In the course of looking for the mastitis patent, I came across another even more exciting patent filed by Phosphagenics – the application of TPM to nutraceuticals and cosmeceuticals. I’d be happy to sit there all day and read it but most of you will have less time and more sense than me, so I’ve condensed it (honestly!) and rearranged the key information just regarding nutraceuticals for this post.
THE APPLICATION OF TPM IN NUTRACEUTICALS
WHO?
Any animal, in particular mammals such as humans, domestic pets, livestock and other farmed animals.
WHY?
In addition to humans, various animal species including domestic pets, livestock and other farmed animals may suffer from nutrient deficiencies in their diets.
(Additionally)direct supplementation of vitamins and nutrients to animals has been reported to increase nutritional concentrations in the foods produced from those animals, including meat, milk and eggs.
Many supplements containing nutraceutical actives providing vitamins, minerals and nutrients are currently available. However, there are problems associated with the bioavailability of some nutraceutical actives. As one example, nutraceutical actives may be poorly bioavailable due to their hydrophobicity (i.e. (sic) poorly water solubility). Nutraceutical actives that are not readily bioavailable need to be administered in large amounts in order to ensure that a sufficient amount of the vitamin and/or nutrient is absorbed. This can increase the cost of the dose of a nutraceutical active quite dramatically, particularly if the nutraceutical active is difficult to isolate or expensive to purchase. It may also mean that multiple and/or large capsules need to be administered. Accordingly, there is a need for improved or alternative active compositions having improved bioavailability.
HOW?
(This invention) is suitable for topical, enteral or parenteral administration of the nutraceutical and cosmeceutical actives.
Suitable dosage forms for enteral administration would include but not be limited to capsules, tablets, pills, or specialty tablets such as buccal, sublingual, chewable tablets or orally-disintegrating tablets. Another example of a suitable dosage form would be edible thin films. Other suitable dosage forms for enteral administration include liquid solutions or suspensions. Suitable liquid solution or suspension dosage forms may be in the form of a drink, such as sports drinks containing electrolytes (e.g. gatorade), or syrup and elixirs. Other suitable liquid solution or suspension dosage forms include nasal delivery solutions and oral suspensions. Specifically liquid solutions or suspensions in the form of a "drench" may be suitable for use with large animals such as cows. The dosage form for enteral administration may also be a powder or solid crystal, which can be either dissolved or suspended in a liquid before administration. Alternatively, the powder may be consumed directly or added to a food or drink product for consumption. In the case of farm animals, the formulation may be added directly to the dry feed or in pelleted form.
Particularly in the case of a domestic or farm animal, the dosage form may include injection.
In another example, the dosage form for enteral administration may be a food to which the composition is added before the food is consumed. For example, the food product may for example be a bar such as a health bar, a cereal, bread such as a fortified bread, a cookie, a spread such as butter, a dairy product such cheese or milk, or any other suitable food product.
Examples of suitable dosage forms for parenteral administration include but are not limited to injectables (i.e. solutions, suspensions, emulsions, and dry powders for reconstitution), intramammary infusions, intravaginal delivery systems, and implants.
WHAT?
Suitable nutraceutical actives include, but are not limited to fatty acids, fruit and vegetable extracts, vitamins, phospholipids, certain proteoglycans, certain amino acids, carotenoids, various food additives, various phytonutrients including phytosterols, certain antioxidants, plant oils, fish and marine animal oils, algae oils and essential elements.
The nutraceutical and/or cosmeceutical active may be selected from the group consisting of vitamins, minerals, amino acids, herbs or other botanicals, metabolites, electrolytes, antioxidants, enzymes, organ tissues, gland extracts and prebiotics.
Preferably, the nutraceutical active is selected from the group consisting of CoQ10 (ubiquinone), ubiquinol, omega-3 (DHA or EPA), lycopene, resveratrol, vitamin E, vitamin D, and carotenoids such as beta-carotene, lutein and zeaxanthin, and selenium such as sodium selenite.
EXAMPLES OF TPM/NUTRACEUTICAL APPLICATION FOR ANIMALS
Selenium Selenium is an essential element for humans and animals. In the body selenium helps prevent damage by free radicals (i.e. acts as an antioxidant). It also has varied applications and uses in animal stockfeed., i.e. For example, selenium may be utilised in specialised feeds for horses to aid in muscle problems (tying up) that may be due to a wide range of causes, which include i.e. exercise in excess of training level, respiratory infections, lack of dietary selenium/vitamin E, electrolytes & minerals.
Carotenoid Beta-carotene is a carotenoid which... boosts the immune system in humans and animals. It has been found that supplementing cattle with antioxidants such as beta- carotene, vitamin E, selenium may reduce somatic cell counts and improve the health of cattle with mastitis infections.
Direct supplementation of vitamins and nutrients to animals has been reported to increase nutritional concentrations in the foods produced from those animals, including meat, milk and eggs.
