Studies on the Metabolic Fate of Neticonazole. (II): Transfer into the Fetus and Milk, and Absorption, Distribution, Metabolism and Excretion in Rats after Repeated Administration.

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  • YANO Kenichi
    Research and Development Hedquarters, SS Pharmaceutical Co., Ltd.
  • KOZANO Hajime
    Research and Development Hedquarters, SS Pharmaceutical Co., Ltd.
  • NUMATA Hiroshi
    Research and Development Hedquarters, SS Pharmaceutical Co., Ltd.
  • ESUMI Yoshio
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • MITSUGI Kouichi
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • OOYAMA Toshihiro
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • WATANABE Isao
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • WADA Reiko
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • YATABE Naomi
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • UEDA Takao
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.
  • SUGAI Saburo
    Tokai Research Laboratories. Daiichi Pure Chemicals Co., Ltd.

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  • Ｎｅｔｉｃｏｎａｚｏｌｅの体内動態　（第２報）：　ラットにおける胎仔，乳汁移行性および反復投与試験

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Transfer of 14C-neticonazole (14C-SS717) into the fetus and milk were studied in pregnant or lactating rats after subcutaneous administration, while the absorption, distribution, meta-bolism and excretion of 14C-SS717 were studied in male rats after repeated administration.<BR> 1. On day 13 and 18 of gestation, the radioactivity in the fetus was lower than that in the maternal blood as revealed by autoradigraphy. The distribution of radioactivity into the fetus was nearly uniform and any significant distribution to any tissue of fetus was not observed. The maximum level of radioactivity in the fetus was reached at 4hr after dosing and was lower than the maternal plasma level.<BR>2. Milk levels of the radioactivity in lactating rats were 1.5 ?? 1.7 times higher than that found in the plasma until 8hr after dosing. However, the milk level of radioactivity at 24hr after dosing was same as plasma level, and was not detected at 48hr after dosing.<BR>3. During the multiple dosing, the blood radioactivity level at 24hr after each dosing in-creased constantly with number of dosing and after the 21st dosing it was 3.8 times higher than that after the first dosing.<BR>4. The cumulative excretion of radioactivity within 120hr after the 21st dosing accounted for 64.0 and 32.6% of administered dose in the urine and feces, respectively.<BR>5. In the most of tissues examined, the concentrations of radioactivity reached the steady state within the 21st dosing. However, the accumulation of radioactivity was observed in aorta and skin. The disappearance of radioactivity from tissues after the 21st dosing was relatively slow.<BR>6. In the plasma after the 21st dosing, the unchanged drug and U-2 metabolite, while in the urine U-2, U-5 and U-6 metabolites were detected as a major components.

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