Weight loss abstract
This invention discloses a new and unique combination of octopamine,
yohimbine, bergenin and decaffeinated green tea extract useful as
an oral supplement for increasing weight loss in humans.
Weight loss claims
1. A weight loss method comprising administering a composition
of matter comprising octopamine, yohimibine, bergenin, and decaffeinated
green tea extract in amounts effective to promote weight loss.
2. A weight loss method comprising administering a composition
of matter comprising octopamine, bergenin, and decaffeinated green
tea extract in amounts effective to promote weight loss.
Weight loss description
CROSS-REFERENCE TO RELATED APPLICATIONS
STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT
REFERENCE TO A MICROFICHE APPENDIX
BACKGROUND OF THE INVENTION
Prior art relating to this invention concerns distinct areas previously
not combined to create new and useful formula sets regarding a solid-dosage
form of a weight loss product.
This invention relates a new and unique combination of octopamine,
yohimbine, bergenin and decaffeinated green tea extract useful for
increasing weight loss.
Octopamine is a naturally-occurring catecholamine structurally
related to norephinephrine, and has been proven in in-vitro studies
to be a potent selective beta-3 agonist (C R Acad Sci III 1993;316(5):519-23).
Beta-3 receptors can be found in both human white and brown adipose
tissues, and play an important role in lipolysis and thermogenesis
in our bodies. They are vastly more important than previously thought
by scientists, who often had difficulty in the past discerning the
contribution of each beta-receptor subtype (1,2 and 3) without having
agents selective for each to investigate. Various techniques were
devised to try, but for a long time reports were not in favor of
beta-3 receptors having much of a role in humans. It was not until
a study conducted with ephedrine in 1995, however, that surprising
new data started to arise in support of a beta-3-mediated pathway
to fat loss. Using beta blocking agents investigators were able
to demonstrate that beta-3 agonist activity likely accounted for
at least 40% of the thermogenesis induced by this popular weight
When a synthetic selective beta-3 agonist was finally developed
and studied in humans in 2001, the important role of this receptor
became an unquestionable fact (Clin Pharmacol Ther 2002;71:272-9).
In this investigation a group of 12 otherwise healthy overweight
men noticed a clear increase in lipolysis, as well as total energy
expenditure, with the use of a beta-3 agonist exclusively. We are
sure the intended action of the drug was solely responsible for
these effects because heart-rate and diastolic blood pressure did
not increase in any of the subjects (signs that non-selective beta
agonistic activity were occurring), nor did the concentrations of
the endogenous adrenergic hormones epinephrine and norepinephrine.
Leptin, a hormone often relevant to weight loss, also did not change
during the study. We are left with proof that beta-3 receptors are
important triggers of lipolysis and thermogenesis in humans, and
have opened a new door to weight loss without the uncomfortable
jitters and central nervous system stimulation noted with non-selective
beta agonists like ephedrine (selective beta-3 agonists do not produce
the same strong CNS stimulation).
Yohimbine is an extremely potent naturally-occurring alpha-2 receptor
antagonist. Adrenergic lipolysis in human adipose tissue is regulated
in a dual nature by adrenoceptors. Most notably, activation of the
beta-2 or beta-3 subtype increases the process of lipolysis; while
activation of alpha-2 receptors diminishes it (fat cells appear
to be the only type of cells in the human body that exhibit such
dual regulation by adrenoceptors). Studies with yohimbine, in the
form of yohimbine HCL, have shown that it is capable of increasing
lipolysis in humans after oral dosing, likely via both alpha-2 receptor
antagonism and increases in synaptic norephinephrine release (Eur
J Clin Invest 1988;18:587-94). In effect it serves both beta stimulating
and alpha blocking properties, an ideal combination if we want to
stimulate fat loss. However, when single doses as high as 21.6 mg
(J Clin Pharmacol 1996;36:814-22), or daily cumulative doses as
high as 43.2 mg (J Urol 1995;141:1360-63), were taken, the agent
was well tolerated, and had no significant impact on blood pressure
or heart rate as would be expected of a beta-agonist like ephedrine.
