Patent Application
20080220102
In the age of “Functional food”, it is no wonder that increasingly more nutritional physiologists and experts in the food industry, and also scholars from academic circles are interested in the active ingredients and nutrients present in plants. This interest is attributed to reasons related to consumer psychology in most cases.
Synthetically produced pure active ingredients require consistent maintenance of quality and, owing to the small volume, relatively uncomplicated and less efforts for the formulation to incorporate these substances into food. However, such highly concentrated synthetic products represent problems or barriers with regard to the food law.
Furthermore, the majority of consumers reject chemically produced food additives. Natural nutrients and active ingredients in plants, such as vegetables and fruits, are increasingly gaining acceptance among consumers and nutritional physiologists alike who are not constrained by the economy. In order to utilize this acceptance economically, the producers of food and cosmetics seek after e.g. plant extracts having high concentration of nutrients and active ingredients. New processes have been developed with a view to reduce the portion of undesirable concomitant substances in such extracts. While, in doing so, the natural food character of the extract is being increasingly removed in order to meet the requirements of the food law, the limits of economically justifiable technical feasibility have also been reached.
At the same time, the incorporation of such extracts into food poses another problem. The high amount and number of concomitant substances, which are irrelevant in terms of nutritional physiology or are undesirable to a certain extent, necessitate the use of large amounts of other additives (technological aids) in formulations in order to be able to incorporate the extract homogeneously and stably into the respective end products. However, such formulations have several disadvantages such as economic inefficiency, unpleasant sensory properties or insufficient long-term stability.
Furthermore, most of the interesting nutrients and active ingredients are lipophilic and thus poorly bioavailable to the human organism. Plant-based nutrients and active ingredients that are incorporated into cosmetics exhibit only a very moderate penetration into the skin. Since the extracts have only a relatively small concentration of nutrients and active ingredients, the low resorption of the lipophilic substances contained in the extracts casts the use of such extracts into doubt from the economic point of view.
The object underlying the invention is to process active ingredients, which are present in plants and have physiological or medicinal significance in such a way that they are more easily compatible with the human body even when present in higher concentrations.
For this purpose, the invention provides a solubilizate of a phytoextract containing the active ingredient, which solubilizate contains from about 10% by weight to about 30% by weight of the phytoextract, about 4% by weight to about 35% by weight of water, which can be deionized, demineralized or distilled once or many times, and from about 55% by weight to about 75% by weight of an emulsifier having an HLB-value ranging between 9-16, based on the solubilizate, which is equal to 100% by weight. The invention utilizes the fact that the active ingredient is contained with its natural concomitant substances and in natural concentrations, for example, in the commercially available phytoextract. Even if the active ingredient and its concomitant substances may split into several different micelles, when the micelles reaching the intestine empty out their content into the gut lumen, the latter receives not only the active ingredient but also all concomitant substances in natural concentration in the time average. The weight ratios specified have been selected such that the solubilizate of the invention is clear at body temperature, that is, at 37° C. and thus free from non-micellated portions and in a sufficiently liquid state.
For some phytoextracts, it is recommended, that the solubilizate of the invention contain a light oil, which comprises mainly medium-chain triglycerides, for example, Mygliol 812 or Delios VK kosher, in a proportion ranging from about 5% by weight to about 6% by weight. The oil prevents or complicates the precipitation of substances or substance particles from the solubilizate according to the invention.
The use of non-ionic, micelle-forming emulsifiers, primarily polysorbates, especially polysorbate 80 and/or polysorbate 20 as emulsifiers has proved to be useful. These emulsifiers are not only compatible with the requirements of the food law but also harmless in terms of their sensory properties. For protecting the active ingredients and concomitant substances from oxidation, it is recommended that the solubilizate of the invention contain one or more antioxidants such as, for example, ascorbic acid and/or a tocopherol, preferably a mixed tocopherol in a proportion ranging from about 4% by weight to about 6% by weight.
