NZ530554A - Neuronutrients - Google Patents

Abstract

A neuronutrient health supplement composition comprising pyridoxine alpha ketoglutarate, acetyl L-carnitine, an extract of ginkgo biloba and at least one plasmogen phosphalide, at least one inositol.

Description

New Zealand Paient Spedficaiion for Paient Number 530554 Patents Form # 5 530 5 5 4 INTELLECTUAL PROPERTY OFFICE OF N.Z 1 2 JAN 20(ft RECEIVED NEW ZEALAND Patents Act 1953 COMPLETE SPECIFICATION TITLE : Neuronutrients I, AL-SHAKARCHI, A. Munem Mohammad Daoud Address: 4 Landsberg Way, Windsor Park, Mairangi Bay, Auckland, New Zealand Nationality: A New Zealand citizen do hereby declare the invention for which I pray that a patent may be granted to me and the method by which it is to be performed, to be particularly described in and by the following statement: - 1 PF05.JWP FEE CODE 1050 FIELD OF THE INVENTION The present invention relates to a health supplement, in particular to a health supplement to aid brain function and memory.

BACKGROUND In order to function optimally, the brain needs the proper nutrients, which may be compromised in the modern world. The pressures of daily life make it difficult for modern Americans to devote the necessary time to prepare food properly. As a consequence of this and a constant barrage of advertising, a high proportion of many people's diets consist of fast foods and packaged foods, low in many essential nutrients and high in sodium and sugar. 10 Excess sodium can create a relative imbalance in the sodium/potassium ratio, and potassium is an important nutrient for nerve conduction. Excess simple sugar intake can, paradoxically, cause low blood sugar, thus depriving the brain of the fuel it needs.

Ultimately, all of the health and nutrition issues indeed, all the issues of any kind that we face begin and end with the brain. The body attests to the brain's importance by devoting a 15 huge share of its vital nutritional resources to the care and feeding of this single, and singular, organ. Knowing what the nutritional issues associated with optimal brain nutrition are supporting the brain's production of energy, providing the raw materials for the production and utilization of neurotransmitters, protecting the brain's delicate structures, and supporting the structure of the brain's cell membranes can help you make informed choices 20 about your nutritional needs.

It is an object of the present invention to provide a health supplement to aid brain and memory function. One of the keys to supporting memory power is to give the brain the foods it needs not only to run properly, but also to operate better. One name for these brain foods is neuronutrients—specific vitamins, minerals, fatty acids, amino acids, and trace elements 25 essential to brain function. It is an object of the present invention top provide such neuronutrients and it is yet a further object of the invention to provide such neuronutrients in tablet form. 130110NZ Prov.doc/CA/ca STATEMENTS OF THE INVENTION A composition suitable for administering to warm blooded animals as a health supplement including pyridoxine alpha ketoglutarate and acetyl L-carnitine wherein the composition further includes at least one plasmalogen phosphalide, one or more inositols, and extract of 5 ginkgo biloba.

Preferably, the or each plasmalogen phosphalide can be selected from the group comprising phosphatidyl choline and phosphatidyl ethanolamine.

Preferably the or each inositol can be selected from the group comprising phosphatidyl inositol and inositol.

Preferably the composition further comprises vitamins.

More preferably still, the vitamins can be selected from the group comprising A, C, E and a B complex.

More preferably the vitamin B complex can be selected from the group comprising Bl, B2, B3, B5, B6 and B12.

Preferably, the composition further comprises a metal derivative.

Preferably, the metal derivative can be selected from the group comprising mono, di, tri and tetra valent metal derivatives.

More preferably still, the divalent metal derivative can be selected from the group of metals comprising calcium, zinc, copper, manganese, chromium and magnesium.

More preferably still, the divalent metal derivative can be selected from the group comprising calcium ascorbate, carbonate, nicotinate, sebacate, chloride, malate, taurinate, oxide,citrate or succinate.

Preferably, the trivalent metal derivative can be selected from the group of metals comprising boron and chromium.

More preferably still, the trivalent metal derivatives can be selected from the group comprising chloride, nicotinate and citrate. 130110NZ Prov.doc/CA/ca INTELLECTUAL PROPERTY OPPICP OF N.Z 2 8 JAN 2004 RECEIVED Preferably, the monovalent metal derivative can be selected from the group of metals comprising potassium, sodium and lithium.

More preferably, the monovalent metal derivatives can be selected from the group comprising selenite and molybdate.

Preferably, the composition further comprises an amino acid.

More preferably still, the amino acid can be selected from the group comprising L-glutamine, Taurine, N-acetyl L-Tyrosine, and L-Tyrosine.

Preferably, the composition further comprises at least one of the following, L-Pyroglutamic acid, dimethylaminoethanolbitartrate, DL-phenylalanine, choline bitartrate, liopic acid, 10 docosahexaenoic acid, folic acid, biotin, huperzine and/or phosphatidyl serine.

Preferably, the composition further comprises one or more herbal extracts.

More preferably still, the herbal extracts can be selected from the group comprising Siberian ginseng, gotu kola, ginger root, schizandra, cayenne, grape seeds extract, bacopa monniera and rosemary.

Preferably, the composition further comprises an excipient.

Preferably, the extract of Ginkgo biloba is in the range of 1.0-5.0 x 10-3 %w/v.

Preferably, the pyridoxine alpha ketoglutarate is in the range of 10-30 x 10-3 %w/v. Preferably, the acetyl L-carnitine is in the range of 40-150 x 10-3 %w/v.

