Pharmacokinetic studies of 1α, 24(R)-(OH)23D(TV-02)(5):Plasma level and excretion in beagle dogs

Tomohiro OHTA; Hirohide MIMURA; Masaru YAMAMOTO; Mamoru KIYOKI; Takeo OHBA; Tatsuyuki NARUCHI

doi:10.2133/dmpk.5.63

Pharmacokinetic studies of 1α, 24(R)-(OH)₂₃D(TV-02)(5):Plasma level and excretion in beagle dogs

Tomohiro OHTA, Hirohide MIMURA, Masaru YAMAMOTO, Mamoru KIYOKI, Takeo OHBA, Tatsuyuki NARUCHI

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Keywords: 1α, 24(R)-(OH)₂D₃, TV-02, 1α, 24(R)25-(OH)₃D₃, Plasma level, Excretion

JOURNAL FREE ACCESS

1990 Volume 5 Issue 1 Pages 63-69

DOI https://doi.org/10.2133/dmpk.5.63

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Abstract

³H-TV-02([1β-³H]-1α, 24(R)-(OH)₂D₃ was administered subcutaneously (0.4μg/kg) or applied transcutaneously (4μg/2g ointment) to beagle dogs, in order to investigate its plasma profiles and excretion.
After a subcutaneous administration, plasma level of the radioactivity in lipid extracts in which 1α, 24(R)25-(OH)₃D₃ 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/ml) throughout the sampling period (2 ?? 144hr).

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