Furthermore, for obtaining a sediment-free micellization, it is advantageous in many cases if the weight ratio of phytoextract to water ranges from about 1.0 to about 3.0 and the weight ratio of phytoextract to polysorbate ranges from about 1.0 to about 6.0 in the solubilizate of the invention.
For a solubilizate containing about 10% reseda extract, the invention suggests, for example, that the solubilizate contain from about 15% by weight to about 30% by weight of water, about 10% by weight of reseda extract, and from about 60% by weight to about 75% by weight of polysorbate 80.
For a solubilizate containing about 10% by weight of St. John's wort extract, the invention suggests that the solubilizate contain from about 20% by weight to about 35% by weight of water, about 10% by weight of St. John's wort extract, and from about 55% by weight to about 70% by weight of polysorbate 80.
For a solubilizate containing about 10% by weight of tarragon extract, the invention suggests that the solubilizate contain from about 15% by weight to about 30% by weight of water, about 10% by weight of tarragon extract, and from about 60% by weight to about 75% by weight of polysorbate 80.
For a fat-soluble and water-soluble solubilizate containing about 12% hydroxytyrosol, the invention suggests by way of example that the solubilizate contain about 4% by weight of water, about 30% by weight of a hydroxytyrosol extract, which contains about 40% (based on the extract, which is equal to 100%) of hydroxytyrosol, about 58% by weight of polysorbate 80, about 4% by weight of a mixed tocopherol, and about 4% by weight of ascorbic acid.
For a fat-soluble and water soluble solubilizate containing about 15% rooibos extract, the invention suggests by way of example that the solubilizate contain about 15% by weight of water as distilled water, about 15% by weight of rooibos extract, about 60% by weight of polysorbate 80, about 5% by weight of a light oil containing mainly medium-chain triglycerides, and about 5% by weight of ascorbic acid.
For a fat-soluble and water-soluble solubilizate containing about 14% polyphenol, the invention suggests that the solubilizate contain about 14% by weight of water, about 14% by weight of a polyphenol extract, which predominantly contains tannin, gallic acid, and catechine as tanning agents, from about 30% by weight to about 33% by weight of polysorbate 20, from about 30% by weight to about 33% by weight of polysorbate 80, about 6% by weight of a light oil containing mainly medium-chain triglycerides, and from about 0% by weight to about 6% by weight of ascorbic acid.
For a rosemary extract-solubilizate, the invention suggests that the solubilizate contain from about 5% by weight to about 15% by weight of water, from about 15% by weight to about 20% by weight of a rosemary extract, which contains the antioxidant camosic acid, from about 50% by weight to about 75% by weight of polysorbate 80, from about 0% by weight to about 10% by weight of a light oil containing medium-chain triglycerides, from about 0% by weight to about 1.5% by weight of a mixed tocopherol, and from about 4% by weight to about 5% by weight of ascorbic acid.
Finally, for an olibanum-solubilizate, the invention suggests that the solubilizate contain about 24% by weight of water, about 12% by weight of an olibanum extract, which contains about 85% (based on the extract, which is equal to 100%) of boswellic acid, and about 64% by weight of polysorbate 20.
The solubilizates of the invention can be easily incorporated into cosmetic products such as ointments, pharmaceutical preparations, food preparations and food supplements and can be added to non-alcoholic drinks such as fruit juices and mineral water without any additional intermediate steps.
In a method suggested by the invention for producing solubilizates, from about 10% by weight to about 30% by weight of a phytoextract is mixed with from about 4% by weight to about 30% by weight of water, which is preferably deionized and/or demineralized and/or distilled once or many times, under mild heat of, for example, from about 40° C. to about 50° C. and the non-ionic and micelle-forming emulsifier, which has an HLB-value ranging from 9 to 16 and is heated to about 50°, is mixed into this mixture. The composition obtained is heated well, for example, to about 90° C. and homogenized until the fat-soluble and water-soluble solubilizate is obtained.