Preferably, the plasmalogen phosphalide is in the range of 50-200 x 10-3 %w/v. 20 Preferably, the phosphatidyl choline is in the range of 40-150 x 10-3 %w/v.

Preferably, the phosphatidyl ethanolamine is in the range of 5-40 x 10-3 %w/v.

Preferably, the inositol is in the range of 5-50 x 10-3 %w/v.

Preferably, the phosphatidyl inositol is in the range of 5-50 x 10-3 %w/v. 130110NZ Prov.doc/CA/ca INTELLECTUAL PROPERTY OFFICE OF N.Z 2 8 JAN 2004 RECEIVED Preferably, the vitamin B complex is in the range of 30-150 x 10-3 %w/v.

Preferably, the vitamin A is in the range of 2-20 x 10-4 %w/v.

Preferably, the vitamin C is in the range of 5-30 x 10-3 %w/v.

Preferably, the folic acid is in the range of 100-600 x 10-3 %w/v.

Preferably, the botin is in the range of 20-80 x 10-3 %w/v.

Preferably, the calcium derivative is in the range of 20-80 x 10-3 %w/v Preferably, the magnesium derivative is in the range of 20-80 x 10-3 %w/v. Preferably, the zinc derivative is in the range of 3-15 x 10-3 %w/v.

Preferably, the manganese derivative is in the range of 2-8 x 10-3 %w/v. 10 Preferably, the selenium is in the range of 20-80 x 10-3 %w/v.

Preferably, the boron derivative is in the range of 100-400 x 10-3 %w/v.

Preferably, the copper derivative is in the range of 1-8 x 10-4 %w/v Preferably, the molybdenum derivative is in the range of 7-40 x 10-3 %w/v. Preferably, the chromium derivative is in the range of 20-80 x 10-3 %w/v. 15 Preferably, the L-Pyroglutamic acid is in the range of 20-120 x 10-3 %w/v. Preferably, the L-glutamine is in the range of 20-160 x 10-3 %w/v.

Preferably, the acetyl L-carnitine is in the range of 20-160 x 10-3 %w/v.

Preferably, the L-cartinine is in the range of 40-160 x 10-3 %w/v.

Preferably, the dimethylaminoethanolbitartrate is in the range of 10-60 x 10-3 %w/v. 20 Preferably, the taurine is in the range of 5-50 x 10-3 %w/v.

Preferably, the DL phenylalanine is in the range of 5-50 x 10-3 %w/v. 130110NZ Prov.doc/CA/ca Preferably, the choline is in the range of 20-50 x 10-3 %w/v.

Preferably, the N-acetyl L-tyrosine is in the range of 20-120 x 10-3 %w/v.

Preferably, the L tyrosine is in the range of 20-120 x 10-3 %w/v.

Preferably, the gama amino butyric acid is in the range of 5-50 x 10-3 %w/v.

Preferably, the lipoic acid is in the range of 3-15 x 10-3 %w/v.

Preferably, the phsphatidyl serine is in the range of 7-40 x 10-3 %w/v.

Preferably, the docosahexaenoic acid is in the range of 8-30 x 10-3 %w/v.

Preferably, the huperzine is in the range of 7-40 x 10-3 %w/v.

Preferably, the Siberian Ginseng is in the range of 7-40 x 10-3 %w/v.

Preferably, the Gotu Kola is in the range of 7-40 x 10-3 %w/v.

Preferably, the Ginger Root is in the range of 7-40 x 10-3 %w/v.

Preferably, the Schizandra is in the range of 7-40 x 10-3 %w/v.

Preferably, the cayenne is in the range of 7-40 x 10-3 %w/v.

Preferably, the grape seed extract is in the range of 7-40 x 10-3 %w/v.

Preferably, the bacopa monniera or rosemary is in the range of 15-60 x 10-3 %w/v. The present embodiment is shown by way of example only.

DESCRIPTION OF THE PREFEERED EMBODIENTS.

ACETYL L-CARNITINE Acetyl 1-carnitine (ALC) is an important neuroceutical with a variety of beneficial effects on 20 the brain and body. ALC, an acetylated amino acid, has a high degree of structural similarity to the neurotransmitter acetylcholine (ACH) and facilitates the transport of metabolic energy. Animal studies have shown that ALC promotes the synthesis and release of ACH, helps to 130110NZ Prov.doc/CA/ca prevent the accumulation of damaging lipofuscin in brain cells , enhances the stability of cell membranes, and helps protect the brain from free-radical damage by increasing amounts of the potent antioxidant, glutathione. Another major function of ALC is to transport long-chain fatty acids into mitochondria, providing an important energy source for tissues that burn fat 5 for energy, such as muscle.

Acetyl 1-carnitine facilitates the transfer of metabolic energy by acting as carrier for acetyl groups across cell membranes. Acetyl groups are energy-carrying organic molecules that can be transferred to the coenzyme acetyl CoA, which forms the starting point of the central energy-generation process called the Krebs cycle. Aside from its central role in cellular 10 energy production, acetyl CoA, along with choline, is a precursor for the neurotransmitter acetylcholine. ACH is one of the most abundant neurotransmitters in the body, and is necessary for memory and muscle control. ALC promotes the production of acetylcholine both by transferring acetyl groups to acetyl CoA and by inducing the activity of choline acetyltransferase, an enzyme that manufactures acetylcholine by attaching an acetyl group 15 from acetyl CoA onto the choline molecule. ALC has also been shown in animal studies to stimulate a class of neurotransmitter receptors called muscarinic acetylcholine receptors, thus further enhancing the activity of ACH in the brain.

