Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution...
Reexamination Certificate
2000-09-01
2001-09-18
Naff, David M. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
C424S729000, C424S774000, C424S776000, C424S777000, C424S439000, C514S283000
Reexamination Certificate
active
06290994
ABSTRACT:
TECHNICAL BACKGROUND OF THE INVENTION
The present invention relates to a new composition which stimulates cerebral activity, based on the discovery of the powerful action which certain eburnamenine ring alkaloids have when they are administered together with compounds of xanthine structure.
PRIOR ART
In general, the alkaloids of eburnane skeleton are peripheral vasodilators which are widely known (U.S. Pat. No. 4,400,514, Spanish Patent 549,105), which act as cerebral oxygenators Drug Res. [26(10a): 1947-1989 (1976)], and as memory activators [Drug Res. 26(10a):1947-1950 (1976); Eur. J. Clin. Pharmacol. 28:567-571 (1985); Drug Rev. Res. 14:191-193 (1988); Inter. Clin. Psychopharmacology 2:325-331 (1987)]. Furthermore, addition salts of eburnates are known which have properties similar to them or greatly improved properties and which furthermore are soluble in aqueous solutions from which potable solutions can be prepared; by way of example, it is sufficient to cite the citrate of vinpocetine [EP Patent 0154756], a cerebral oxygenator and vasodilator which has a better bioavailability and less toxicity than vinpocetine, its starting base.
With respect to the xanthic bases, we may cite, among the best known, theobromine which acts, among other things, as a cardiotonic [A. Lelo et al.: Brit J. Clin. Pharmacol. 22:177 (1986)]. Another interesting xanthine base is propentophylline, which acts as peripheral and cerebral vasodilator [K. Nagata et al.: Arzneimittel Forsch. 35:1034 (1985)] and as adenosine inhibitor [B. B. Fredheim et al.: Acta Pharmacol. Toxicol. 58:187 (1988)] and as cognitive activator [I. Hindmarch, Z. Subhan, Ibid. 5:379 (1985)], among others. Theophylline is a cardiac stimulant and muscular relaxant [(J. L. Cohen,
Analytical Profiles of Drug Substances
, Vol 4, K. Florey, Ed., Academic Press (N.Y.), p. 466-493 (1975)]. Finally, caffeine is a widely known general stimulant which is extracted from tea and coffee.
DESCRIPTION OF THE INVENTION
It has been known for some time that extracts of decoctions of certain plants such as coffee, tea, cocoa and ginseng, both that coming from Korea and that coming from Manchuria in their different species, white or red, such as the so-called Siberian ginseng (
Eleoterococcus senticosus
), including the oral administration of the plant itself as found in nature or ground with some processing, have a characteristic tonic and stimulating effect which results in a general invigorating of the physical condition and a parallel stimulating action of mental activity, which, depending on the plant in question, is more or less pronounced, on some of the feelings of physical well-being and/or mental alertness which are produced with a greater and more substantial action depending on the vegetable species.
The duration and intensity of the stimulating effect on the central nervous system (CNS) can be obtained, both in the short term and in the long term, depending on the concentration of the extract or species of plant used and, in the final analysis, depending on the amount and combination of active principles which are contained in the plant.
The popular and in some cases medical use of these compounds in their different forms has been known for many years and there have also been known certain side effects which at times are undesirable which exist such as the insomnia produced in certain individuals by coffee, or in a certain degree of nervousness in some persons who are very sensitive to chocolate.
In each case, these effects are taken into account, which does not prevent the daily use of these products which have an undeniable popularity throughout the different areas of the world.
In some countries, coffee is used more in all its varieties, such as arabica or robusto, while in other countries tea, from green tea in Japan and China to the innumerable varieties of tea of India or Europe or Arabia, is used most.
Chocolate and cocoa derivatives are widely used in the Orient as stimulants of physical and psychic vigor.
There is extensive scientific literature, both chemical as well as pharmacological and medical, as well as traditional literature, which can illustrate what has been stated above, but we shall not make reference thereto due to the great length which such a bibliography would require.
We believe that there is a great need for a composition which can be administered as a beverage, which has a stimulating effect on the central nervous system, in particular, stimulating the memory and the cognitive activity, but which has fewer undesired side effects than those observed with the customary beverages of daily consumption. In other words, beverages which can potentiate the stimulating effect, but reduce the undesired effects.
The active ingredients which are responsible for the stimulating effects have in general been widely identified so that it is known that caffeine is one of the principal activators of the mental alertness and well-being produced by coffee or tea, and theobromine is responsible for the effect of cocoa and derivatives of chocolate.
The action found has been attributed to these xanthic bases, and even theophylline, which is very closely related to caffeine and theobromine, is a member of this basic xanthic structure which has closely related properties.
Furthermore, it has been seen that the compounds obtained by synthesis exhibit a large part of the properties of the natural extracts, the dosing of their administration being in some cases easier.
The ginsenocides responsible for the invigorating caused by the administration of ginseng in its various forms and formulations have also been identified.
It may even be said that there is a large scientific arsenal which explains and lists the active principles which are produced by synthesis or are found in nature, as well as their pharmacological activity.
Furthermore, the properties of the alkaloids of eburnamenine structure are known for their interesting effects on the cerebral circulation, the cerebral vascular resistance in the cerebral vessels and their activity of increasing cerebral metabolism, which can be quantified by the increase in the consumption of glucose by the nerve cells as well as its greater resistance to cerebral hypoxia. Among the alkaloids used in therapy which correspond to this group, we may mention vinpocetine, vincamine, bromovincamine, eburnamonine or vincamone, among others, which are used with great success in the treatment of the deterioration of the cognitive functions in cerebral vascular problems, which arise in general in persons of advanced age.
The inventors have recently encountered an unexpected result after the oral administration to healthy volunteers of different ages of these traditional beverages combined with the compounds of eburnamenine ring mentioned. This effect has been obtained and optimized by using different relative concentrations of the components, that is to say by effecting a gradation of the concentrations of the xanthic bases used and the eburnamenine ring derivatives in the case of coffee, cocoa or tea, or dosing the theophylline in the case of its use as component or else dosing the concentration of the natural ginsenocides or the concentrations of active principles of
Eleteorococus senticosus
in the case of the different ginseng extracts used.
This marked and unexpected powerful synergistic effect is obtained in all cases with the different concentrations or relative contents used in each case, and in this way there can be observed a possible adaptation of the optimum concentration to the individual need measured as response in mental alertness or in the increase in cognitive capacity or else in the extent of the reduction or absence of the undesired effects.
Also, by the present invention there can be obtained compositions which give rise to effects more in the short term or more in the long term, it being possible, therefore, to use these compositions in the form of beverages in a rational manner, stimulating the activi
Calvo Lazaro Elena
Calvo Lazaro Paula
Calvo Mondelo Fernando
Lazaro Flores Consuelo
Manresa Ferrero María Teresa
Decox, S.L.
Meller Mike
Naff David M.
Ostrolenk Faber Gerb & Soffen, LLP
LandOfFree
Beverage containing caffeine or theobromine and vinpocetine... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Beverage containing caffeine or theobromine and vinpocetine..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Beverage containing caffeine or theobromine and vinpocetine... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2446412