Patent Grant
7199116
The invention relates to methods of modulating the Basal Metabolic rate of a mammal.
Mammals, particularly humans, are believed to have a Basal Metabolic rate which defines the rate at which they convert calories to energy. It is widely believed that the Basal Metabolic rate is influenced by dieting, with the body reacting to a reduced caloric intake by slowing down the Basal Metabolic rate of the dieter. This diet induced reduction in the Basal Metabolic rate is one of the reasons thought to be responsible for the ineffectiveness of achieving weight loss by dieting.
Accordingly, a need exists for a method of safely modulating the Basal Metabolic rate of a dieting mammal.
The basal metabolic rate, or resting energy expenditure, of a dieting mammal may be modulated by administering a metabolic modulating agent to the dieting mammal. The metabolic modulating agent is 7-oxo DHEA or a pro-drug thereof incapable of in vivo conversion to testosterone.
Definitions
As utilized herein, including the claims, the term “dieting” means eating and drinking sparingly with the intent to lose weight.
As utilized herein, including the claims, the term “7-oxo DHEA” means Δ5-androstene-3-ol-7, 3-ol-7,17-dione.
As utilized herein, including the claims, the term “3-acetyl 7-oxo DHEA” means Δ5-androstene-3-acetoxy-7,17-dione.
Description
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. I have surprisingly discovered that 7-oxo DHEA is effective for modulating the metabolism of a dieting mammal so as to prevent or at least moderate any diet-induced decrease in metabolism. Such moderation of the metabolism should be effective for accelerating the weight loss achievable by dieting.
The Metabolic Modulating Agent
The metabolic modulating agent effective for modulating the Basal Metabolic rate of a dieting mammal is the steroid Δ5-androstene-3β-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 Δ5-androstene-3β-ol-7,17 dione from DHEA, with one such procedure described in U.S. Pat. No. 5,296,481.
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 Δ5-androstene-3β-acetyl-7,17 dione (3-acetyl 7-oxo DHEA). The 3β-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 Δ5-androstene-3β, 17β-diol-7-one, Δ5-androstene-3β, 7α-diol-17-one, Δ5-androstene-3β, 7β-diol-17-one and the corresponding acetyl esters of these steroids.
Administration
Administration Route
The metabolic modulating 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.
Mucosal administration of the metabolic modulating agent includes such routes as buccal, endotracheal, nasal, pharyngeal, rectal, sublingual, vaginal, etc. For administration through the buccal/sublingual/pharyngeal/endotracheal mucosal, the metabolic modulating 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 metabolic modulating agent may be formulated as a cream, douche, enema or suppository.
Oral consumption of the metabolic modulating agent may be effected by incorporating the metabolic modulating agent into a food or drink, or formulating the metabolic modulating agent into a chewable or swallowable tablet or capsule.
Ocular administration may be effected by incorporating the metabolic modulating agent into a solution or suspension adapted for ocular application such as drops or sprays.
Subcutaneous administration involves incorporating the metabolic modulating agent into a pharmaceutically acceptable and injectable carrier.
For transdermal administration, the metabolic modulating agent may be conveniently incorporated into a lipophilic carrier and formulated as a topical creme or adhesive patch.
Dose Rate
The range of dosages and dose rates effective for achieving the desired modulation of metabolism may be determined in accordance with standard industry practices.
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