Damaged brain neurons are characterized by a decreased ability to produce energy. Like coenzyme Q-10, acetyl-L-carnitine enhances neuronal energy production by functioning as a 20 shuttle - transporting fuel sources into mitochondria, the energy producing machinery of the neuron. It also assists in removing toxic by products of brain metabolism and acts as a potent antioxidant. Acetyl-L-carnitine has been demonstrated to protect laboratory animals from developing full-blown Parkinsonism when exposed to specific chemicals know to induce the disease.

N-ACETYL L-TYROSINE AT-Acetyl 1-Tyrosine, an acetylated form of 1-tyrosine, is converted in the body to key biologic compounds, including the neurotransmitters dopamine, norepinephrine and epinephrine. These neurotransmitters, collectively known as the catecholamines, are critically important for a sense of "readiness" to meet life challenges. Catecholamines are 30 produced in the adrenal glands, and are primary players in mediating our bodies' response to stress. 130I10NZ Prov.doc/CA/ca There is some evidence that 1-tyrosine or its catecholamine metabolites are necessary for the production of coenzyme Q10, a cofactor in the electron-transport chain, a process that occurs in every cell of the body and results in the synthesis of the energy-generating molecule ATP. It is also involved in the production of thyroid hormones, important metabolism regulators, 5 and melanin, the skin pigment that protects us from ultraviolet radiation. Source Naturals N-Acetyl 1-tyrosine combines this remarkable nutrient with the B vitamins pyridoxine (B6) and folic acid to assist its conversion to its various metabolic products PHOSPHATIDYL CHOLINE Phosphatidyl choline is an important phospholipid which contains the B vitamin-like 10 substance choline. It is a principal component of cell membranes, found in virtually every cell in the body. In addition, it is an important precursor to the neurotransmitter acetylcholine, which is associated with memory and muscle control.

Soy lecithin also contains the essential cell membrane phospholipids phosphatidyl inositol, phosphatidyl ethanolamine and related phosphorus-containing lipids.

PHOSPHATIDYL SERINE COMPLEX Phosphatidyl serine (PS) is a key cell membrane phospholipid, which is essential for normal neuron structure and function. Phospholipids are fat-like substances containing a hydrophilic (water-loving) phosphate-based head group (which forms the outward surface of the cell membrane) and two hydrophobic (water-hating) fatty acid tails (which form the inner surface 20 of the cell membrane). PS readily crosses the blood-brain barrier, promoting entry into the brain.

Phospholipids are the primary structural component of all cell membranes, and cells depend on the maintenance of a certain combination of them for proper function. This is a particularly important issue with regards to neuron function, as nerve impulses are 25 transmitted across the neuronal membrane.

Phosphatidyl serine, because of its particular chemical structure, associates preferentially with a class of membrane-bound proteins called ATPases. ATPases regulate, among other things, the balance of sodium and potassium in intra- and extracellular fluids, a balance that is necessary for the integrity of our cells and also for the electrochemical impulses that make 130110NZ Prov.doc/CA/ca up our thoughts and feelings. Without phosphatidyl serine, these vitally important membrane-embedded proteins could not function. Another factor in the importance of PS is that it can be converted to the acetylcholine precursor phosphatidyl choline, thus possibly supporting optimal acetylcholine levels in the brain.

The composition of cell membrane phospholipids changes as we age; this change is a factor in age-related cognitive decline. Extensive studies have shown that supplementing the diet with PS helps to maintain the proper balance of phospholipids in nerve cell membranes as we age.

Research carried out at Stanford University evaluating 149 patients suffering from dementia 10 demonstrated that orally administered phosphatidylserine produced a marked improvement on performance tests related to memory and learning in demented patients. Like acetyl-L-carnitine and coenzyme Q-10, phosphatidylserine plays an important role in maintaining the ability of brain neurons to produce energy. Phosphatidylserine is a fundamental component of the fatty membranes surrounding the mitochondria where energy production occurs. In 15 addition, it also serves as a critical component of the membrane surrounding neurons and thus plays a fundamental role in the process by which brain cells both receive and transmit chemical messages.

Vitamin B1 and Magnesium Two nutrients, which are intimately involved in many aspects of nerve health and function. 20 The major coenzyme form of vitamin Bl, thiamine pyrophosphate (TPP), is necessary for the conversion of pyruvate into acetyl CoA, a key step in the Krebs cycle. This step is pivotal for the production of energy, and is also essential for the production of acetylcholine, a key neurotransmitter associated with memory and muscle control. Thiamin is also maintains the myelin sheath, the protective coating that shields the axons of nerve cells and assists in the 25 transmission of the nerve impulses along their length. Magnesium plays an important role in nerve cell function and neuromuscular transmission and activity. Magnesium also promotes muscle relaxation. Excessive alcohol intake as well as black tea and coffee intake increase the requirements for thiamin and magnesium, this important mineral is critical in a program designed to preserve and enhance brain function for several important reasons. First, 30 adequate amounts of magnesium are necessary for the electrical depolarization of the neuronal membrane. This is the process by which chemical messages are transmitted from 130110NZ Prov.doc/CA/ca one neuron to the next. Next, magnesium enhances the function of various brain antioxidants thus helping to protect the brain against free radical damage. Finally, magnesium helps to prevent the production of specific chemicals within the body, which increase inflammation. In Alzheimer's disease, Parkinson's disease, and multiple sclerosis, inflammation represents 5 a fundamental mechanism enhancing the formation of brain damaging free radicals.

Dimethylaminoethanol Bitartrate Dimethylaminoethanol, or DMAE, is an important neuroceutical, which may have beneficial effects on cognitive function and nerve cell membrane integrity. DMAE is a natural substance found in several foods, including sardines and anchovies.