Green tea leaf (camellia sinensis) extract has been around for
centuries, and has been used in herbal medicine for about as long.
Early on its beneficial properties were noticed, particularly in
Asian cultures where Green Tea has been widely consumed and often
thought of as a having numerous positive health benefits. In recent
years scientists have been investigating the content and actions
of Green Tea, and are coming to confirm with solid evidence many
of its positive effects including those as an anti-oxidant, cholesterol
lowering, antidepressant, capillary-strengthening and lipolysis-enhancing
agent. Early suggestions were that its caffeine content was solely
responsible for its ability to increase fat loss; however this was
fundamentally dismissed in a study published in 1999 that demonstrated
green tea to have an effect that could not be duplicated with an
equivalent dose (50 mg) of caffeine (Int J Obesity 2000;24:252-58).
In this investigation green tea increased 24 hour energy expenditure
significantly, where the caffeine had no noticeable effect. It looks
now like its high content of tea-catechins, particularly EGCG, which
are the source of its activity here. Studies with Green Tea extract
with standardized amounts of EGCG have suggested it exerts a direct
effect on thermogenesis by increasing the respiration rate of brown
fat cells, and furthermore that it can strongly enhance the lipolytic
action of other chemicals or agents acting on this system (Am J
Clin Nutr 1999;70:1040-5). In-vitro tea catechins like EGCG were
shown to inhibit the COMT enzyme, which is responsible for degrading
the adrenergic hormone norephinephrine (J Med Chem 1975;18:120-2).
Since norepinephrine has an important role in human thermogenesis
and fat metabolism, this likely accounts for much of its positive
Bergenin comes from eastern herbal medicine originally, where it
is found in the form of a plant extract called "Shengma".
It is one of the now known active components of this plant extract,
and has been shown to have an action in the body that augments the
lipolytic action of norepinephrine. In-vitro studies have confirmed
that while this compound itself does not directly stimulate lipolysis
or have measurable adrenergic activity, but it markedly enhances
lipolysis enduced by an adrenergic hormone such as norepinephrine
(J. Nat Prod 1998;61:1006-11). It is further documented to oppose
the lipogenic (fat building) actions of insulin. Its exact mode
of action is unknown at this time, but it is believed to involve
increased norepinephrine binding affinity to phosholipids on fat
By triggering adrenergically-mediated lipolysis and thermogenesis
with a carefully blended combination of octopamine and yohimbine,
while simultaneously supporting the adrenergically-mediated activities
of these compounds with a carefully blended composition of bergenin
and decaffeinated green tea extract, this new product provides a
unique and effective method for losing weight.
BRIEF SUMMARY OF THE INVENTION
Prior art relates many dietary supplement formulations for the
purpose of increasing weight loss. Many, however, focus on the use
of strong central nervous system stimulants such as caffeine and
ephedrine (or its alkaloids). Although effective in many cases,
stimulant-based weight loss products are often uncomfortable for
many users due to the side effects related to their potential effects
on the central nervous system, which may include restlessness, increased
heart rate, sweating or insomnia. Prior art also discloses four
compounds of interest to this inventor that are without strong stimulant
properties, but which heretofore had not been combined to create
a new and useful weight loss product. The problem of this invention
was therefore to provide a new and unique composition for increasing
weight loss in humans, but without the use of strong stimulants.
According to this invention this problem is solved with a carefully
blended composition containing octopamine, yohimbine, bergenin and
decaffeinated green tea extract.
BRIEF DESCRIPTION OF THE SEVERAL VIEWS OF THE DRAWING
DETAILED DESCRIPTION OF THE INVENTION
This invention discloses the formula sets that embody the invention
of the supplement composition for increasing weight loss in humans.
