Pharmacokinetics, absorption, distribution and disposition of [125I]-oligotide following intravenous or oral administration in the rat.
Oligotide (O) was labelled with 125I. The radiolabelled compound ([125I]-Oligotide ([125I]-O)) retained the biological activity of parent O. Following single intravenous administration the half lives of radioactivity associated with O and/or O related components in plasma were 9-10 min and 9-10 h for alpha and beta phases respectively. Following single oral administration the half life of radioactivity associated with O and/or O related components in plasma was 11.45-12.76 h for beta fase. Following multiple oral administration once daily for 7 days, the half life of radioactivity associated with O and/or O related components following the 7th dose was 10-12 h for beta phase. The areas under plasma total radioactivity versus time curves were dose-dependent. Following single intravenous administration the major proportion of the administered dose was excreted via urine, while following single oral administration excretion via urine and faeces accounted for similar proportions of the administered dose. Following both single and oral administration the levels of radioactive components derived from [125I]-O in organs examined were generally highest in highly perfused organs.
Fisher
J
J
Inveresk Research International, Tranent, Scotland.
Holland
T K
TK
Pescador
R
R
Porta
R
R
Ferro
L
L
D000042:Absorption; D000284:Administration, Oral; D000818:Animals; D000990:Antithrombin III / Q000494:pharmacology; D006207:Half-Life; D007275:Injections, Intravenous; D007457:Iodine Radioisotopes; D008297:Male; D009838:Oligodeoxyribonucleotides / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D010974:Platelet Aggregation / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D009838:Oligodeoxyribonucleotides; C099595:oligotide; D000990:Antithrombin III