Metabolic Fate of YM866, a Novel Fibrinolytic Agent (III). Feto-placental Transfer and Excretion into Milk in Rats.

Oikawa, Keishi; Kamimura, Hidetaka; Watanabe, Takashi; Higuchi, Saburo; Kurosawa, Satoshi; Jin, Yoshitaka; Tsutsumi, Shuichiro; Hayashi, Kazushi; Takekoshi, Toshio

doi:10.2133/dmpk.11.30

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“…Similar results were reported for other radioiodinated proteins -[ 1251]-granulocyte colony stimulating factor (5), calcitonin (6) and e 25 1]-tissue plasminogen activator (7). The radioactivity in TCA precipitates from milk was 25-40% of the total radioactivity.…”

Section: Discussionsupporting

confidence: 84%

Pharmacokinetics of [125I]-recombinant human interleukin-11:

Uchida¹,

Aoyama²,

Mori³

et al. 1998

Eur. J. Drug Metab. Pharmacokinet.

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Placental transfer and excretion into milk of [125I]-rhIL-11 (recombinant human interleukin-11) after subcutaneous administration in female rats were investigated. After administration of [125I]-rhIL-11 to rats on the 14th day of gestation, radioactivity in the kidney was the highest among excised tissues, being 3 times higher than that in the plasma at 1.5 h. Radioactivity in other tissues, including the mammary gland, ovary, uterus, placenta and amniotic fluid, was lower than that in the plasma. Although radioactivity in fetuses was detected 6 h after administration, the level was only 2% of the plasma concentration in dams, and the radioactivity was not found in fetal-derived TCA precipitates. These results indicate that rhIL-11 does not readily pass through the placenta into the fetus. After subcutaneous administration of [125I]-rhIL-11 to lactating rats 14 days after delivery, radioactivity in milk was 1.1-1.6 times that in the plasma of dams. Radioactivity in clotted milk in the stomachs of suckling infants was almost equal to that in the dam's milk; however, only a small amount of radioactivity was detected in infant kidneys.

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Section: Discussionsupporting

confidence: 84%