Drug – bio-affecting and body treating compositions – Whole live micro-organism – cell – or virus containing – Fungus
Reexamination Certificate
2000-12-15
2001-10-23
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Whole live micro-organism, cell, or virus containing
Fungus
C514S002600, C514S556000, C514S561000, C514S562000
Reexamination Certificate
active
06306392
ABSTRACT:
This is a 371 of PCT/IT00/00129 filed Apr. 17, 2000.
The present invention relates to a composition for the prevention and/or treatment of alterations of those organs which perform the most intense metabolic function, such as the liver, kidneys, cardiovascular system and brain.
More particularly, such composition is useful to treat or prevent hepatosis, nephropathies and cardiovascular or cerebral damages such as damages provoked by ageing or due to an altered metabolism of such organs or provoked by toxic substances.
Accordingly, the composition may take the form and exert the action of a dietary supplement or of an actual medicine, depending upon the support or preventive action, or the strictly therapeutic action, which the composition is intended to exert in relation to the particular individuals it is to be used in.
More particularly the present invention relates to an orally, parenterally, rectally, or transdermally administrable composition which comprises in combination:
(a) propionyl L-carnitine or a pharmacologically acceptable salt thereof, optionally in combination with another “carnitine”, where for “carnitine” is intended L-carnitine or an alkanoyl L-carnitine selected from the group comprising acetyl L-carnitine, valeryl L-carnitine and isovaleryl L-carnitine or their pharmacologically acceptable salts; and
(b) glutathione or glutathione-containing yeast;
(c) a glutathione-free yeast if the component (b) consists of glutathione.
Glutathione (GSH), N-(N-L-L-&ggr;-glutamyl-cysteinyl) glycine, plays an essential role in the organic redox and detoxification reactions. Glutathione is synthesised in the body starting from glutamic acid and cysteine which, in the presence of ATP, form &ggr;-glutamyl-cysteine, which, again in the presence of ATP, reacts with glycine giving rise to the formation of glutathione. Glutathione is ubiquitously present in the body. Its greatest concentrations, however, are to be found in the liver, heart and brain, i.e. in those organs where the metabolic, energy and detoxification reactions are more important. These tissues also contain glutathione peroxidase and glutathione reductase, which regulate the redox system related to the glutathione cycle, ensuring maintenance of sufficient amounts of reduced glutathione after the latter has been oxidised.
Though the biochemical and detoxifying activities of glutathione have long been known, particularly against heavy metals (which are among the most important environmental pollutants) or against liver-damaging drugs such as paracetamol, only the most recent researches have revealed the predominant role of glutathione among the various redox systems, as well as its specific pharmacological role. A direct involvement of glutathione in exerting a protective effect against the formation of atheromatous plaques has been observed by directly measuring the presence of the glutathione-related antioxidant/prooxidant system in such plaques. These researches revealed low concentrations of glutathione and fairly poor activity of the glutathione-related redox system. There was a particularly marked reduction in the glutathione peroxidase concentration and at the same time an increase in the concentration of oxidising factors. These abnormalities are not evident, however, in normal vascular tissue.
Glutathione also plays a major protective role in diseases of the liver. Moreover, the liver-protecting effects of many drugs are mediated by glutathione. It has also been reported that increased glutathione may reduce liver transplant rejection.
At the neurocerebral level, too, the role of glutathione distinguishes itself from that of the other better known redox systems in affording protection against the tissue and cell damage detected during ageing, in Parkinson's disease, or in Alzheimer's disease. At the cerebral level, in fact, glutathione is capable of playing various roles, and particularly that of a possible neurotransmitter. A deficiency of glutathione may increase the levels of cytotoxic substances and trigger the apoptosis of distinct sets of neuronal cells.
During ageing an increase in oxidative processes is observed and a reduction in natural antioxidant substances, including most notably glutathione, with the result that glutathione deficiency may be regarded as one of the causes of ageing. The favourable role of glutathione can also be observed at the intestinal level where its presence affects the formation of hydroperoxides and lipid peroxides, performing an important function of intestinal detoxification and in preventing the associated liver and bowel diseases.
L-carnitine and its alkanoyl derivatives are well known for the important role they may play at the metabolic level, particularly with regard to the oxidation and utilisation of fatty acids through &bgr;-oxidation.
L-carnitine, in fact, whether ingested with the diet or synthesised by the body, is concentrated by the blood in the organs which are metabolically most active in the utilisation of fatty acids, such as the skeletal muscles and heart.
An L-carnitine deficiency may be the cause of myopathy, whereas the oral administration of L-carnitine improves the clinical state associated with such diseases. L-carnitine also performs an important function in the mitochondrial oxidation of glucose in terms of energy production, with the result that adequate levels of L-carnitine are necessary for normal energy metabolism at the cardiac and muscular levels.
Its administration improves resistance to stress in subjects suffering from coronary insufficiency, as well as enhancing coronary flow, producing an improvement in the clinical effects of cardiac decompensation.
Other biological properties of L-carnitine and its alkanoyl derivatives, particularly of propionyl L-carnitine, are its ability to stabilise the cell membranes and protect them against the lesions induced by oxidative processes.
It has now surprisingly been found that a combination composition comprising as active ingredients:
(a) propionyl L-carnitine or one of its pharmacologically acceptable salts;
(b) glutathione or a glutathione-containing yeast;
(c) a glutathione-free yeast if the component (b) consists of glutathione; is extremely effective in the prevention and/or treatment of abnormalities of the metabolically most active organs such as the liver, kidneys, cardiovascular system and brain, both as a result of the potent synergistic effect exerted by its components and as a result of their increased tissue uptake, particularly of glutathione. Such a composition is particularly useful for the prevention or treatment of liver disease, kidney disease and cardiovascular or cerebral damage, such as, for instance, that produced by ageing, whether due to impaired metabolism of the above-mentioned organs or to toxic substances.
It has also been found that, advantageously, component (a) may further comprise another “carnitine”, selected from the group comprising acetyl L-carnitine, valeryl L-carnitine and isovaleryl L-carnitine, or their pharmacologically acceptable salts or mixture thereof.
When component (a) of the composition consists of a mixture of carnitines, a mixture of L-carnitine, acetyl L-carnitine and propionyl L-carnitine or the pharmacologically acceptable salts thereof, is preferred.
When component (b) consists of glutathione, component (c) will then consist of a glutathione-free yeast, selected from the group comprising
Saccharomyces cerevisiae
and
Saccharomyces fragilis.
Other examples of such yeasts are well known to experts in the field.
When component (b) consists of a glutathione-containing yeast, the yeast should preferably contain from 7 to 10% of glutathione by weight. A non-limiting example of a suitable glutathione-containing yeast is the YH—Torula Yeast extract (
Candida utilis
) produced by Kohjin, Japan.
The (a):(b):(c) weight-to-weight ratio ranges from 100:1:100 to 1:10:10 and preferably from 10:1:10 to 1:1:1.
It has also been proved that both the synergistic effect and the tissue uptake are further increased when the composition also contai
Henley III Raymond
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
Sigma-Tau HealthScience S.p.A.
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