DMAE is a precursor for the B vitamin-like substance choline. The neurotransmitter acetylcholine is formed from choline and acetyl CoA, a coenzyme form of vitamin B5. Acetylcholine is an important neurotransmitter, necessary for memory and muscle control. DMAE has been shown to increase levels of free choline in the brain, which is necessary for optimal production of acetylcholine. It crosses the blood-brain barrier more easily than 15 choline, directly accessing the tissues of the brain where it is needed most.

DMAE also acts as an antioxidant, as it neutralizes a free radical known as the hydroxyl radical. In this way, DMAE helps stabilize cell membranes and promotes healthy nerve cell conduction, important goals in maintaining healthy brain function as we age.

Gamma Amino Butyric Acid Gamma amino butyric acid, or GABA, is an amino acid. GABA is the primary inhibitory neurotransmitter in the brain; this means that rather than stimulating neurons to fire, GABA inhibits neuronal activity. Inhibitory neurotransmitters are important because they prevent the brain from being overloaded by stimuli. Thus GABA is associated with mental states of calm and serenity. GABA also promotes muscle relaxation.

Ginkgo biloba Extract 24% Lipid peroxidation is a critical issue for brain health for several reasons. First, aside from water, the brain is composed primarily of lipids. The health of cell membranes in the brain is critical because the transmission of nerve impulses depends on electrochemical gradients, 130110NZ Prov.doc/CA/ca which can only function properly if these membranes are intact. This includes the myelin sheath, the fatty insulation covering the axons of most neurons, the integrity of which is essential for proper nerve impulse conductivity. Also, free radical damage to cell membranes directly contributes to the buildup of lipofuscin or "age pigment" which some researchers 5 believe may contribute to age-related cognitive decline.

Ginkgo has been shown in numerous studies to dilate blood vessels and enhance their strength and flexibility. This is particularly important for the brain: much of the blood supply upon which the brain depends is carried by tiny, fragile capillaries, with a diameter so small that red blood cells can only pass through one at a time, single file. In addition to 10 strengthening and dilating blood vessels, ginkgo inhibits platelet stickiness, thus "thinning the blood" and further enhancing blood flow.

L-PYROGLUTAMIC ACID 1-Pyroglutamic acid (also called 2-oxo-pyrrolidone carboxylic acid or 1-PCA) is a cyclized derivative of the amino acid glutamate. Aside from functioning as an amino acid, glutamate 15 is also the most abundant excitatory neurotransmitter in the central nervous system, and may play a role in learning and memory. 1-Pyroglutamic acid is also a precursor to the important inhibitory neurotransmitters glycine and GABA, which are associated with the mental states of calm and serenity.

In addition, 1-pyroglutamic acid is associated with the activity of the key neurotransmitter 20 acetylcholine (ACH), necessary for muscle control and memory. Studies show that orally administered 1-pyroglutamic Boron Studies have shown that a low boron diet influences brain waves. They have shown when subjects ate less boron they were less alert.

Vitamin E Of the various types of chemicals found within the body, fat is the most susceptible to being damaged by free radicals. This explains why the brain, having such a high content of fat, is at such an increased risk for free radical damage. Vitamin E is a "fat soluble" antioxidant meaning that its protective effect is most realized in tissues with a high fat content - like the 30 brain. Indeed, diets rich in natural sources of vitamin E are associated with a reduction in the 130110NZ Prov.doc/CA/ca risk of Parkinson's disease. In individuals already given the diagnosis, the progression of Parkinson's disease has been dramatically slowed with vitamin E and C supplementation.

Alpha Lipoic Acid This is a powerful antioxidant able to regenerate important brain antioxidants including 5 vitamins E, C, and glutathione. Unlike other antioxidants, alpha lipoic acid is both fat-soluble and water-soluble. This greatly enhances its ability to be absorbed from the gut and permits increased penetration into the brain.

N-Acetyl-L-Cysteine (NAC) While glutathione represents one of the most important of the brain's antioxidant's defenses, it is generally considered useless when given orally. NAC is readily absorbed from the gut and dramatically increases the body's production of brain protecting glutathione. The ability of NAC to increase brain glutathione is enhanced in the presence of adequate amounts of vitamin C and E. In addition to enhancing glutathione production, NAC itself is a potent antioxidant and has been demonstrated to reduce the formation of the free radical nitric oxide, which has been implicated as having a causative role in Parkinson's disease, Alzheimer's disease, and several other neurodegenerative disorders.

Vitamin B12 (Cyanocobalamin) Deficiency of vitamin B12 has been associated with mental slowness, confusion, depression, memory difficulties, and abnormalities of nerve function, Alzheimer's disease, and multiple sclerosis. Not only is vitamin B12 critical for the maintenance of myelin, the protective insulating coat surrounding each neuron, but it also helps reduce the level of a particular amino acid, homocysteine, which has been associated with increased risk for Alzheimer's disease, stroke, and myocardial infarction.

Folic Acid A large number of studies have confirmed a direct relationship between folic acid status and various neurological problems including dementia, memory loss, and even depression. Like vitamin B12, the importance of folic acid in preserving normal brain function likely stems from its role in reducing homocysteine. Homocysteine is a toxic amino acid, elevation of which is associated with more rapid deterioration in some forms of dementia as well as a 30 dramatic increase in stroke risk. 130110NZ Prov.doc/CA/ca Niacin (as niacinamide) Like pyridoxine, niacin is a B vitamin and a key cofactor in the fundamental process of brain cell energy production. Deficiencies of niacin can profoundly affect brain cell metabolism resulting in dementia.

