soluble
powder, liquid, tablet or
capsule). In the present example, the formulation used for the first dose
(i.e., Night Before)
preferably does not comprise caffeine to reduce the probability that the user
experiences
insomnolence. The "Night Before" (alternately, "first close") formulation is
preferably
administered in advance of alcohol consumption to preferably prevent, reduce
or eliminate
hangover symptoms. For prevention, the first dose preferably comprises honey
extract and
Opuntia Ficus Indica to prevent or reduce inflammation and reduce blood
alcohol
concentrations, while dimenhydrinate is preferably included to limit or
prevent the development
uf iiuç. Loperamidc is preferably included to 'maintain water retention, while
ranitidine is
preferably included to prevent or lessen the severity of acid reflux (i.e.,
rather than allowing the
symptom to occur in the first place and treating it afterwards). Caffeine is
preferably MN
included in the first dose as this may prevent the patient from sleeping. The
"Morning After"
(alternately "second dose") dosage preferably reduces the amounts of Opuntia
Ficus Indica,
honey extract, and dimenhydrinate as the treatment objective preferably
switches from hangover
prevention to hangover symptom relief. The second dose formulation targets the
spectrum of
hangover symptoms (e.g., fatigue, weakness, alertness, drowsiness,
dehydration, headache,
dieu.ihc.-,a, gas, intestinal bloating, and heartburn) to preferably provide
signitioant relief of thc
hangover symptoms. Caffeine is preferably included in the second dose to
increase the patients'
CA 02919586 2016-02-01
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alertness and functionality. An electrolyte, NaCl, is also added in the second
dose to preferably
reduce nausea symptoms. The "Morning After +6hrs" (alternately "third dose")
dosage is
administered to preferably ensure or enhance the effectiveness of treating the
hangover
symptoms. Caffeine is preferably held at a consistent strength to preferably
provide alertness
while limiting caffeine side effects. For both the second dose and third dose,
acetaminophen is
added to preferably enhance the effectiveness of headache and pain relief
jointly and
synergistically with ibuprofen, while being administered at a preoeterrnined
time Imerva Lu
not impact or reduce the impact possible metabolism interaction between high
dosages of alcohol
and high dosages of acetaminophen. Opuntia Ficus Indica and honey extract are
reduced and/or
eliminated in the second dose and third dose preferably to maintain the
consumption dose for
size and mass of the patient.
100901 Example 10
Nipht Before Morning After = Morning After
+6 hrs
Caffeine 0 mg 80 mg 80 mg
Ibuprofen 200 mg 200 mg 200 mg
Acetaminophen 0 mg 0 mg 325 mg
Dimenhydrinate 0 mg 0 mg 25 mg
Rani tidine 75 mg 75 mg 75 mg
Simethicone 0 mg 125 mg 125 mg
Loperamide 2 mg 2 mg 2 mg
NaCI 0 mg 25 mg 25 mg
Honey Extract 25 mg 10 mg 0 mg
Opuntia Ficus Indica 1000 IU 800 III 0 IU
CA 02919586 2016-02-01
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[0091] A
second normal strength 3-step dosage (e.g., night, morning and morning after
+6
hours) regimen may preferably, but need not necessarily, comprise the
administration of
formulations of the composition in an oral dosage form (e.g., a soluble
powder, liquid, tablet or
capsule). The "Night Before" (alternately, "first dose") formulation is
preferably administered in
advance of alcohol consumption to preferably prevent, reduce or eliminate
hangover symptoms.
For prevention, the first dose preferably comprises honey extract and Opuntia
Ficus Indica to
prevent or reduce inflammation and reduce blood alcohol concentrations, while
dimenhydrinate
is nreferablv included to limit or prevent the development of nausea.
Loperamide is preferably
included to maintain water retention, while ranitidine is preferably included
to prevent or lessen
the severity of acid reflux (i.e., rather than allowing the symptom to occur
in the 'first place and
treating it afterwards). Caffeine is preferably not included in the first dose
as this may prevent
the patient from sleeping. The "Morning After" (alternately "second dose")
dosage preferably
reduces the amounts of Opuntia Ficus Indica, honey extract, and dimenhydrinate
as the
treatment objective preferably switches from hangover prevention to hangover
symptom relief.
The second dose formulation targets the spectrum of hangover symptoms (e.g.,
fatigue,
weakness, alertness, drowsiness, dehydration, headache, diarrhea, gas,
intestinal bloating, and
heartburn) to preferably provide significant relief of the hangover symptoms.
