Pharmacokinetic studies of 1.ALPHA.,24(R)-(OH)2D3(TV-02)(5). Plasma level and excretion in beagle dogs.
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<SUP>3</SUP>H-TV-02([1β-<SUP>3</SUP>H]-1α, 24(R)-(OH)<SUB>2</SUB>D<SUB>3</SUB> was administered subcutaneously (0.4μg/kg) or applied transcutaneously (4μg/2g ointment) to beagle dogs, in order to investigate its plasma profiles and excretion.<BR>After a subcutaneous administration, plasma level of the radioactivity in lipid extracts in which 1α, 24(R)25-(OH)<SUB>3</SUB>D<SUB>3</SUB> was detected in addition to unchanged TV-02, reached the maximum value of 237 pg eq/ml after 4hr and decreased with apparent half-lives of 17hr and 116hr for α and β phase, respectively. 13% and 81% of radioactivity were excreted in urine and feces, respectively. After a transcutaneous application, the radioactivity in plasma was below the detection limit (Ca. 12pg eq/m<I>l</I>) throughout the sampling period (2 ?? 144hr).
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