Pyridoxine Pyridoxine is a B vitamin critical for maintenance of adequate cellular metabolism. Its role in preserving brain function has been demonstrated in several studies showing a direct relationship between low levels of pyridoxine and severity of dementia. Like folic acid and B12, pyridoxine helps reduce homocysteine.

Rosemary extracts 6% carnosic acid Carnosic acid standardized rosemary extract to be as effective as activin (grape seed extract) and pycnogenol and twice as effective as vitamin E at inhibiting the oxidation of cholesterol in human aortic endothelial cells. This and other studies prove Carnosic acid to be an effective fat-soluble antioxidant. Brain tissue is mostly fat.

The following example is a preferred embodiment of the present invention and shows a composition in the form of an oral composition (tablet form) and the constituent components that go into making that composition. Of course, in alternative embodiments not described, any appropriate selection or combination of the component parts used in the formulation of the oral composition of the example given below, could be used to form alternative 20 compositions, that could be oral compositions in the form of tablets or fluids or injectable compositions. 13011ONZ Prov.doc/CA/ca Each tablet contains: Vitamins and Minerals Vitamin A (as Beta-Carotene) About 1 mg 1000IU %USRDA % Vitamin B1 (Thiamine) as Thiamin Mononitrate, or HC1) mg Vitamin B2 (Riboflavin) mg Vitamin B3 (Inositol Hexanicotinate 100 mg & Niacinamide 50 mg) Vitamin B5 (Pantothenic Acid, or D-Calcium Pantothenate) mg mg Vitamin B6 (Pyridoxine HC1) 10 mg Vitamin B12 (Cyanocobalamin) 25 meg Folic Acid 400 meg Biotin 50 meg Vitamin C (Calcium, or Zinc Ascorbates) mg Vitamin E (D-Alpha Tocopheryl Succinate, or Acetate) U I 666% 586% 100% 500% 500% 420% 50% 17% 32% 100% Calcium (Ascorbate, or Carbonate, or Malate, or Succinate) 50 mg % Magnesium (Malate, or Succinate, or^Omg 12.5% 130110NZ Prov.doc/CA/ca Taurinate, or Oxide) Zinc (Ascorbate) 10 mg 67% Manganese (Citrate) 5 mg * Selenium (Sodium Selenite) 50 meg 72% Boron (Citrate) 250 meg * Copper (Sebacate) 0.5 mg 25% Molybdenum (Sodium Molybdate) 25 meg 33% Chromium ( Chromium Chloride, or 50 meg 42% Nicotinate) * U.S. RDA not established.

Amino Acids & Other Ingredients: * L-Pyroglutamic Acid 80 mg * L-Glutamine 100 mg * Acetyl L-Carnitine , or L-Carnitine 100 mg DMAE (Dimethylaminoehtanol * 40 mg Bitartrate) Taurine (L-Taurine, or Magnesium * mg Taurinate) DLPA (DL-Phenylalanine) 30 mg * Phosphatidyl-Choline lOOmg * Phosphatidyl-Ethanolamine 25 mg Choline (Bitartrate) 40 mg 130110NZ Prov.doc/CA/ca N-Acetyl L-Tyrosine, or L-Tyrosine 80 mg GABA (Gamma Amino Butyric Acid) 30 mg PAK (Pyridoxine alpha-Ketoglutarate) 20 mg Ginkgo biloba Leaf Extract (with 24% Ginkgo Flavone Glycosides from 1500 mg mg Ginkgo Biloba Leaf in a 50:1 concentration) Phosphatidyl-Inositol, or Inositol 30 mg Lipoic Acid 10 mg Phosphatidyl Serine 25 mg DHA powder (docosahexaenoic acid) 20 mg Huperzine A (huperzia serrata club moss) meg Standardized Herbal Extracts Formula 200 mg (Siberian Ginseng, 25 mg; Gotu Kola, 25 mg; Ginger Root, 25 mg; Schizandra, 25 mg; & Cayenne, 25 mg; Grape Seed Extract 25 mg, and Bacopa monniera (water hyssop), or Rosemary, 50 mg) Total active ingredients = 1207 mg Excipients 293 mg Weight of one Tablet = 1500 mg 130110NZ Prov.doc/CA/ca Excipients / One Tablet Microcrystalline Cellulose 2-6% = 100 mg.

Mg Stearates / Stearic Acid 2-6% = 20 mg.

Silicon Dioxide 1-3% = 15 mg Hydroxypropylcellulose 0.5-2.5% = 30 mg.

Sodium Carboxymethylcellulose 0.5-2% = 33 mg.

Maltodextrin/or/Fructose 2-6% = 55 mg. OR FOS (FructoOlogoSaccharides.

Talc 2-5% = 40 mg. 293 mgs.

Example 1207 mg. Ingredients + 293 mg. Excipients = One Tablet 1500 mgs. Weight The shape of the tablet is Capsule-Shape Maximum length = 20 mm.

Maximum Width = 9 mm 20 Maximum Thickness = 8 mm.

Maximum Weight 1500 mgs. + 3% = 1545 mgs.

Minimum Weight 1500 - 3% = 1455 mgs.

Direct press tabletting process (Direct Compaction) The Tablets to be coated by any thin film polymer, if required.

Suggested Use: Two to Four tablets daily between meals. If digestive irritation occurs, take with meals. Or, take as recommended by your health care professional.