Caffeine is
preferably included in the second dose to increase the patients' alertness and
functionality An
electrolyte, NaCl, is also added in the second dose to preferably reduce
nausea symptoms. The
"Morning After +61irs" (alternately "third. dose") dosage is administered to
preferably ensure or
enhance the effectiveness of treating the hangover symptoms. Caffeine is
preferably held at a
consistent strength to preferably provide alertness while limiting caffeine
side effects. For both
the second dose and third dose, acetaminophen is added to preferably enhance
the effectiveness
of headache and pain relief jointly and synergistically with ibuprofen, while
being adminigered
CA 02919586 2016-02-01
j4 -
at a predetermined time interval as to not impact or reduce the impact
possible metabolism
interaction between high dosages of alcohol and high dosages of acetaminophen.
Opuntia Ficus
indica and honey extract are reduced and/or eliminated in the second dose and
third dose
preferably to maintain the consumption dose for size and mass of the patient.
[00921 Example 11
Night Before Morning After Morning After
+6 hrs
Caffeine 0 mg 120 mg 120 mg
Ibuprofen 400 mg 400 mg 400 mg
Acetaminophen 0 mg 500 mg 500 mg
Dime nhydri n ate 25 mg 0 mg 0 mg
Raniti di ne 150 mg 150 mg 150 mg
Simethicone 0 mg 125 mg 125 mg
Loperamide 2 mg 2 mg 2 mg
NaCl 0 mg 25 mg 25 mg
Honey Extract 25 mg 10 mg 0 mg
Opuntia Ficus Indica 1600 IU 1000 IU 0 IU
10093] A first extra strength 3-step dosage (e.g., night, morning and
morning after +6 hours)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the composition in an oral dosage form (e.g., a soluble powder, liquid, tablet
or capsule). The
extra strength formulations preferably, but need not necessarily, comprise
greater amounts of one
or more medicinal ingredients as compared to the regular strength
formulations. The "Night
13efore" (alternately, "first dose") formulation is preferably administered in
advance of alcohol
consumption to preferably prevent, reduce or eliminate hangover symptoms. For
prevention, the
CA 02919586 2016-02-01
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first dose preferably comprises honey extract arid Opuntia Ficus Indica to
prevent or reduce
inflammation and reduce blood alcohol concentrations, while dimenhydrinate is
preferably
included to limit or prevent the development of nausea. Loperarnide is
preferably included to
maintain water retention, while ranitidine is preferably included to prevent
or lessen the severity
of acid reflux (i.e., rather than allowing the symptom to occur in the first
place and treating it
afterwards). uarteine is preferably not Included ill L1I ìi duw:.- as thi3
rnay prevent the patient
fsrom sleeping. The "Morning After" (alternately "second dose") dosage
preferably reduces the
amounts of Opuntia Ficus Indica, honey extract, and climenhydrinate as the
treatment objective
preferably switches from hangover prevention to hangover symptom relief. The
second dose
formulation targets the spectrum of hangover symptoms (e.g,, fatigue,
weakness, alertness,
drowsiness, dehydration, headache, diarrhea, gris, inteminal bloating, and
heartburn) to preferably
provide significant relief of the hangover symptoms. Caffeine is preferably
included in the
second dose to increase the patients' alertness and. fhtictionality. An
electrolyte, NaC1, is also
added in the second dose to preferably reduce nausea symptoms, The "Morning
After +6hrs"
(alternatoly "third cloe") dosage. 'lc adrniniqtered to preferably ensure or
enhance the
effectiveness of treating the hangover symptoms. Caffeine is preferably held
at a consistent
strength to preferably provide alertness while limiting caffeine side effects.
For both the second
dose and third dose, acetaminophen is added to preferably enhance the
effectiveness of headache
and pain relief jointly and synergistically with ibuprofen, while being
administered at a
predetermined time interval as to not impact or reduce the irnpact possible
metabolism
interaction between high dosages of alcohol and high dosages of acetaminophen.
Opuntia Ficus
Indica and honey extract are reduced and/or eliminated in the second dose and
third dose
preferably to maintain the consumption dose for size and mass of the patient.
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[00941 Example 12
Night Before 1Viorning After Morning After
+6 hrs
Caffeine 0 mg 150 mg 120 mg
Ibuprofen 400 mg 400 mg 400 mg
Acetaminophen 0 mg 325 mg 500 mg
Di rn enhydrinate 0 mg 0 mg 25 mg
Ranitidi ne 150 mg 150 mg 150 mg
S imethicone 0 mg 125 mg 125 mg
Loperam i de 2 mg 2 mg 2 mg
NaC1 0 mg 25 mg 25 mg
Honey Extract 25 mg 10 mg 0 mg
Opuntia Ficus Indica 1600 TU 1000 IU 0 TU
[0095] A second extra strength 3-step (e.g,, night, morning and morning
after + 6 hours)
regimen may preferably, but need not necessarily, comprise the administration
of formulations of
the composition in an oral dosage form (e.g., a soluble powder, liquid, tablet
or capsule). The
"Night Before" (alternately, "first close") formulation is preferably
administered in advance of
alcohol consumption to preferably prevent, reduce or eliminate hangover
symptoms. For
prevention, the first dose preferably comprises honey extract and Opuntia
Ficus Indica to
prevent or reduce inflammation and reduce blood alcohol concentrations, while
dimenhydrinate
is preferably included to limit or prevent the development of nausea.
