Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-12-28
1996-06-25
Killos, Paul J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514274, 25218212, A01N 4354
Patent
active
055300030
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
This application is a 371 of PCT/JP93/00587 filed Apr. 30, 1993.
TECHNICAL FIELD
The present invention relates to a novel pharmaceutical composition for curing rheumatism.
BACKGROUND ART
Chronic articular rheumatism is a chronic systemic inflammatory disease involved mainly with the joints and patients with rheumatism suffer from the difficulties in daily life due to disorders of the functions of the joints.
Salicylic acid has been employed as medicine for curing rheumatism for a long time. Currently, there have extensively been employed sodium gold thiomalate, penicillamine, auranofin, lobenzarit 2Na, bucillamin, methotrexate (MTX), and so on. These medicine, however, cannot be said satisfactory, fox example, because they are low in the curing effects, short in pharmaceutical continuity, and they have some severe side effects.
DISCLOSURE OF INVENTION
The present invention has the object to provide a novel pharmaceutical composition for curing rheumatism having low in side effects, high in safety and superior in curing effects.
As a result of extensive research with the attempt to solve the problems inherent in such conventional compositions as described hereinabove, it has been found that 5-fluorouracil, employed currently as an anti-tumor agent, or an N-derivative thereof to be converted into 5-fluorouracil within the body, can exhibit a high degree of pharmaceutical activity as an agent for curing rheumatism. This invention has been completed on the basis of this finding.
The present invention provides a pharmaceutical composition for curing rheumatism containing, as an active ingredient, 5-fluorouracil or an N-derivative thereof to be converted into the 5-fluorouracil within the body.
The 5-fluorouracil (5-FU) to be employed as the active ingredient according to the present invention may be represented by the following general formula: ##STR1##
Further, the substance to be converted into the 5-fluorouracil within the body is an N-derivative of the 5-fluorouracil and there may be mentioned tegafur and doxyfurlysine as will be described hereinafter: ##STR2##
The 5-fluorouracil and the N-derivative thereof may be employed together with a modulator which may be employed when the 5-fluorouracil or its N-derivative is employed as an anti-tumor agent. Although, for example, methotrexate and leucovolin may be employed as a modulator, there may preferably be employed uracil as represented by the general formula: ##STR3## The rate of the uracil to be formulated may be approximately 4 moles per mole of the 5-fluorouracil or the N-derivative thereof.
The pharmaceutical composition for curing rheumatism according to the present invention may be administered in conventional manner, such as via an oral route or by injection. The daily dosage of the agent may range from 300 mg to 1,200 mg and it is preferred to administer the daily dosage three or four times.
The pharmaceutical composition for curing rheumatism according to the present invention is of a type novel and different from conventional ones and it can demonstrate the high extent of efficacy and long pharmaceutical continuity against chronic articular rheumatism, without showing any severe side effects.
BEST MODE FOR CARRYING OUT THE INVENTION
EXAMPLES
The present invention will be described more in detail by way of examples.
EXAMPLE 1
The following experiment was carried out by using a pharmaceutical agent (agent A) with tegafur and uracil formulated in the mole ratio of 1 to 4 (tegafur: uracil) and with only tegafur (agent B).
The agents A and B were tested for their ability of migration into the tissues on an adjuvant arthritis model.
Eight-week SD-type male rats (JCL) were subcutaneously injected in the paws of their right rear legs with a suspension of Mycobacterium butyricum in liquid paraffin (0.6 mg/0.1 ml; Difco). The rats with arthritis occurred in the 15th day were selected as test animals and each group consisting of eight rats was subjected to the test.
The test animals were orally administered with a solution or su
REFERENCES:
J. Sur. Res, 14[3] (1973) pp. 247-253.
Ann. Rheum Dis, 46 [10], (1987 Oct.) pp. 763-767.
Dott Limited Company
Killos Paul J.
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