MIXING PROCESS: Recommended Procedure; 1/. Combine all ingredients in Phase A (Herbal Extracts) in order listed with 130110NZ Prov.doc/CA/ca mixing, under very low humidity (less than 40%). 21. Combine all ingredients in Phase B (Vitamins) in order listed with mixing, under very low humidity (less than 40%). 3/. Separately combine ingredients in Phase C (Trace elements) and 5 ensure fully mixed. 4/. Combine all ingredients in Phase C (Minerals) in order listed with mixing, under very low humidity (less than 40%).

/. Separately combine ingredients in Phase D (Amino Acids) and ensure fully mixed. 6/. Combine all ingredients in Phase D (Supplements) in order listed with mixing, under very low humidity (less than 40%). 7/.Add premixed Phase An ingredients in large mixer (e.g., Sigma, or Cubic Mixer) and by continuous mixing adds the other premixed Phases B, C, and D in order listed- ensure fully mixed. 8/. Ideally homogenize or mill (as required) prior to pressing process to tablets, similar to Male tablets.

Research documents that ginkgo can improve the retention of learned behaviour, in other words, short-term memory formation. It can also enhance mental alertness and general cognitive performance and gently elevate mood.

One explanation for the herb's ability to boost memory power is that ginkgo is an antioxidant, meaning it scavenges the blood for harmful free radicals (toxins) which would otherwise damage or destroy brain cells. Another reason is that ginkgo improves blood flow to the brain. Increased circulation to the brain means that more blood sugar (the prime energy 130110NZ Prov.doc/CA/ca source) can be delivered to brain cells, thereby increasing mental alertness. Greater blood flow also means increased oxygen availability to brain cells In addition to ginkgo, PS, and DHA, contains other substances known to benefit brain function. Folic acid enhances brain blood circulation. Vitamin B12 is an essential component 5 in the protective wrapping (myelin sheath) around nerve fibers; B12 deficiencies are associated with poor memory and reasoning skills, and age-associated cognitive decline. Acetyl-L-carnitine (an amino acid) enhances energy production in the mitochondria (cellular energy "factories") of brain cells and improves communication across the brain hemispheres.

The product offers PS, DMAE, acetyl-L-carnitine, choline, ginkgo, glutamine, and 10 pyroglutamic acid, but adds to this mixture several other useful substances. Provides the "full potency therapeutic dosages, as based on clinical research, in each tablet. Ashwaganda, an herb from Indian Ayurvedic medicine, is included for its antiaging benefits; when the body ages quickly or even prematurely, brain function is inevitably affected, so slowing the aging process in itself helps maintain cognitive abilities.

Gotu kola is considered a "fountain of youth herb" in Chinese herbology; in Ayurvedic medicine, it is an energy tonic believed to strengthen brain cells and stimulate mental alertness.

Glutamine is one of the most prevalent amino acids found in the brain. It functions as a neurotransmitter that is a major fuel source for the brain and the entire body.

Choline is a nutrient needed for producing neurotransmitters, Minerals such as calcium and magnesium are included to form neural electrolytes involved in the flow of electricity through the brain; the antioxidant vitamins A and E help protect nerve cell membranes against damage by toxins and free radicals and aid in the transmission of nerve cell signals; and the amino acid DL-phenylalanine is a key building block for the 25 neurotransmitter norepinephrine, enabling nerve cells to communicate. The nutrients, working together, produce a synergistic benefit and an action that surpasses the contributions of the individual nutrients acting alone, "Fatty acids play a key role in brain health and disease because they are so abundant in nervous tissue, including the bran's gray matter and white matter and the myelin sheaths. Fatty acids are the building blocks for neuron cell 13011ONZ Prov.doc/CA/ca membranes (as well as phospholipids, which are made of fatty acids plus phosphorus and glycerol) and help protect brain cells from damage by toxins. Fatty acids not only affect the structural integrity of brain cell membranes, but they influence the way these cells make connections with neurotransmitters.

Phosphatidyl serine (PS) is a large fat molecule found in trace amounts in lecithin, derived from soybeans. While it's present throughout the body, its levels are especially high in nerve cell membranes. Although the brain normally produces enough PS, if the diet is deficient in essential fatty acids, or vitamins such as folic acid and B12, PS production may be blocked.

The one of the main component of this supplement (derived from micro algae) is DHA 10 (docosahexaenoic acid), the primary structural fatty acid in the retina of the eye and the gray matter of the brain. (DHA, which is an omega-3 long-chain fatty acid, is unrelated to DHEA, which is a hormone.) That explains why adequate levels of DHA are required for proper brain and eye development and function. In fact, about 60% of the brain is made of fats, of which DHA is the most abundant.

DHA is believed to assist nerve cells in the brain, retina, and elsewhere in the nervous system in sending messages to other cells by way of electrical current. According to Martek, this vegetable oil form of DHA "closely matches" the DHA found in human breast milk.

Neurotransmitters and Brain Chemical Precursors—A neurotransmitter is a brain chemical with the specific function of enabling communications to happen between brain cells, called 20 neurons. Electrical thought impulses are changed into neurotransmitters at the dendrites, the branching tips of a nerve cell; then they are passed on to the next nerve cell. Among the 100 neurotransmitters identified to date, six are involved in most mental activities.

This product supplies DMAE, a key precursor to the neurotransmitter acetylcholine. DMAE stands for di-methyl-aminoethanol, a substance naturally found in anchovies and sardines 25 and believed to slow down, possibly prevent, mental deterioration and memory loss, and to elevate concentration and learning ability. DMAE does this primarily by helping the body create acetylcholine, which is required for short-term memory storage and recall and communication between the brain and all body muscles. 130110NZ Prov.doc/CA/ca This product included multiple-nutrient formula provides vitamins (B complex and C), minerals (magnesium, manganese, and zinc), herbal extracts and 12 neuronutrients such as DMAE, several amino acids and antioxidants, and phosphatidyl choline as neurotransmitter precursors, all essential to acetylcholine synthesis, as well as several amino acids intricately 5 involved in brain function: L-glutamine (a precursor for glutamic acid, a neurotransmitter which switches on brain activity) and L-pyroglutamic acid (which activates brain cells that use acetylcholine).

