Pharmacokinetic studies of 1.ALPHA.,24(R)-(OH)2D3(TV-02)(4). Plasma level, foeto-placental transfer and excretion into milk after subcutaneous administration to female rats.
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<SUB>3</SUB>H-TV-02([1β-<SUP>3</SUP>H]-1α, 24(R)-(OH)<SUB>2</SUB>D<SUB>3</SUB>)was given to non-pregnant, pregnant and lacting rats by a single subcutaneous administration (0.4μg/kg).<BR>1. Plasma profiles : Plasma levels of the radioactivity in lipid extracts and unchanged TV-02 reached the maxima after 2hr, then was eliminated in two -phasic fashion. 1α, 24(R)25-(OH)<SUB>3</SUB>D<SUB>3</SUB> was detected as a main metabolite in plasma.<BR>2. Foeto-placental transfer : The radioactivity in lipid extracts from the fetus on the day 19 was nearly equal to that on the day 14 of gestation.<BR>The concentration of radioactivity (lipid extracts) in the fetus was much lo wer than that in maternal plasma or placenta.<BR>3. Excretion into milk : The radioactivity was detected in lipid extracts from the milk, and milk/plasma concentration ratios were less than 1 within 8hr.<BR>The concentration of unchange TV-02 in the milk was 0.07-0.19 times lower than that in the maternal plasma.
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