Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2002-11-07
2003-10-28
Meller, Michael (Department: 1654)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Reexamination Certificate
active
06638541
ABSTRACT:
FIELD OF THE INVENTION
This invention relates to compositions comprising natural sources of tryptophan, particularly protein-bound tryptophan from plants, processes for making said compositions; physical formulations of said compositions, and use of said compositions for enhancing sexual desire and performance in mammals.
BACKGROUND OF THE INVENTION
Tryptophan is an essential amino acid found in numerous naturally occurring plant proteins and which has a number of interesting medicinal qualities including treatment of insomnia as well as an adjunct in the treatment of a number of psychiatric disorders. After absorption, tryptophan circulates in the blood as approximately 80% bound to plasma albumin with the remaining 20% circulating as free tryptophan, and under appropriate conditions, tryptophan is transported into the brain. Once across the blood brain barrier (BBB), tryptophan becomes available for metabolism into serotonin, a neurotransmitter implicated in mood and sleep regulation (Boman, 1988). Serotonin, in turn, is metabolized to melatonin; a sleep related hormone found in the pineal gland, a small cone-like structure in the epithalamus of the brain that regulates the 24-hour circadian rhythm in humans. Ingestion of a sufficient quantity of tryptophan per se consistently results in reduced sleep latency i.e. the time from “lights out” to sleep, and an improvement in overall quality of sleep through improved sleep architecture (Boman, 1988). Tryptophan metabolism to serotonin also serves well in conditions where depleted serotonin levels exists such as anxiety disorders, depression, obsessive-compulsive some pain disorders, aggression and eating disorders.
The hypnotic effects of tryptophan are well studied and follow a fairly flat dose-response curve with a plateau at approximately 1000 mg (for review see Schneider-Helmut and Spinweber, 1986). When given alone, as little as 250 mg of tryptophan is sufficient to produce improved sleep in people with mild insomnia, or in those reporting longer-than-average sleep latency (Hartmann and Spinweber, 1976; Hartmann 1982). Dosages of 1000 mg are associated with more consistent results (Schneider-Helmut and Spinweber, 1986) but higher dosages (2,000-12,000 mg) offer little extra benefit and, indeed, the highest dosages (12,000 mg) are associated with disrupted sleep architecture despite a reduction in sleep latency (Griffiths et al 1972).
The aforesaid medical conditions have been addressed in PCT published application No. WO 01/89319, published Nov. 29, 2001, in the names of Hudson, Susan P. and Hudson, Craig J. Aforesaid WO 01/89319 describes compositions comprising at least partially defatted meal from a plant source containing protein-bound tryptophan, preferably squash seeds, and, optionally, a carbohydrate source provided in an amount capable of facilitating transport of in vivo generated tryptophan across the blood brain barrier. Also described are dietary supplements, foods and beverages comprising the composition of the invention to induce sleep, address an anxiety disorder, depression, obsessive compulsive, aggression chronic pain and eating disorder or provide tryptophan supplementation to individuals in need thereof.
It is generally accepted that medications that increase brain serotonin levels will result in reduced libido as well as reduced overall sexual function (Bradford 2001). Medications associated with reduced libido, include antidepressants, especially those in the Selective Serotonin Reuptake Inhibitor (SSRI) class, as well as the serotonin precursor, tryptophan (Young 1986).
There are previous rare reports of increased sexual desire/function in persons that have taken substantial dosages of tryptophan, i.e. in excess of 6 gm per day.
Further, previous reports suggest that essentially all persons that have reported increased sexual desire or performance while taking tryptophan were also taking concomitant medications. There are no reports of tryptophan resulting in increased sexual desire or performance in instances where tryptophan was taken alone in relatively low doses as an orphan medication.
Yet further, there are no reports of the effect of tryptophan-bound proteins in enhancing sexual desire or performance.
SUMMARY OF THE INVENTION
We have surprisingly discovered that aforesaid as defined in WO 01/89319 at least partially defatted meal compositions provide enhances sexual desire and performance in a mammal.
We have surprisingly discovered that human subjects in a selected sleep study who ingested a high protein food composition rich in protein-bound tryptophan reported an increase in sexual desire and performance. These results were from studies that provided very much lower amounts (<250 mg) of possible tryptophan per se as calculated from the tryptophan-bound protein ingested, relative to the amounts described in the aforesaid prior art (>6 gm/day).
Thus, it is an object of the present invention to provide a plant source of tryptophan for use in enhancing sexual desire and performance in mammals.
Accordingly, in one aspect the invention provides a composition comprising a meal from a plant source containing protein-bound tryptophan, and a physiologically acceptable diluent or carrier therefore for enhancing sexual desire and performance in mammals.
Most preferably, the meal is at least partially defatted.
The naturally derived, tryptophan-rich compositions developed according to aforesaid WO 01/89319 by enriching the protein-bound tryptophan content of a tryptophan-rich protein source have been found to enhance sexual desire and performance in mammals. Compositions of use in the invention comprise a plant source naturally containing protein-bound tryptophan, preferably squash seeds, such as butternut squash seeds, peppercorn squash seeds and pumpkin seeds. Preferably, the plant source is at least partially defatted to concentrate the protein-bound tryptophan content. The composition further, preferably, comprises a carbohydrate source, such as glucose, in an amount sufficient to enhance uptake of tryptophan across the blood brain barrier and to circumvent the competition for BBB transport sites into the central nervous system (CNS). The composition can further optionally comprise physiologically acceptable vehicle(s), flavorings, colors and other nutrients, such as vitamins, preferably vitamin B3 and/or vitamin B6.
In a preferred embodiment, the composition comprises at least partially defatted squash seeds, particularly butternut squash, pumpkin and peppercorn squash seeds, glucose and vitamins B3 and B6.
The invention further pertains to dietary supplements, in the form of, e.g. a tablet, powder, suspension, liquid, capsule or gel; foods, e.g., dietary bar, cookie, baked good, snack food, candy, candy bars, beverages and like edible foods comprising the composition of the invention.
It is described in aforesaid WO 01/89319 that using second derivative spectroscopy, that certain plant sources and, specifically, plant seeds possess relatively high levels of protein-bound tryptophan and that these materials can be used to provide tryptophan in vivo. A process was developed to produce edible compositions having enhanced levels of protein-bound tryptophan as a natural protein source of tryptophan richer than the known natural source. Plants that use gramine typically contain high levels of tryptophan and can be used herein as the plant source. It is desirable, but not essential, that the starting plant material contain at least 200 mg/100 g or at least 0.2% tryptophan in its protein-bound form. Tryptophan concentration can be determined using known methods, including, for example, high pressure liquid chromatography (HPLC), second derivative spectroscopy or any other known methodology. Second derivative spectroscopy is the preferred method to quantitatively analyze tryptophan levels as it eliminates background absorbence.
According to an embodiment of the invention, protein-bound tryptophan levels present in the plant material source are enhanced using a series of steps to extract oil from the
Hudson Craig J.
Hudson Susan P.
Meller Michael
Morgan & Lewis & Bockius, LLP
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