Loperamide is preferably
included to maintain water retention, while ranitidine is preferably included
to prevent or lessen
the everity of acid reflux (i.e., rather than allowing the symptom to occur in
the first place and
treating it afterwards). Caffeine is preferably not included in the first dose
as this may prevent
the patient from sleeping. The "Morning After" (alternately "second dose")
dosage preferably
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reduces the amounts of Opuntia FiC14.1 Indica, honey extract, and
dimenhydrinate as the
treatment objective preferably switches from hangover prevention to hangover
symptom relief.
The second dose formulation targets the spectrum of hangover symptoms (e.g.,
fatigue,
weakness, alertness, drowsiness, dehydration, headache, diarrhea, gas,
intestinal bloating, and
heartburn) to preferably provide significant relief of the hangover symptoms.
Caffeine is
preferably included in the second dose to increase the patients alertness arid
functionality An
electrolyte, NaC1, is also added in the second dose to preferably reduce
nausea symptoms. The
"Morning After -h6hrs" (alternately "third dose") dosage is administered to
preferably ensure or
enhance the effectiveness of treating the hangover symptoms. Caffeine is
preferably held at a.
consistent strength to preferably provide alertness while limiting caffeine
side effects. For both
the second dose and third dose, a.cetarninophen is added to preferably enhance
the effectiveness
of headache and pain relief jointly and synergistically with ibuprofen, while
being administered
a a predetermined time interval as to not impact or reduce the impact possible
metabolism
interaction between high dosages of alcohol and high dosages of acetaminophen.
A smaller
dosage of acetaminophen is preferably administered during the second dose,
while a larger
dosage of acetaminophen is preferably administered during the third dose to
preferably improve
hangover symptom relief, Opuntia Ficus Indica and honey extract are reduced or
eliminated in
the second dose and third close to preferably maintain the consumption dose
for size and mass of
the patient.
10096] Example 13
[0097] Background:
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[0098] A test formulation comprising a combination of caffeine (30 mg),
dimenhydrinate (25
mg), ibuprofen (200 mg), and ranitidine (75 mg) in was prepared in a capsule
dosage form to
study the effective of the combination on preventing, reducing, and/or
eliminating hangover
symptoms.
[0099] Objective:
[00100] To assess whether the test formulation described above is effective in
preventing,
reducing, and/or eliminating hangover symptoms associated with a hangover.
[00101] Methods:
[00102] Three (3) study subjects volunteered. Each subject consumed a greater
volume of
alcohol than each subject was accustomed to in order to increase the
likelihood of developing a
hang-over. The following morning, each subject was administered at least I
capsule of the test
formulation and then qualitatively assessed whether the hangover symptoms
improved.
[00103] Results:
[00104] All three (3) subjects participated and each consumed a larger volume
of alcohol than
each subject was accustomed. Each subject self-reported on the presence of at
least one of the
following hangover symptoms: nausea, headache, drowsiness, and/or heartburn.
Each subject
ingested at least 1 capsule of the test formulation and one (l) subject
ingested 2 capsules of the
test formulation separated by 4 ¨ 6 hours. Each subject rated an improvement
in the hangover
aymptarn reported. No obviou5a adverse effertc rif the ti formulation were
identified.
[00105] Conclusions:
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[00106] The test formulation may be effective in ameliorating symptoms in
potential
hangover patients. Further studies may be needed to qualitatively and/or
quantitatively assess
symptom improvement and determine the preferred medicinal ingredients to
include in the
composition as well as the potential adverse effects associated with same.
[00107) The
sthove description is ninFini to be exemplary only, ancl one skilled in the
art will
recognize that changes may be made to the embodiments described without
departing from the
scope of the invention disclosed, Modifications which fall within the scope of
the scope of the
present invention will be apparent to those skilled in the art, in light of a
review of this
disclosure, and such modifications are intended to fall within the appended
claims.
[00108] This concludes the description of presently preferred embodiments of
the invention.
The foregoing description has been presented for the purpose of illustration
and is not intended
to be exhaustive of to limit the invention to the precise form disclosed.
Other modification,
variations and alterations are possible in light of the above teaching and
will be apparent to those
skilled in the art, and may be used in the design and manufacture of other
embodiments
according to the present invention without departing from the spirit and scope
of the invention.
It is intended the scope of the invention be limited be limited not by this
description but only by
the claims forming a part hereof.
