XANTHINE COMPOUND FORMULA FOR HAIR LOSS

     A patent was recently issued to a U.S. biotech firm for the concomitant oral administration of Xanthine based stimulants, neurotransmitter precursors, nootropic herbs, cognition enhancing neurosteroids, and cerebral vasodilators that would result in simultaneous cognitive enhancement, increased energy, weight loss, and prevention of hair loss, specifically, androgenetic alopecia.
     This formulation has several compounds already recommended in our hairloss protocol, in addition to some others. The ingredients listed in the patented compound are:

Ingredients
mg./oral unit
Ginkgo Biloba Extract 5.0
Theophylline 25.0
Caffeine 27.5
Green Tea Extract 84.0
L-Pyroglutamate 75.0
Xathinol Nicotinute 38.0
Acetyl-L-Carnitine 750 mg.
Choline 60 mg.
DMAE 60 mg.
Magnesium Glycinate 25 mg.
Potasium Aspartate 50 mg.
L-Phenylalanine 50 mg.


     The recommended dose for hairloss prevention is 2 "units" a day. Following are excerpts from the patent itself:

United States Patent 6,436,946
Mann August 20,2002


     Xanthine-containing compositions for oral administration and uses related thereto.


Description

TECHNICAL FIELD

     The present invention relates generally to pharmaceutical compositions and methods for their use, and more specifically to xanthine-containing compositions that enhance cerebral cortical activity, enhance short-term memory, suppress appetite and/or reduce hair loss.
     Cognitive cofactors include biosynthetic precursors to neurotransmitters and neurosteroids, cerebral vasodilators, mineral cofactors, nootropic herbs and essential amino acids. Exemplary cognitive cofactors include ginkgo biloba; glutamic acid and salts thereof, niacin and derivatives containing the niacin nucleus; acetyl-L-carnitine; dimethylaminoethanol (DMAE); L-phenylalanine; choline and salts thereof; glycine and salts thereof, aspartic acid and salts thereof, squalane; squalene; pregnenolone; dehydroepiandrosterone (DHEA); and dehydroepiandrosterone-3-sulphate.
     Another aspect of the invention provides a method for enhancing cerebral cortical activity. According to this method, an effective amount of a composition as described above is administered to a subject (such as a warm-blooded animal, including a human subject) in need of enhanced cerebral cortical activity.
     In another aspect of this invention, a method is disclosed for enhancing short term memory. According to this method, an effective amount of a composition as described above is administered to a subject in need of enhanced short term memory.
     A further aspect of this invention is a method for enhancing weight loss. According to this method, an effective amount of a composition as described above is administered to a subject in need of weight loss.
     In still a further aspect of this invention, a method is disclosed for retarding hair loss in a subject in need thereof. According to this method, an effective amount of a composition as described above is administered to a subject experiencing or prone to hair loss.
     These and other aspects of this invention will become evident upon reference to the following detailed description.
     The invention provides, in one embodiment, a therapeutic composition for oral administration which includes caffeine, a second xanthine other than caffeine, and a cognitive cofactor as defined above. Thus, the invention provides compositions for oral administration which include caffeine, a xanthine compound other than caffeine and ginkgo biloba; caffeine, a xanthine compound other than caffeine, and glutamic acid or ester or salt thereof, caffeine, a xanthine compound other than caffeine, and niacin or derivative thereof, caffeine, a xanthine compound other than caffeine and acetyl-L-carnitine; caffeine, a xanthine compound other than caffeine, and dimethylaminoethanol; caffeine, a xanthine compound other than caffeine, and an amino acid or ester or salt thereof; caffeine, a xanthine compound other than caffeine, and L-phenylalanine; caffeine, a xanthine compound other than caffeine, and choline or a salt thereof, caffeine, a xanthine compound other than caffeine, and glycine or ester or salt thereof, caffeine, a xanthine compound other than caffeine, and aspartic acid or ester or salt thereof, caffeine, a xanthine compound other than caffeine, and squalane; caffeine, a xanthine compound other than caffeine, and squalene; caffeine, a xanthine compound other than caffeine, and pregnenolone; caffeine, a xanthine compound other than caffeine, and dehydroepiandrosterone; caffeine, a xanthine compound other than caffeine, and dehydroepiandrosterone-3-sulfate. In one embodiment, the xanthine compound other than caffeine is theophylline. In another embodiment, the niacin or derivative thereof is xanthinol nicotinate. In still another embodiment, the glutamic acid or ester or salt thereof is pyroglutamate. In yet a further embodiment of the invention, the afore-listed compositions contain only the mentioned compounds as active ingredients.
     The inventive composition may be administered to achieve a variety of beneficial effects. Thus, the composition may serve as a stimulant, to increase cerebral cortical activity, to elevate mood, to enhance short-term memory, to provide increases in musculature and athletic performance, decreases in appetite, and a decrease in hair loss. These beneficial effects are discussed further below.
