Ganglioside containing compositions for treating diarrhea

Details Ganglioside containing compositions for treating diarrhea Ganglioside containing compositions for treating diarrhea

1980-11-13

1982-08-31

Rosen, Sam

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

A61K 3170

Patent

active

043472443

DESCRIPTION:

BRIEF SUMMARY
The present invention concerns a new medicine and the pharmaceutical compositions containing it.
More specifically, the invention concerns a new medicine making it possible to treat prophylactically or curatively acute diarrhea, and in particular cholera.
The medicine of the invention is characterized by the fact that it consists of a medium onto which is fixed a ganglioside or ganglioside derivative having an affinity for the toxins produced by the bacteria responsible for diarrhea and in particular for the choleraic toxin, said medium being compatible with oral administration.
The usable media are all those which are compatible with oral use, having a strong and preferably irreversible affinity for the gangliosides or which can be chemically linked with the gangliosides. They should preferably have a high specific surface (use of porous media). They must also allow satisfactory contact between the ganglioside and the toxins to be neutralized.
The media are chosen for example from the group consisting of: activated carbon, latex, polysaccharides such as cellulose, modified or not, and porous mineral media such as silica, alumina, titanium oxide, or their natural or synthetic derivatives such as glass, silicates, kaolin, etc., possibly bearing polysaccharides.
Preferably, the medium is pharmaceutical-quality activated carbon, and in particular carbon marketed under the name ACTI-CARBONE WL 3S.
Generally speaking, all pharmaceutical-quality carbons are suitable.
It is known that among the various gangliosides the G.sub.M1 ganglioside and certain of its derivatives have a strong and specific biochemical affinity for choleraic toxins and structurally related toxins. This affinity is also observed with certain derivatives of the G.sub.M1 ganglioside. This is in particular the case with the G.sub.M1 lysoganglioside. The G.sub.M1 lysoganglioside is obtained by alkaline hydrolysis of the G.sub.M1 ganglioside according to the process described by HOLMGREN, MASSON and SVENNER-HOLM, Medical Biology (1974), 52, 229-233. This alkaline hydrolysis is aimed at transforming the two N-acetyl functions and the N-actyl function of the G.sub.M1 ganglioside into an NH.sub.2 amine function.
Other ganglioside derivatives also have an affinity for the choleraic toxin.
In the present application, by convention "derivative of the G.sub.M1 ganglioside" or "G.sub.M1 " will designate any ganglioside derivative which has an affinity for the choleraic toxin, and in particular the products resulting from a partial or total hydrolysis of the N-acyl or N-acetyl groupings into NH.sub.2 groupings of the G.sub.M1 ganglioside, but also the mono- or a-sialo-gangliosides resulting from the acid treatment of the gangliosides or their derivatives (in particular their derivatives resulting from total or partial hydrolysis of the N-actyl or N-acetyl groupings).
The products of partial de-acylation of the gangliosides have free-amine groupings which can be brought to light by a positive reaction in the ninhydrine test and are mobile in chromatography on a thin layer of silica gel in the chloroform-methanol-water system (60:32:7), and have the specific affinity properties of the gangliosides from which they derive. They maintain these properties of affinity even if they are coupled to solid media by means of the amine groupings appearing upon partial deacylation.
They are prepared by treatment of the gangliosides with a basic aqueous solution at a temperature between 0.degree. and 120.degree. C., said temperature being lower as the medium is more basic. For a final solution with alkalinity comparable to normal soda or potassium, it is important not to exceed 100.degree. C. For an alkalinity comparable to deci-normal soda or potassium, it is important not to exceed 120.degree. C.
The reaction time must be sufficient for the appearance of free-amine groupings, but the reaction must be halted before total de-acylation. The reaction time can be easily determined in each case by simple experimentation, using for example the ninhydrine test, seeking an inte

REFERENCES:
patent: 3101299 (1963-08-01), Ferrand
patent: 3400197 (1968-09-01), Lippmann
patent: 3627885 (1971-12-01), Rondelet
Tayot et al.-Chem. Abst., vol. 90 (1979), p. 81812z (original article pub. 1978).

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