Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-03-27
1999-09-14
Lee, Howard C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514557, 514629, 514669, 514738, 514867, A61K 31195, A61K 3116, A61K 31045
Patent
active
059523808
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an agent for preventing and treating diarrhea, and particularly to a pharmaceutical agent for preventing and treating a diarrheic symptom caused by administration of cancer chemotherapeutics.
BACKGROUND ART
Diarrhea often develops as a side-effect disorder during the clinical treatment course by pharmacotherapy, whose typical symptom is characterized by the frequent defecation of liquid or liquid-like stools. In particular, the diarrhea due to the administration of cancer chemotherapeutics is often so serious that most patients with such a diarrhea symptom are no longer allowed to receive the further continuous treatment. Furthermore, this diarrhea endangers the patient's physical strength and nourishment, leading to slowing down the recovery pace from leukopenia, thrombocytopenia and the like, symptoms caused by administration of cancer chemotherapeutics.
There are already various chemotherapeutics widely used, for example, antimetabolites, such as 5-fluorouracil and derivatives thereof such as 5-fluorouracil, doxifluridine and tegafur, 5-fluorouridine, and methotrexate, compounds derived from plants, such as camptothecin, etoposide and vincristin sulfate, alkylating agents such as cyclophosphamide, anticancer antibiotics such as adriamycin and mitomycin C, cisplatin, and carboplatin, but these chemotherapeutics are known to commonly cause the foregoing diarrhea when used. In particular, this side effect is serious in the cases that its onset has been caused by, in particular, the continuous intravenous drip infusion of 5-fluorouracil or the administration of 5-fluorodeoxyuridine, doxifluridine, tegafur, cyclophosphamide, vincristine sulfate or irinotecan. So far, little is known about the detailed mechanism of diarrhea development. However, as far as cancer chemotherapeutics are concerned, it is speculated that diarrhea might be influenced pathologically by factors such as a direct affection to digestive tract mucosa, namely, chemical changes of mucosal cells, and further changes of enterobacterial flora. Yet there has been no established effective means for improving diarrheric symptom due to cancer chemotherapy, though effort is continued by some attempts such as alleviation of the diarrhea by changes in the usage and dose of cancer chemotherapeutics, improvement in their preparations, modification and conversion of compounds.
However, none of such attempts have seen sufficient improvement against the foregoing diarrhea symptoms as yet. Thus, there is growing demand for development of an agent for preventing and treating diarrhea, which has higher safety and stronger efficacy.
As described above, the present state is such that there are not yet any efficacious and safe agents for preventing and treating diarrhea, specifically a pharmaceutical agent for alleviating diarrhea due to cancer chemotherapy. It is therefore an object of the present invention to provide an excellent agent for preventing and treating diarrhea.
The present inventors have thus carried out an extensive investigation. As a result, it has been found that conagenin or a salt thereof is efficacious against various diarrheic symptoms, in particular, a diarrheic symptom due to cancer chemotherapy, thus leading to completion of the present invention.
DISCLOSURE OF THE INVENTION
Namely, the present invention is directed to an agent for preventing and treating diarrhea, comprising conagenin or a salt thereof as an active ingredient.
The present invention is also directed to use of conagenin or a salt thereof for the preparation of an agent for preventing and treating diarrhea.
The present invention is further directed to a method of preventing and treating diarrhea, which comprises administering an effective amount of conagenin or a salt thereof to a patient with diarrhea.
BEST MODE FOR CARRYING OUT THE INVENTION
Conagenin is a compound represented by the following structural formula, R)2,4-dihydroxy-3-methyl-pentanoyl!-2-methylserine" in nomenclature. ##STR1##
Conagenin has been al
REFERENCES:
patent: 5098935 (1992-03-01), Ishizuka et al.
patent: 5447719 (1995-09-01), Kamataki
Ishizuka Masaaki
Maeda Kenji
Shiraishi Tadayoshi
Takeuchi Tomio
Toko Toshiyuki
Kanegafuchi Kagaku Kogyo & Kabushiki Kaisha
Lee Howard C.
Taino Pharmaceutical Co., Ltd.
Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
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