JPS61129122A - Antitumor agent consisiting of anthranilic acid - Google Patents

Abstract

PURPOSE:An antitumor agent having effects on reduction i n number of tumor cells, inhibitory ratio of tumor cells, prolongation of life, inhibition of tumor multiplication, etc. in tumor of animal and human, containing an anthranilic acid derivative as an active ingredient. CONSTITUTION:An antitumor agent containing an anthranilic acid derivative shown by the formula (R is C, or N) or its salt as an active ingredient. When it is used, it is used in powder, fine granule, granule as oral administration, in ampule of injection, bottle, etc. as parenteral administration, and suppository, ointment, etc. may be used. An amount of the active ingredient is generally 0.01-100wt%., preferably 0.05-80wt% in the composition. a dose is preferably 0.5-500mg/kg daily in case of human.

Description

DETAILED DESCRIPTION OF THE INVENTION The present application relates to an antitumor agent, specifically an antitumor agent containing a substance represented by general formula (I).

The present inventors, in their research for the development of antitumor agents, discovered that the use of a substance represented by the general formula (I>) against tumors has an antitumor effect, and completed the present application.

The substance used in this application has the general formula (1) = (where R is C
or N) or its salt (hereinafter referred to as the present substance).

The substance in question is Medical Drugs of Japan, 7th edition, 743-74.
4 pages, 1983, Yakugyo Jihosha, Recent New Drugs, Volume 33,
Also included are substances that have known anti-inflammatory effects and are described in Yakuji Nipposha, 1982, p. 267. Its safety has also been fully confirmed.

This substance is effective against animal or human tumors. The effectiveness of this substance was determined by confirming its effectiveness in reducing the number of tumor cells, suppressing tumor growth, etc.

When this substance is used as an antitumor agent, it can be used in a form convenient for obtaining medicinal efficacy depending on the symptoms. It may be used alone or in combination with pharmaceutically acceptable diluents and other agents.

The materials can be presented in dosage unit form containing an effective dosage of the active ingredient. Its forms include suspension, liquid,
Emulsions, etc. For parenteral use, it can be in the form of ampoules or bottles as injection solutions. Suppositories and ointments are also available. The diluent may be solid, liquid, or semi-solid, and examples include the following. That is, excipients, fillers, binders, wetting agents, disintegrants, surfactants, lubricants, dispersants, buffers, fragrances, preservatives, solubilizing agents, solvents, and the like.

In the compositions used in the present invention, the active ingredient is generally present in an amount of 0.01 to 100% by weight, preferably 0.05 to 80% by weight.

The substance is administered orally or parenterally to humans and animals. Oral administration includes sublingual administration.

Parenteral administration includes injection administration (eg, subcutaneous, intramuscular, intravenous injection, infusion), rectal administration, and the like. Alternatively, it may be applied.

This substance is affected by whether the subject is an animal or a human, as well as by age, individual differences, medical conditions, etc. Therefore, in some cases, doses outside the range shown below may be administered, but in general, when administering to humans, The dosage of the substance is 0.1-110 per day
00I1/Kg, preferably 0.5-500ay/Kg
It is.

It may be administered in 2 to 4 divided doses.

Example 1 Antitumor effect against Sarcoma-180 Sarco
1 x 106 ma-180 cells were transplanted subcutaneously into the lower axilla of ICR-JCL mice, and once every other day starting 24 hours after transplantation.
On the 0th occasion, the present substance (R-C, Aρ salt) dissolved or suspended in a 0.5% CMG solution was orally administered at 50'O/. Tumor nodules were excised on the 25th day after transplantation, and the growth inhibition rate ([, R, %) was calculated using the following formula.

(1-T/C)x100=1. R, (%) T: Administration group average tumor weight C: Control group average tumor weight 10 animals were used per group, and the average value was used.

The growth inhibition rate was 43.6%. This thing's LD5o
is 1.497 to 9 in mice orally.

Example 2 Antitumor effect against Ehrlich cancer [CR
- 2 x 106 Ehrlich cancer cells were intraperitoneally transplanted into JCL mice, and 14 times daily starting 24 hours after transplantation,
．． This substance dissolved or suspended in 5% CMC solution (
RN) 500II1 g/Ng was orally administered. On the 14th day after transplantation, the rats were sacrificed, and the ascites fluid was collected and the number of septal cells in the ascites was measured.

The average value was calculated from 10 animals per group. The control group was 18.3.
The number of Ehrlich cancer cells in the ascites was 11.0×107 cells/d in the group administered with the substance of the present invention.

Formulation Example 250 Rg of this substance (R=N) was placed in a capsule to prepare a capsule.

Claims (2)

[Claims] (1) General formula (I): ▲There are mathematical formulas, chemical formulas, tables, etc.▼(I) (where R is C or N) Tumor agents. (2) The antitumor agent according to claim 1, wherein R is C and is an Al salt.