SOME ANTHELMINTIC PROPERTIES OF OCTYLCHLORORESORCINOL AGAINST ASCARIS LUMBRICOIDES IN MAN

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Among a series of highly effective alkylchlororesorcinols against Ascaris luinbricoidgs, effects of which were discovered in our laboratory in 1948/49 (1, 2, 3) as a result of systematic studies with the co-operation of Dr. Tomita and Dr. Uyeo (4, 5, 6) of the Pharmaceutical Institute of Kyoto University in the synthesis of these compounds, a member that proved lowest in toxicity as well as in local irritant action was 4-n-octyl-6-chlororesorcinol. Ashikaga (1) of our laboratory first studied clinical effects of this compound in 1949 and obtained satisfactory results, which, in due time, were confirmed by Hattori and his co-workers (7). For about a year after this there came forth no significant report on clinical studies of this compound. But, last year, reports by Hattori et al. (8) and by Inouye et al. (9) came out, and according to these reports, the efficacy of the compound seems to have suffered rather a severe diminution. Not only that but also, we too have discovered, after having examined two kinds of tablets of this compound prepared by a pharmaceutical Co., that, to our surprise, there occurred a great deal of deterioration in its efficacy compared to earlier data. Whereupon, we again examined the efficacy of three samples of crystalline octylchlororesorcinol that were synthetized since its first trial and found every one of them to be unsatisfactory. In order to know to what causes this change could be ascribed, we decided to launch our researches in the following two directions: Firstly, to find out if any drug-resistance against this compound had been developed on the part of Ascaris under the recent circumstances in which hexylresorcinol became so popular and widely used, and secondly, to re-investigate the problems concerned with the purity of the compound. On the first point, however, recent Mannami's investigations (10) of actual cases revealed no convincing evidence of manifestations of drug-resistance that would explain the above-mentioned change in the efficacy. In respect to the second point, however, the analysis performed by Tomita et al. of Kyoto University showed, oddly enough, that the one lower in efficacy to be the purer. Puzzled by these findings, we finally asked there for a new sample of this drug to be prepared under the same condition as when we received it for the first time. The newly prepared crystals, when tested, proved to be much more efficacious than the other low-efficacy crystals, though the former had lower melting point than the latter. Confronted with these facts, it became necessary for the authors to clarify as to what difference or differences in the properties of these two samples, which are supposed to be alike, the distinct difference in the behavior of these samples could be attributed. In this paper, the authors tried to solve the problem by studying if there is any difference in the physical and chemical properties of all samples of octylchlororesorcinol that have been used in the clinical investigations and by comparing pharmacologic properties of the low-efficacy crystals with those of the newly prepared efficacious crystals.
公益社団法人日本薬理学会の論文

SOME ANTHELMINTIC PROPERTIES OF OCTYLCHLORORESORCINOL AGAINST ASCARIS LUMBRICOIDES IN MAN

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