EXAMPLES OF TPM/NUTRACEUTICAL APPLICATION FOR HUMANS
Omega-3 Omega-3 polyunsaturated fatty acids are essential fatty acids which must be obtained via dietary sources since they cannot be manufactured by the body. Omega-3 fatty acids are most often found in fish oil, but may also be manufactured commercially. Long chain omega-3 fatty acids include DHA and EPA. DHA is widely believed to provide healthy brain development, particularly in young children, can support fetal and maternal development and enhance skin and eye function.
Scientific research indicates benefits from omega-3 supplementation in human conditions including cardiovascular disease, rheumatoid arthritis, and high blood pressure. Deficiency of omega-3 may contribute to the development of psychiatric disorders including depression, bipolar disorder, schizophrenia, dementia, dyslexia and postpartum psychiatric disorders.
Omega-3 has extremely low water solubility and thus the oral bioavailability of omega-3 is quite low. Approximately 1-3g of Omega-3 is recommended in order to allow adequate intake given the low bioavailability and problems associated with formulation of Omega-3. Accordingly, administration of Omega-3 must either be via very large single dose capsules or via multiple capsules (3-6 capsules, depending on the brand and/or formulation). Another problem associated with the administration of omega-3 is the fish aftertaste, which can be very undesirable for people to take. There is therefore a need for an improved formulation for the delivery of (sic) CoQ10.
Results from Animal Testing
Co-administering omega-3 and non-neutralised tocopheryl phosphate significantly increased bioavailability of DHA in the plasma. adding non- neutralised tocopheryl phosphate to the formulation (formulation 2f) increased DHA levels to 275% (150 Mg/ml).
CoQ10 CoQ 0 plays an essential role in the production of energy in heart cells, and helps to maintain a healthy cardiovascular system. Clinical studies have shown that there is a correlation between cardiovascular disease and low tissue levels of CoQ10. Natural levels of CoQ 0decline as we age, and can also decline if we are taking certain medications, such as statins to lower the cholesterol levels in people with or at risk of cardiovascular disease. There is therefore a benefit associated with restoring the levels of CoQ 0 in the body.
CoQ 0 is an extremely water insoluble nutraceutical active, and is therefore poorly absorbed from dietary sources (i.e. only about 5 to 10% of the CoQ 0 is bioavailable). The CoQio used to prepare nutraceutical products is typically very expensive as CoQ10 is readily degraded due to its light and oxygen sensitivity. Production of CoQio is therefore quite laborious and requires nitrogen blanketing procedures to ensure that the stability and/or activity of CoQ10 is maintained. Although there are numerous CoQ10 products available on the market, the oral bioavailability of these products is low due to the low water solubility of CoQ 0 used in these formulations. It is therefore necessary to use excesses of CoQ 0 in order to ensure that sufficient amounts of CoQi0 are delivered. Alternative approaches to the delivery of CoQi0 use nanotechnology to improve the bioavailability of CoQi0, however, such approaches also add to the cost.
Results from Animal Testing
(The tested) formulation... provides a significant increase in the peak plasma CoQ10 concentrations, over a 24 hour period following a single dose of the formulation.
THE MARKET?
Simply almost every human and animal on this planet could benefit in the following ways:
• improved delivery of vitamins and minerals for humans • improved delivery of nutrients to farm animals to improve their health • improved nutritional value of animal products such as meat, milk and eggs • improved delivery of nutrients in pet food • improved body building supplements • specialized feeds for the horse and horseracing industry • safe, cheap, easy and effective treatment of mastitis in dairy cattle
APPROVAL FOR MARKET?
(AUS) The Therapeutic Goods Act 1989 requires that at the time of Listing, sponsors must certify that they hold information or evidence to support any claim that the applicant makes relating to the medicine. All indications and claims made about therapeutic goods must be capable of substantiation - that is, evidence must be held by sponsors which demonstrates the indications and claims are true, valid and not misleading.http://www.tga.gov.au/industry/cm-evidence-claims.htm
(US) Under , the Dietary Supplement Health and Education Act of 1994 a firm is responsible for determining that the dietary supplements it manufactures or distributes are safe and that any representations or claims made about them are substantiated by adequate evidence to show that they are not false or misleading. This means that dietary supplements do not need approval from FDA before they are marketed. http://www.fda.gov/Food/DietarySupplements/ConsumerInformation/ucm110417.htm#what
(EU) Proof, in the form of scientific dossiers, must establish to EFSA’s satisfaction that products intended for sale are safe and bioavailable. No claims may henceforth be made unless scientific dossiers establish to EFSA’s satisfaction that the claims are proven to a near conclusive degree. http://www.thebusinessmuse.com/mediablog/?p=405
Everyone has heard of the face which launched a thousand ships – well this is a platform technology capable of launching a thousand products.
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