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Weight Loss Patent Abstract
Accelerating weight loss by admtinistering to a dieting mammal the
weight loss accelerating agent 7-oxo DHEA or a pro-drug thereof
incapable of in vivo conversion to testosterone.
Weight Loss Patent Claims
1. A method of achieving accelerated weight loss comprising administration
of a weight loss accelerating agent to a dieting mammal wherein
the weight loss accelerating agent is 7-oxo DHEA or a pro-drug thereof
incapable of in vivo conversion to testosterone.
2. The method of claim 1 wherein the weight loss accelerating agent
is administered orally.
3. The method of claim 2 wherein the weight loss accelerating agent
is administered at least once daily.
4. The method of claim 1 wherein the dieting mammal is a human.
5. The method of claim 2 wherein the dieting mammal is a human.
6. The method of claim 3 wherein the dieting mammal is a human.
7. The method of claim 4 wherein the weight loss accelerating agent
is 3-acetyl 7-oxo DHEA or 3-ester thereof.
8. The method of claim 5 wherein the weight loss accelerating agent
is 3-acetyl 7-oxo DHEA or 3-ester thereof.
9. The method of claim 6 wherein the weight loss accelerating agent
is 3-acetyl 7-oxo DHEA or 3-ester thereof.
Weight Loss Patent Description
[0001] This application claims the benefit of U.S. Provisional Application
No. 60/439,753, filed Jan. 13, 2003.
FIELD OF INVENTION
[0002] The invention relates to methods of achieving weight loss.
BACKGROUND
[0003] The steroid .DELTA.5-androstene-3-ol-7,17-dione (7-oxo DHEA)
is believed to stimulate various beneficial biological responses
including (i) inducing the synthesis of various thermogenic enzymes
which are effective for regulating metabolism and thereby promoting
weight control without affecting caloric intake, and (ii) inducing
the synthesis of the major thyroid hormone triiodothyronine (T.sub.3)
which is effective for increasing the basal metabolic rate and thereby
promoting weight control without affecting caloric intake.
[0004] The ability of 7-oxo DHEA to promote weight control is widely
believed to be mediated through enhanced thermogenesis (conversion
of foodstuffs to heat energy rather than chemical energy such as
ATP and/or triacylglycerides). The thermogenic effect mediated by
7-oxo DHEA is believed to result from the ability of 7-oxo DHEA
to stimulate the synthesis of thermogenic enzymes including mitochondrial
glycerol 3-phosphate dehydrogenase (G3P-DH), cytosolic malic enzyme
(ME) and fatty acyl CoA oxidase. Such enzymes tend to reduce the
efficiency of energy metabolism within the body.
[0005] While highly effective for safely promoting weight control,
a continuing need exists to accelerate the weight loss effect achieved
with 7-oxo DHEA.
SUMMARY OF THE INVENTION
[0006] Weight loss can be accelerated during dieting by the administration
of a weight loss accelerating agent while dieting. The weight loss
accelerating agent is 7-oxo DHEA or a pro-drug thereof incapable
of in vivo conversion to testosterone.
DETAILED DESCRIPTION OF A PREFERRED EMBODIMENT
Definitions
[0007] As utilized herein, including the claims, the term "dieting"
means eating and drinking sparingly with the intent to lose weight.
[0008] As utilized herein, including the claims, the term "7-oxo
DHEA" means .DELTA.5-androstene-3-ol-7,17-dione.
[0009] As utilized herein, including the claims, the term "3-acetyl
7-oxo DHEA" means .DELTA.5-androstene-3-acetoxy-7,17-dione.
Description
[0010] I have surprisingly discovered that 7-oxo DHEA is effective
for accelerating the weight loss achievable by dieting. Without
intending to be limited to any particular theory, I believe that
the administration of 7-oxo DHEA to a dieting mammal is effective
for accelerating weight loss because 7-oxo DHEA modulates the metabolism
of the dieting mammal. It is widely believed that dieting is an
ineffective means for achieving weight loss because the body reacts
to the reduced caloric intake by slowing down the metabolism of
the dieter. By modulating the metabolism of the dieting mammal,
7-oxo DHEA would be effective for preventing or at least moderating
any diet-induced decrease in the metabolism and thereby accelerate
weight loss achievable by dieting.
The Weight Loss Accelerating Agent
[0011] The weight loss accelerating agent effective for accelerating
weight loss when combined with dieting is the steroid .DELTA.5-androstene-3.beta.-ol-7,17
dione (7-oxo DHEA). 7-oxo DHEA is a derivative of dehydroepiandrosterone
(DHEA). 7-oxo DHEA does not appreciably stimulate, increase or otherwise
enhance the production of sex hormones. The steroid is commercially
available from a number of sources including Steraloids, Inc. of
Wilton, N.H. A number of procedures are available for synthesizing
.DELTA.5-androstene-3.beta.-ol-7,17 dione from DHEA, with one such
procedure described in U.S. Pat. No. 5,296,481.
[0012] Pro-drugs of 7-oxo DHEA (i.e., compounds readily metabolized
in vivo to the active 7-oxo DHEA) may also be usefully employed.
One example of a pro-drug is the commercially available .DELTA.5-androstene-3.beta.-acetyl-7,17
dione (3-acetyl 7-oxo DHEA). The 3.beta.-acetyl group is hydrolyzed
in vivo by esterases located in the blood and various tissue to
produce the active 7-oxo DHEA, and is believed to be less susceptible
to oxidation during the manufacturing process relative to 7-oxo
DHEA. Other suitable pro-drugs include .DELTA.5-androstene-3.beta.,17.beta.-diol-7-one,
.DELTA.5-androstene-3.beta.,7.alpha.-diol-17-one, .DELTA.5-androstene-3.beta.,7.beta.-diol-17-one
and the corresponding acetyl esters of these steroids.
Administration
Administration Route
[0013] The weight loss accelerating agent can be administered by
virtually any of the commonly accepted practices for the administration
of pharmaceutical preparations including specifically, but not exclusively,
mucosal administration, oral consumption, ocular administration,
subcutaneous injection, transdermal administration, etc. Oral administration
is generally preferred.
[0014] Mucosal administration of the weight loss accelerating agent
includes such routes as buccal, endotracheal, nasal, pharyngeal,
rectal, sublingual, vaginal, etc. For administration through the
buccal/sublingual/pharyngeal/endotracheal mucosal, the weight loss
accelerating agent may be formulated as an emulsion, gum, lozenge,
spray, tablet or an inclusion complex such as cyclodextrin inclusion
complexes. Nasal administration is conveniently conducted through
the use of a sniffing powder or nasal spray. For rectal and vaginal
administration the weight loss accelerating agent may be formulated
as a cream, douche, enema or suppository.
[0015] Oral consumption of the weight loss accelerating agent may
be effected by incorporating the weight loss accelerating agent
into a food or drink, or formulating the weight loss accelerating
agent into a chewable or swallowable tablet or capsule.
[0016] Ocular administration may be effected by incorporating the
weight loss accelerating agent into a solution or suspension adapted
for ocular application such as drops or sprays.
[0017] Subcutaneous administration involves incorporating the weight
loss accelerating agent into a pharmaceutically acceptable and injectable
carrier.
[0018] For transdermal administration, the weight loss accelerating
agent may be conveniently incorporated into a lipophilic carrier
and formulated as a topical creme or adhesive patch.
Dose Rate
[0019] The range of dosages and dose rates effective for achieving
the desired accelerative weight loss effect may be determined in
accordance with standard industry practices.
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