     It has been surprisingly found that the inventive compositions provides a sustained and noticeable stimulant effect far beyond that typically observed upon ingestion of an equivalent amount of caffeine or second xanthine compound alone. The invention is therefore also directed to a method of employing the composition of the invention to enhance cerebral cortical activity and thereby provide a stimulatory effect. Thus, the invention provides a method for enhancing cerebral cortical activity in a subject in need thereof A "subject in need thereof" may be a warm-blooded animal who has been diagnosed to have attention deficiency disease. According to the method, an effective amount of a composition as described above is administered to a subject in need of enhanced cerebral cortical activity. Furthermore, the inventive composition affords this stimulant effect with an amelioration of the diffuse chronic depolarization and subsequent cortical depression commonly associated with stimulants alone. Accordingly, methods for enhancing cerebral cortical activity while ameliorating the diffuse chronic depolarization and subsequent cortical depression commonly associated with stimulants alone is provided by the present invention.
     It has also been surprisingly found that the inventive composition may afford substantial enhancements in short term memory as compared with caffeine alone. The invention is therefore also directed to a method of employing the composition of the invention to aid short term memory recall. Thus, the invention provides a method for enhancing the short term memory a subject in need thereof, comprising oral administration to the subject of an effective amount of a composition of the invention as described above.
     In a preferred embodiment, the inventive composition contains a biosynthetic precursor to a neurosteroid. When the composition contains a biosynthetic precursor to a neurosteroid, it is particularly preferred to administer such a composition to a subject in need of increases in muscular development and athletic performance, decreases in appetite and/or decreases in hair loss. Thus, subjects who are predisposed to alopecia may be in need of oral administration of the composition of the present invention, in order to reduce hair loss.
     It has also been surprisingly found that the inventive composition causes a significant reduction in the appetite of an overweight person who consumes the composition. Overweight persons who consume the inventive composition experience weight loss because their caloric consumption decreases as their interest in food is reduced. The inventive composition is therefore useful for weight reduction and longterm weight management. Thus, the invention provides a method for achieving weight reduction comprising administering to a subject in need thereof an effective amount of the composition of the invention as described above.
     The stimulant aspect of the present invention may be enhanced by increasing the amount of phenylalanine present in the inventive composition. Concurrently, the anorectic effect of such a composition (having a high phenylalanine content) may also be substantially augmented. In conjunction with a xanthine compound according to the present invention, a composition with an elevated phenylalanine content provides a notable increase in weight loss, and when combined with the components of the composition of Formulation IV (below), the amount of weight lost may be increased. The composition disclosed in Formulation III is exemplary of compositions of the invention having an elevated phenylalanine content. The compositions of Formulations III and IV may be administered orally in a variety of different forms, including, but not limited to, capsules, tablets, powder, and syrups
     It has also been surprisingly found that the inventive composition causes a dramatic reduction in hair loss in subjects predisposed to androgenetic alopecia. The invention is therefore also directed to a method of employing the composition of the invention to retard hair loss. Thus, the invention provides a method for retarding hair loss from a subject experiencing hair loss and/or predisposed to androgenetic alopecia, comprising oral administration to the subject of an effective amount of a composition of the invention as described above.

HAIR LOSS

     The following example illustrates the administration of a representative composition of the present invention to achieve a reduction in hair loss.
     Five subjects with persistent chronic hair loss were given Formulation I from Example 1 on a daily basis over a three week time span. They were asked to count hairs lost each day, and this data was averaged each week to determine the average hair loss per day, per week. The results of this experiment were as follows:

Hairs lost/day
Subject 1
Week 1
226
Week 3
130
Subject 2
Week 1
168
Week 3
76
Subject 3
Week 1
345
Week 3
82
Subject 4
Week 1
179
Week 3
58
Subject 5
Week 1
246
Week 3
66



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