Huperzine A is an isolated alkaloid compound derived from Chinese club moss {Huperzia serrata or Club moss). In traditional Chinese medicine the dried or fresh herb was boiled in water, strained and consumed as a tea for kidney and bladder complaints, as well as a treatment for fevers and inflammation. Though there are toxicities associated with the consumption of the whole herb, the purified Huperzine an alkaloid is proven safe. , Blocks the enzyme that otherwise breaks down acetylcholine.

Gotu kola (centella asiatica) has been traditionally used as a neural tonic that slowly supports mental stamina and brain The intention underlying this combination is to enhance brain energy metabolism. ADVANTAGES The present invention provides a composition that is more effective as a health supplement because the components that go into making the composition act in a synergistic fashion to produce an improved health supplement.

Throughout the description and claims of this specification, the word "comprise and variations of that word such as "comprises" and "comprising" are not intended to exclude other additives, components, integers or steps.

Furthermore, this invention may broadly be said to consist in the parts elements and features 25 referred to or indicated in the specification of the application, individually or collectively and any or all combinations of any two or more of the parts, elements or features, and where specific integers are mentioned herein which have known equivalents are deemed to be incorporated herein as if individually set forth. £ 20 130110NZ Prov.doc/CA/ca

Claims (64)

-22- Throughout the description and claims of this specification the word "comprise" and variations of that word, such as "comprises" and "comprising", are not intended to exclude other additives, components, integers or steps. 5 10 15 130110NZ Prov.doc/CA/ca -23- CLAIMS

1. A composition suitable for administering to warm blooded animals as a health supplement including pyridoxine alpha ketoglutarate and acetyl L-carnitine wherein the composition further includes at least one plasmalogen phosphalide, an inositol, and extract of ginko 5 biloba.

2. A composition as claimed in claim 1, wherein the or each plasmalogen phosphalide can be selected from the group comprising phosphatidyl choline and phosphatidyl ethanolamine.

3. A composition as claimed in claim 1 or claim 2, wherein the or each inositol can be selected from the group comprising phosphatidyl inositol and inositol. 10

4. A composition as claimed in any preceding claim, wherein the composition further comprises vitamins.

5. A composition as claimed in claim 4, wherein the vitamins can be selected from the group comprising A, C, E and a B complex.

6. A composition as claimed in claim 5, wherein the vitamin B complex can be selected from 15 the group comprising Bl, B2, B3, B5, B6 and B12.

7. A composition as claimed in any preceding claim, wherein the composition further comprises a metal derivative.

8. A composition as claimed in claim 7, wherein the metal derivative can be selected from the group comprising mono, di, tri and tetra valent metal derivatives. 20

9. A composition as claimed in claim 8, wherein the divalent metal derivative can be selected from the group of metals comprising calcium, zinc, copper, manganese, chromium and magnesium.

10. A composition as claimed in the preceding claim, wherein the divalent metal derivative can be selected from the group comprising calcium ascorbate, carbonate, nicotinate, 25 sebacate, chloride, malate, taurinate, oxide,citrate or succinate. 130110NZ Prov.doc/CA/ca -24-

11. A composition as claimed in claim 8, wherein the trivalent metal derivative can be selected from the group of metals comprising boron and chromium.

12. A composition as claimed in the preceding claim, wherein , the trivalent metal derivatives can be selected from the group comprising chloride, nicotinate and citrate. 5

13. A composition as claimed in claim 8, wherein the monovalent metal derivative can be selected from the group of metals comprising potassium, sodium and lithium.

14. A composition as claimed in the preceding claim, wherein the monovalent metal derivatives can be selected from the group comprising selenite and molybdate.

15. A composition as claimed in any preceding claim, wherein the composition further 10 comprises an amino acid.

16. A composition as claimed in the preceding claim, wherein the amino acid can be selected from the group comprising L-glutamine, Taurine, N-acetyl L-Tyrosine, and L-Tyrosine.

17. A composition as claimed in any preceding claim, wherein the composition further comprises at least one of the following, L-Pyroglutamic acid, 15 dimethylaminoethanolbitartrate, DL-phenylalanine, choline bitartrate, liopic acid, docosahexaenoic acid, folic acid, biotin, huperzine and/or phosphatidyl serine.

18. A composition as claimed in any preceding claim, wherein the composition further comprises one or more herbal extracts.

19. A composition as claimed in the preceding claim, wherein the herbal extracts can be 20 selected from the group comprising Siberian ginseng, gotu kola, ginger root, schizandra, cayenne, grape sees extract, bacopa monniera and rosemary.

20. A composition as claimed in any preceding claim, wherein the composition further comprises an excipient.

21. A composition as claimed in the preceding claim, wherein the extract of Ginkgo biloba is 25 in the range of 1.0-5.0 x 10-3 %w/v. 130110NZ Prov.doc/CA/ca -25 -

22. A composition as claimed in any preceding claim, wherein the pyridoxine alpha ketoglutarate is in the range of 10-30 x 10-3 %w/v.

23. A composition as claimed in any preceding claim, wherein the acetyl L-carnitine is in the range of 40-150 x 10-3 %w/v. 5

24. A composition as claimed in any preceding claim, wherein the plasmalogen phosphalide is in the range of 50-200 x 10-3 %w/v.