If the quantity of solubilizate, which contains as much active ingredient as is required to meet the daily human requirement, is dissolved in 1-liter of drinking water, the drink obtained therefrom indicates a turbidity of about 5.0 on a scale of from 0 to 2000 of a standard turbidimeter.
The following extracts are relevant to the invention.
Flavanoids, such as e.g. flavone “luteolin” C15H10)6 or luteolin-7-glucoside C21H20O11, which is contained in reseda luteola (dyer's rocket, weld), artichokes, capsicum or maidenhair-tree leaves, or can be educed therefrom by various methods is considered to be an extremely effective substance to prevent the formation of cholesterol in blood and actively promotes fat digestion. Flavanoids are polyphenols that are most frequently found in food.
It is extremely difficult to incorporate the extracts mentioned above into the respective end products in a homogeneous and stable manner and the substance “luteolin” present therein is both poorly bioavailable and unstable. The solubilization of this extract reduces these problems considerably.
In addition to flavanoids such as, rutin, hyperoside, quercitrin, and quercitin, an extract derived from St. John's wort (Hypericum Perforatum) contains naphthodianthrone pseudohypercin, hepericin, and hyperforin.
Since generations, St. John's wort is considered to be a reliable and effective medicinal plant for the treatment and prevention of neurodegenerative disorders. This effect is mainly attributed to the substances of hypericin and hyperforin contained therein.
It is difficult to incorporate this extract as well into the respective end products and the active ingredients present therein are extremely unstable and poorly bioavailable. The solubilization of this extract enables easy incorporation into the end products, stabilizes the active ingredients, and results in significantly higher bioavailability and penetration.
3. Tarragon Extract (Artemisia dracunculus)
This plant originating in the South Russia and the Mongolian steppes contains inter alia high amounts of potassium, ascorbic acid, magnesium, vitamin A, and iodine. Tarragon is used inter alia as a medicinal plant in connection with rheumatic ailments and scurvy. In addition, tarragon is believed to provide relief in
Tarragon also promotes the formation of gastric juices.
The problems enumerated in items 1) and 2) above also apply to this extract. These problems can be significantly attenuated by a solubilization of the extract.
The invention will be explained below with reference to some exemplary embodiments.
Reseda extract
Reseda extract
Reseda extract
Reseda extract
Mix reseda extract with product water (at 50° C.). Heat polysorbate to 50° C. and incorporate into the mixture composed of extract and water with stirring. Heat again thoroughly (approx. 90° C.) and homogenize.
Mix hyperforin with product water (at approx. 45° C.). Heat polysorbate to 50° C. and incorporate into the mixture composed of extract and water with stirring. Heat again thoroughly (approx. 90° C.) and homogenize.
Mix tarragon extract with product water (at approx. 50° C.). Heat polysorbate to 50° C. and incorporate into the mixture composed of extract and water with stirring. Heat again thoroughly (approx. 90° C.) and homogenize. The solubilizates obtained from the exemplary embodiments described above are fat-soluble and water-soluble, and stable against thermal influencing and stomach acids. The turbidity (based on the respective daily requirement in e.g. a 1 liter drink) on a scale of 0-2000 is approx. 5.0.
Appearance:
Dark brown, viscous
Storage Conditions:
Dark and cool (<25°)
Appearance:
Dark brown-black, viscous gel-like
Storage Conditions:
Dark, at room temperature (<25°)
Dark and cool (<25°)
Dark, at room temperature (<25°)
Dark and cool (<25°)
Dark, at room temperature (<25°)
Dark, at room temperature (<25°)
Brownish, clear, viscous.
| Number | Date | Country | Kind |
|---|---|---|---|
| 10 2005 032 352.9 | Jul 2005 | DE | national |
| 10 2005 056 381.3 | Nov 2005 | DE | national |
| 10 2006 024 911.9 | May 2006 | DE | national |
| Filing Document | Filing Date | Country | Kind | 371c Date |
|---|---|---|---|---|
| PCT/EP2006/006655 | 7/7/2006 | WO | 00 | 1/7/2008 |
