Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1991-12-06
1995-07-18
Griffin, Ronald W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 23, 514824, 536 2, A61K 3170, A61K 31725
Patent
active
054341418
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The invention relates to a medicament which can be administered orally for the treatment and prophylaxis of metabolic disorders, especially to influence lipid and cholesterol metabolism, that is to say hyperlipidaemia and atherosclerosis.
In Western industrialised countries there has for some time been observed to be a rapid increase in metabolic disorders, especially disorders of lipid metabolism, whose main cause is overeating with, at the same time, lack of exercise. There is gradual development of elevated blood levels of particular lipids which increase the risk of atherosclerotic cardiac and peripheral vascular diseases. In this connection, the lipids are transported in the circulation in the form of very small droplets (chylomicrons) which are stabilised by a protein film (.alpha.- or .beta.-globulin).
The heavy consumption of meat often results in a surplus of cholesterol because this steroid is already biosynthesised in adequate quantity in the human liver. The natural mechanism of regulation of the cholesterol level is impaired when the diet is rich in lipids, and the result is a permanent elevation of plasma cholesterol. Sparingly soluble cholesterol is deposited, inter alia, in the lining of the aorta, in the cornea and in the lens of the eye. Elevated blood cholesterol levels are at least partly responsible for the development of arterial angioscleroses. Hypercholesterolaemia is a metabolic disorder which always accompanies hyperlipidaemia and which may be very pronounced, for example, in cases of diabetes mellitus.
The clinical pictures, which differ in pathogenesis but have similar symptoms, of hypertriglyceridaemia=hyperlipidaemia, that is to say the turbidity of the blood serum owing to chylomicrons (droplets which are rich in neutral fats and have a diameter of up to 1 nm) and hypercholesterolaemia, that is to say elevation of the cholesterol content in the blood plasma to above 200 mg are comprised by the collective terms hyperlipoproteinaemia and hyperlipidaemia respectively (compare Pschyrembel, Klin. Worterbuch).
Used to date for the therapy of hyperlipoproteinaemia are mainly ethyl .alpha.-(p-chlorophenoxy)isobutyrate, salts of .alpha.-(p-chlorophenoxy)isobutyric acid and nicotinic acid, and nicotinic acid derivatives, synthetic anion exchanger resins and numerous combination products.
The synthetic anion exchanger resins often lead, because of their chemical and physical properties, to considerable gastrointestinal symptoms. They may, because of their anion-exchanging properties, have an adverse influence on the absorption of other medicaments and of natural minerals.
Plant-based medicaments which can be employed for the treatment of the said metabolic disorders have not hitherto been disclosed. It has now been found, surprisingly, that galacturonic acid has a hypocholesterolaemic action. The experiments described hereinafter demonstrated that intake of galacturonic acid or certain derivatives of this acid results in a distinct lowering of serum cholesterol, that is to say that this compound or compound class is very suitable for the treatment of hyperlipidaemia and atherosclerosis. Thus the invention is, in the first place, directed at the use of galacturonic acid, especially of .alpha.-D-galacturonic acid of the general formula ##STR1## where R.sub.1 =H, hyperlipidaemia and/or atherosclerosis.
The invention additionally relates to the use of polymers of galacturonic acid, especially of .alpha.-D-galacturonic acid of the general formula ##STR2## where R.sub.1 =H
The invention also includes the use of methyl esters of galacturonic acid and polymers thereof, especially of .alpha.-D-galacturonic acid for the purpose indicated in claim 1,
The scope of the invention also covers the use for the purpose indicated in claim 1 of esters, ethers and/or acetals, containing tertiary or quaternary amine anion exchangers, of galacturonic acid, especially of .alpha.-D-galacturonic acid and polymers thereof, where in the case of the esters ##STR3## the amine anion exchangers in the gen
REFERENCES:
patent: 2370961 (1945-03-01), Hollander
patent: 4122179 (1978-10-01), Vegezzi
patent: 4615891 (1986-10-01), Nocek et al.
patent: 4617276 (1986-10-01), Nocek
Schafer Hans-Ludwig
Schneider Werner
Griffin Ronald W.
Steigerwald Arzneimittelwerk GmbH
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