25. A composition as claimed in any preceding claim, wherein the phosphatidyl choline is in the range of 40-150 x 10-3 %w/v.

26. A composition as claimed in any preceding claim, wherein the phosphatidyl 10 ethanolamine is in the range of 5-40 x 10-3 %w/v.

27. A composition as claimed in any preceding claim, wherein the inositol is in the range of 5-50 x 10-3 %w/v.

28. A composition as claimed in any preceding claim, wherein the phosphatidyl inositol is in the range of 5-50 x 10-3 %w/v. 15

29. A composition as claimed in any preceding claim, wherein the vitamin B complex is in the range of 30-150 x 10-3 %w/v.

30. A composition as claimed in any preceding claim, wherein the vitamin A is in the range of 2-20 x 10-4 %w/v.

31. A composition as claimed in any preceding claim, wherein the vitamin C is in the range 20 of 5-30 x 10-3 %w/v.

32. A composition as claimed in any preceding claim, wherein the folic acid is in the range of 100-600 x 10-3 %w/v.

33. A composition as claimed in any preceding claim, wherein the botin is in the range of 20-80 x 10-3 %w/v. 25

34. A composition as claimed in any preceding claim, wherein the calcium derivative is in the range of 20-80 x 10-3 %w/v 130110NZ Prov.doc/CA/ca -26-

35. A composition as claimed in any preceding claim, wherein the magnesium derivative is in the range of 20-80 x 10-3 %w/v.

36. A composition as claimed in any preceding claim, wherein the zinc derivative is in the range of 3-15 x 10-3 %w/v. 5

37. A composition as claimed in any preceding claim, wherein the manganese derivative is in the range of 2-8 x 10-3 %w/v.

38. A composition as claimed in any preceding claim, wherein the selenium is in the range of 20-80 x 10-3 %w/v.

39. A composition as claimed in any preceding claim, wherein derivative is in the range of 10 100-400 x 10-3 %w/v.

40. A composition as claimed in any preceding claim, wherein the copper derivative is in the range of 1-8 x 10-4 %w/v

41. A composition as claimed in any preceding claim, wherein the molybdenum derivative is in the range of 7-40 x 10-3 %w/v. 15

42. A composition as claimed in any preceding claim, wherein the chromium derivative is in the range of 20-80 x 10-3 %w/v.

43. A composition as claimed in any preceding claim, wherein the L-Pyroglutamic acid is in the range of 20-120 x 10-3 %w/v.

44. A composition as claimed in any preceding claim, wherein the L-glutamine is in the 20 range of 20-160 x 10-3 %w/v.

45. A composition as claimed in any preceding claim, wherein the acetyl L-carnitine is in the range of 20-160 x 10-3 %w/v.

46. A composition as claimed in any preceding claim, wherein the L-cartinine is in the range of 40-160 x 10-3 %w/v. 25

47. A composition as claimed in any preceding claim, wherein the dimethylaminoethanolbitartrate is in the range of 10-60 x 10-3 %w/v. 130110NZ Prov.doc/CA/ca -27-

48. A composition as claimed in any preceding claim, wherein the taurine is in the range of 5-50 x 10-3 %w/v.

49. A composition as claimed in any preceding claim, wherein the DL phenylalanine is in the range of 5-50 x 10-3 %w/v. 5

50. A composition as claimed in any preceding claim, wherein the choline is in the range of 20-50 x 10-3 %w/v.

51. A composition as claimed in any preceding claim, wherein the N-acetyl L-tyrosine is in the range of 20-120 x 10-3 %w/v.

52. A composition as claimed in any preceding claim, wherein the L tyrosine is in the range 10 of 20-120 x 10-3 %w/v.

53. A composition as claimed in any preceding claim, wherein the gama amino butyric acid is in the range of 5-50 x 10-3 %w/v.

54. A composition as claimed in any preceding claim, wherein the lipoic acid is in the range of 3-15 x 10-3 %w/v. 15

55. A composition as claimed in any preceding claim, wherein the phsphatidyl serine is in the range of 7-40 x 10-3 %w/v.

56. A composition as claimed in any preceding claim, wherein the docosahexaenoic acid is in the range of 8-30 x 10-3 %w/v.

57. A composition as claimed in any preceding claim, wherein the huperzine is in the range 20 of 7-40 x 10-3 %w/v.

58. A composition as claimed in any preceding claim, wherein the Siberian Ginseng is in the range of 7-40 x 10-3 %w/v.

59. A composition as claimed in any preceding claim, wherein the Gotu Kola is in the range of 7-40 x 10-3 %w/v. 25

60. A composition as claimed in any preceding claim, wherein the Ginger Root is in the range of 7-40 x 10-3 %w/v. 130110NZ Prov.doc/CA/ca §30554

61. A composition as claimed in any preceding claim, wherein the Schizandra is in the range of 7-40 x 10-3 %w/v.

62. A composition as claimed in any preceding claim, wherein the cayenne is in the range of 5 7-40 x 10-3 %w/v.

63 A composition as claimed in any preceding claim, wherein the grape seed extract is in the range of 7-40 x 10-3 %w/v.

64. A composition as claimed in any preceding claim, wherein the bacopa monniera or rosemary is in the range of 15-60 x 10-3 %w/v. 10 Andre Chissel 15 For PIPERS PATENT & TRADE MARK ATTORNEYS 20 INTELLECTUAL PROPERTY OFFICE OF N.Z 12 JAN 2004 RECEIVED Document2//ca