Antimalarial drug

Details Antimalarial drug Antimalarial drug

1995-09-07

1998-07-14

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 55, 514 56, 514 58, A61K 31715, A61K 3173, A61K 31725

Patent

active

057804524

DESCRIPTION:

BRIEF SUMMARY
(TECHNICAL FIELD)

This invention relates to an antimalarial drug which comprises a sulfated polysaccharide as an active ingredient and another antimalarial drug which comprises quine in addition to a sulfated polysaccharide.


(BACKGROUND ART)

Malaria is a disease caused by plasmodia or malaria parasites, and quinine, chloroquine, primaquine and the like are currently used as typical therapeutic drugs, which, however, are not always sufficiently effective because of the generation of resistant parasites against these drugs. Also, it is known that sulfated polysaccharide are possessed of an anti-blood coagulation activity, an antiretroviral activity (Japanese Patent Application Laid-Open (Kokai) No. Sho 62-215529) and the like.
In such prior art background, it is an object of the present invention to provide a new antimalarial drug which has higher therapeutic effect.


(DISCLOSURE OF THE INVENTION)

With the aim of resolving the aforementioned problems, the inventors of the present invention have conducted intensive studies and found as the result that a sulfated polysaccharide has an antimalarial activity and that joint use of the sulfated polysaccharide and quinine exerts synergistic effect on the antimalarial activity. The present invention has been accomplished on the basis of these findings.
Accordingly, the present invention relates to an antimalarial drug which comprises a sulfated polysaccharide or a pharmaceutically acceptable salt thereof as an active ingredient and to another antimalarial drug similar to the above drug which further comprises quinine as another active ingredient.
Firstly, the former one, namely an antimalarial drug which comprises a sulfated polysaccharide or a pharmaceutically acceptable salt thereof as an active ingredient, will be described.
Examples of the sulfated polysaccharide to be used as an active ingredient of the antimalarial drug of the present invention include synthetic or natural sulfated polysaccharide such as sulfated curdlan, dextrin sulfate, chondroitin sulfate, heparin, carrageenan and the like. Of these, sulfated curdlan is preferred because it is weak in anticoagulation activity as a side effect. The sulfated polysaccharide having a sulfur content of from 5 to 25% by weight, preferably from 10 to 20% by weight, and most preferably from 12 to 17% by weight, and a weight average molecular weight of from 5,000 to 500,000, preferably from 20,000 to 200,000, and most preferably from 50,000 to 120,000, when measured by the gel filtration method (GPC), are preferably used.
Examples of the pharmaceutically acceptable salts of the sulfated polysaccharide include inorganic salts such as sodium salt, potassium salt, calcium salt, magnesium salt and the like.
The antimalarial drug of the present invention can be made into optional dosage forms such as injections, drippings, suppositories and the like with no particular limitation.
Preparation of the active ingredient of the present invention into a pharmaceutical drug can be made in the usual way, also with no particular limitation, making use of fillers or carriers such as lactose, glucose, mannitol, maltose, amino acids, gelatin, distilled water, ethanol and the like.
Dose of the antimalarial drug of the present invention varies depending on the age, body weight and symptoms of each patient and its administration method, and is generally from 1 to 1,000 mg/kg weight.multidot.day, preferably from 10 to 500 mg/kg weight.multidot.day, in terms of the active ingredient. The antimalarial drug of the present invention can be administered continuously or repeatedly.
The antimalarial drug of the present invention exerts its antimalarial effect when administered before or after malarial infection.
Next, the latter one, namely an antimalarial drug which comprises a sulfated polysaccharide or a pharmaceutically acceptable salt thereof and quinine as active ingredients, will be described.
As described in the foregoing, according to the findings of the present inventors, a sulfated polysaccharide and quinine exert synergistic

REFERENCES:
patent: 5512672 (1996-04-01), Yamamoto et al.
Transactions of the Royal Society of Tropical Medicine and Hygiene, vol. 88, No. 6, pp. 686-687, Nov. 1994, Ivan Havlik et al., "The Effect of Curdlan Sulphate On In Vitro Growth of Plasmodium Falciparum".
Biochemical Parmacology, vol. 39, No. 4 (1990), pp. 793-797.

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