Organic compounds -- part of the class 532-570 series – Organic compounds – Oxygen containing
Reexamination Certificate
2000-01-21
2001-07-17
Page, Thurman K. (Department: 1615)
Organic compounds -- part of the class 532-570 series
Organic compounds
Oxygen containing
C568S832000, C568S816000, C424S439000, C424S464000
Reexamination Certificate
active
06262316
ABSTRACT:
The present invention relates to an oral preparation for the prophylactic and/or therapeutic treatment of inflammation in the mucous membrane of mammalian gastrointestinal tract caused by Helicobacter sp. infection. The preparation comprises at least one type of xanthophylles, preferably naturally produced astaxanthin.
BACKGROUND OF THE INVENTION
Since a few years
Helicobacter pylon
is classified as a primary cause of type B gastritis in humans.
Various Helicobacter sp. infect different animals, and must penetrate the gastric surface mucous layer [O'Toole PW et al., Mol Microbiol 1994, 14:691-703] to colonize the gastric epithelium and sub-mucosa [Wadström T et al., Aliment Pharmacol Ther 1996, 10(suppl 1): 17-28.; Valkonen K H et al., Infect immun 1994, 62:3640-3648.; Moran A P et al., J Appi Bacteriol 1993, 75:184-189.; Wadström T et al., Eur J Gastroenterol Hepatol 1993, 5 (suppl 2):512-515]. Helicobacter is a flagellated motile organism probably penetrating the gastric mucous layer rapidly and efficiently with spiral movements associated with the unique spiral shape of this pathogen (Helicobacter from helix, which is Latin for spiral).
Helicobacter pylori
can cause drastic changes of the gastric mucous membrane barrier functions in an early infection (i.e. type B gastritis) with breakdown of the hydrophobic lining of the gastric epithelium. This can cause back-flow of acid and pepsin from the lumen into the mucosa to cause peptic ulcers in the stomach and duodenum. It seems likely that this breakdown of the mucosa barrier also affects the uptake in the gastric mucosa of a number of substances in food such as certain food-associated carcinogens.
Xanthophylles, including astaxanthin, is a large group of carotenoids containing oxygen in the molecule in addition to carbon and hydrogen. The carotenoids are produced de novo by plants, fungi and some bacteria [Johnson E. A. and Schroeder W. A., 1995, Adv In Biochem Engin. Biotechn. 53: 119-178]. In biological tests astaxanthin has been shown to possess clearly the best antioxidative properties compared to other carotenoids [Miki W., 1991, Pure and Appl Chem 63 (1): 141-146].
At present, the therapeutic treatment of inflammation in the mucous membranes of mammalian gastrointestinal tract caused by Helicobacter sp. infection, mainly involves the use of so-called proton pump inhibitors, such as Losec® (omeprazol), and in case of gastric ulcers different antibiotics (which may cause the development of resistant strains).
DESCRIPTION OF THE INVENTION
The present invention provides an oral preparation for the prophylactic and/or therapeutic treatment of inflammation in the mucous membrane of mammalian gastrointestinal tract caused by Helicobacter sp. infection, which comprises a prophylactically and/or therapeutically effective amount of at least one type of xanthophylles.
The oral preparation according to the invention may comprise a mixture of different types of xanthophylles or different forms of the same xanthophyll, such as a mixture of synthetic astaxanthin and naturally produced astaxanthin.
In a particular embodiment of the invention the mammalian gastrointestinal tract is the human stomach, and the Helicobacter sp. is
H. pylori.
The mechanism of the prophylactic and therapeutic effect of the xanthophylles in the treatment of inflammation in the mucous membrane of the mammalian gastrointestinal tract caused by Helicobacter sp. infection is not known, but it is believed that the antioxidative properties of the xanthophylies, which are soluble in fat/oil, play an important role in the protection of the hydrophobic lining of the mucous membrane so that Heilcobacter sp. cannot colonize.
In a preferred embodiment of the invention, the xanthophyll is dissolved in an oil of food grade.
In another preferred embodiment the type of xanthophyll is astaxanthin, particularly astaxanthin in a form esterified with fatty acids.
In yet another preferred embodiment the astaxanthin derives from a natural source, particularly a culture of the alga Haematococcus sp. [Renström B. et al, 1981, Phytochem 20(11) :2561-2564].
The oral preparation according to the invention may further comprise carbohydrate structures, such as lipopolysaccharides, polysaccharides and glycoproteins.
At present, the most preferred embodiment of the invention comprises algal meal having astaxanthin in esterified form with fatty acids dissolved in small droplets of naturally occurring oil and naturally occurring carbohydrate structures in the partially disrupted cell walls.
The oral preparation of the invention may comprise additional ingredients which are pharmacologically acceptable inactive or active in prophylactic and/or therapeutic use, such as flavoring agents, and a prophylactically and/or therapeutically effective amount of a water soluble antioxidant, especially ascorbic acid (vitamin C).
The oral preparation is presented in a separate unit dose or in mixture with food. Examples of separate unit doses are tablets, gelatin capsules and predetermined amounts of solutions, e. g. oil solutions, or emulsions, e.g. water-in- oil or oil-in-water emulsions. Examples of foods in which the preparation of the invention may be incorporated is dairy products, such as yoghurt, chocolate and cereals.
Another aspect of the invention is directed to a method of prophylactic and/or therapeutic treatment of inflammation in the mucous membrane of mammalian gastrointestinal tract caused by Helicobactersp. infection, which comprises administration to said mammal of an oral preparation according to the invention.
The daily dosis of the active ingredient of the invention will normally be in the range of 0.01 to 10 mg per kg body weight for a human calculated on the amount of astaxanthin, but the actual dosis will depend on the mammalian species and the individual species-specific biological effect.
REFERENCES:
patent: 07 099 924 (1995-04-01), None
patent: 07 300 421 (1995-11-01), None
patent: WO 95 00130 (1995-01-01), None
patent: WO 96 23489 (1996-08-01), None
Database WPI, Week 9603, Derwent Publications Ltd., London, GB AN 96-026969 XP002067981 (JP 07 300 421 AA, Nov. 14, 1995).
Database WPI, Week 9524, Derwent Publications Ltd., London, GB; AN 95-182023 XP002067980; (JP 07 099 924 A, Apr. 18, 1995).
P. Bubrick, “Production of Astaxanthin from Haematococcus”, Bioresource Technology, vol. 38, 1991, pp. 237-239.
D. Bagchi et al., “Production of Reactive Oxygen species By Gastric Cells in Association withHelicobacter Pylori” Free Redical Research, vol., 24, No. 6, 1996, Amsterdame, NL, pp. 439-450.
Alejung Pär
Wadström Torkel
Astacarotene AB
Bacon & Thomas
Page Thurman K.
Pulliam Amy E
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