The combination of octopamine, yohimbine, bergenin and decaffeinated
green tea extract increases lipolysis, thermogenesis and weight
loss, and is safe and much less apt to cause the side effects normally
associated with stimulant-based weight loss products.
We now discuss in detail the preferred versions, variants, or embodiments
of this invention.
A representative formula for an oral Weight Loss Product is as
follows, one tablet contains: Octopamine 150 mg Yohimbine 5 mg Bergenin
Decaffeinated Green Tea Extract (standardized for 60% EGCG content)
100 mg Plus additional excipients:
A sufficient quantity of each to make a suitable tablet: dicalcium
phosphate, magnesium stearate, silica, stearate, stearic acid, microcrystalline
cellulose and croscarmellose sodium.
The scientific rationale for this formulation is as follows:
In the body adrenergic receptors closely mediate the disposition
of fat stores. Stimulation of beta receptors sends a signal to release
fatty acids from fat cells, and stimulating alpha receptors sends
an opposite message, or to block the breakdown and release of fatty
acids (Am J Clin Nutr 1992;55:228s-36s). Stimulation of beta receptors
is a common focus for those looking for weight loss, as this subtype
is directly responsible for triggering lipolysis. Many weight loss
compositions focus on the use of ephedrine for example, which is
a non-selective agonist of beta receptors. Its activity is strong
as a lipolytic agent, being that it triggers lipolysis and thermogenesis
through beta-2 and beta-3 receptors. It also has strong central
nervous system effects through its activation of beta 1 and beta
2 receptors, and therefore can produce related side effects such
as sweating, nervousness, insomnia, increased heart rate or restlessness.
This invention therefore focuses on the use of a selective beta-3
agonist only. Studies with ephedrine have demonstrated that at least
40% of its thermogenic activity likely comes from beta-3 receptor
agonist activities (Int J Obes Relat Metab Disord. 1995;19(9):678-85),
so targeting this receptor specifically is an idea option to this
inventor. Octopamine is an extremely potent naturally occurring
beta-3 agonist, and studies have supported clearly that it is selective
for this receptor in mammals.
Yohimbine is a potent naturally occurring alpha-2 receptor antagonist,
and blocks the messaging system than negatively regulates lipolysis
in human fat cells. It also strongly stimulates the synaptic release
of norepinephrine, an endogenous beta-agonist extremely important
to lipolysis. As such it serves a dual purpose, both by blocking
alpha-2 activation and increasing the level of norepinephrine available
to fat cells. Studies have furthermore shown that in reasonable
doses it does not act as a strong central nervous system stimulant,
so when used in direct accordance to this invention it should not
be a strong instigator of stimulant-related side effects.
Decaffeinated green tea extract is included in this invention specifically
for its EGCG content. Studies have shown that tea catechins such
as EGCG inhibit the COMT enzyme in-vitro. The COMT enzyme is responsible
for the degredation of norepinephrine, and EGCG can therefore increase
the level of available norepinephrine available to fat cells by
slowing down its removal from the body. It was included to work
specifically with the other agents in this invention, so as to maximize
stimulation of the adrenergic system without external stimulants.
Bergenin is an active constituent found in the dried rhizomes of
the plant species thunbergii. Bergenin was shown in in-vitro studies
to increase the lipolytic activity of norepinephrine. Its exact
mode of action is unknown, but it is believed to increase norephinephrine
binding to phospholipids in fat cells. As such it is an excellent
synergistic addition to our composition. It itself exerts no direct
adrenergic activity, as was elucidated in the study, but strongly
bolsters the lipolytic action of norepinephrine, one of the bodies
important adrenergic, lipolytic and thermogenic hormones and a large
focus of this invention.
Without further elaboration, it is believed that one skilled in
the art can, using the preceding description, utilize the present
invention to its fullest extent. The specific formulas are included
as the preferred embodiment of the composition formula ranges, and
not to further qualify the description. Claim references to specific
components include the component itself, as well as all concentrated,
extracted, or purified forms of said ingredients.