Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from leguminosae
Reexamination Certificate
2002-05-07
2003-11-04
Lankford, Jr., Leon B. (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from leguminosae
C424S725000
Reexamination Certificate
active
06641849
ABSTRACT:
This application is the US national phase of international application PCT/IT00/00391 filed Oct. 2, 2000 which designated the U.S.
The present invention relates to a composition suitable for the prevention and/or treatment of circulatory disorders both at peripheral and cerebral level.
Correspondingly, the composition may take the form and exert the activity 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 according to the particular individuals for whom it is to be used.
More specifically, the composition according to the present invention comprises as characterising active ingredients:
(a) a carnitine selected from the group consisting of acetyl L-carnitine and propionyl L-carnitine or a pharmacologically acceptable salt thereof or mixtures thereof, and
(b) an extract of
Ginkgo biloba
or one or more of the ginkgolides isolated from
Ginkgo biloba
or mixtures thereof.
The biological and pharmacological properties of the carnitines at both the cardiac level and the vascular and cerebral energy level are very well known.
Both L-carnitine and, to different extents, its analogues such as acetyl L-carnitine and propionyl L-carnitine are capable of exerting a beneficial action both in myocardial insufficiency and in coronary disorders, as well as in peripheral vascular disorders.
These beneficial effects of the carnitines are due to the complex mechanism of action of these substances, relating particularly to the possibility of supplying energy to the various cell and tissue metabolic processes through activation of the metabolic systems of &bgr;-oxidation of fatty acids and of enhanced utilisation of glucose or through inhibition of lipid peroxidation processes and a reduction of free radicals.
Of particular interest would appear to be the interaction which L-carnitine and, above all, acetyl L-carnitine exert at the cerebral level.
It has been found, in fact, that acetyl L-carnitine after postischaemic reperfusion can restore the metabolism of the phosphorous-bearing derivatives and of glucose and in general, the cerebral function as well as being capable of preventing the more marked post-ischaemic neurological damages.
The same protective activity of acetyl L-carnitine has also been detected after stroke as well as in relation to the products of peroxidation.
These experimental findings underlie the beneficial clinical effects obtained with acetyl L-carnitine in the various phenomena related to cerebral ageing.
Ginkgo biloba
extracts also present a pharmacological and clinical activity characterised by a permanent beneficial action at the circulatory level and particularly at the cerebral circulatory level, with the result that significant results have been achieved with its use in the treatment and prevention of both peripheral and, above all, cerebral vascular insufficiency.
Ginkgo biloba
is a plant of the family Ginkgoaceae originally native to China and Japan, but now widespread throughout Europe and used for many years now in popular medicine as an anti-inflammatory, anti-asthma and anti-cough agent and, more recently, after isolating its active constituents, in a series of diseases characterised by circulatory insufficiency or by inflammatory or degenerative abnormalities induced by peroxidative phenomena, such as atherosclerosis, thrombosis or respiratory disorders.
The analyses carried out on the active constituents present in the leaves of
Ginkgo biloba
, particularly through gas-chromatography (HPLC) analysis, have revealed a multiplicity of chemically and pharmacologically differentiated substances, consisting most notably in the group of the flavonoids, benzoids, diterpenes and sesquiterpenes and in organic acids.
The flavonoids isolated include amentoflavone, bilobetin, isoginkgetin, sciadopitysin, ginkgetin, catechin and epicatechin, isoquercetin, iso-rhamnetol-3-0-rutinoside, kaempferol-3-0-rutinoside, kaempferol-7 -0-glucoside, syringetin-3-0-rutinoside, quercetin-3-0-rutinoside, luteolin, kaempferol, quercetin and myricetin.
The benzoids include gallocatechin and epigallocatechin. The diterpenes include ginkgolide A, ginkgolide B, ginkgolide C, ginkgolide J and ginkgolide M.
The sesquiterpenes include bilobalide, and the organic acids include 6-hydroxykinurenic acid, hydroxybenzoic acid, kinurenic acid, ascorbic acid and 3-methoxy-4-hydroxybenzoic acid.
Extensive reports in the literature have shown that all these compounds, both alone and in combination, are capable of exerting an antioxidant action, by scavenging free radicals, a vascular regulatory action and an anti-anoxic action, as well as modulating cerebral energy metabolism.
Most of the studies, especially the clinical trials, have been conducted not only on the compounds isolated from
Ginkgo biloba
extracts, but also on a standardised
Ginkgo biloba
extract containing 24% of glycoside flavonoids and 6% of terpene lactones.
The antioxidant activity of
Ginkgo biloba
extracts has been confirmed by experiments conducted both in vitro and in vivo. It has been observed in vitro that
Ginkgo biloba
extracts are capable of inhibiting the lipid peroxidation of the erythrocyte membranes induced by hydrogen peroxide as well as the peroxidation of the polyunsaturated fatty acids present in the membranes of the hepatic microsomes induced by ferrous ions. It has been observed in vivo that
Ginko biloba
extracts are capable of exerting a protective effect on spinal lesions induced by ischaemia and related to lipid peroxidation. Also very clearly demonstrated is the inhibitory activity of Ginkgo biloba extracts on platelet activating factor (PAF), which is a factor not only recognised as underlying platelet aggregation but also as being responsible for ischaemic circulatory disorders at both the cardiac and cerebral levels. The anti-ischaemic activity of
Ginkgo biloba
extracts has been confirmed in several clinical trials, and such extracts have also proved effective in preventing intermittent claudication and peripheral arteriopathy in general. Diseases related to erectile vascular disorders and tinnitus have shown improvement with the use of
Ginkgo biloba
extracts.
It is in cases of cerebral insufficiency of both vascular and degenerative origin, however, that the use of
Ginkgo biloba
extracts has yielded the most important results. Clinical experiments have demonstrated that the administration of
Ginkgo biloba
extracts is capable of having beneficial effects on senile dementia and on Alzheimer's disease, as well as upon depression, showing, in these studies, too, their superiority over drugs such as tacrine widely used in these conditions.
It has now been surprisingly found that a composition containing as its characterising active ingredients:
(a) a carnitine selected from the group consisting of acetyl L-carnitine and propionyl L-carnitine or a pharmacologically acceptable salt thereof or mixtures thereof, and
(b) an extract of
Ginkgo biloba
or one or more of the ginkgolides isolated from
Ginkgo biloba
or mixtures thereof
is particularly useful in the prevention and/or treatment of peripheral or central circulatory insufficiency at the myocardial, cerebral and peripheral vascular level, as well as of coronary disorders, nervous depression, insomnia, fatigue, intermittent claudication, tinnitus or penile erectile disorders, cerebral functional deficits, both vascular and metabolic, and articular or gastric inflammatory reactions.
The term “ginkgolides isolated from
Ginkgo biloba
” is meant to include ginkgolide A, ginkgolide B, ginkgolide C, ginkgolide J and ginkgolide M mentioned above.
The combination of acetyl L-carnitine or propionyl L-carnitine or a pharmacologically acceptable salt thereof or mixtures thereof with a
Ginkgo biloba
extract has been shown not only to exert a complementary effect of the two types of components, but also a real synergistic effect, revealing a reciprocal enhancement of their activity which may be extremely useful in achiev
Davis Ruth A.
Lankford , Jr. Leon B.
Nixon & Vanderhye P.C.
Sigma-Tau HealthScience S.p.A.
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