Concentration of temarotene (Ro 15-0778) and its metabolite Ro 14-6113 in plasma and skin of hairless rat.
The aim of this preliminary report was to measure plasma and skin concentrations of Ro 15-0778 and its phenolic metabolite Ro 14-6113 in hairless rats receiving orally 10 mg/kg of Temarotene once daily during 10 days. Blood (2-3 ml) and skin (200-300 mg) samples were taken at different time points between 0.5 and 240 h after the last dose. We used a highly sensitive HPLC method for simultaneous determination of the two compounds with a quantification limit of 2 ng/ml in plasma and 10 ng/g in total skin (epidermis and dermis). After 10 h, plasma concentrations of Ro 14-6113 were 5-13 times higher than for Ro 15-0778. Ro 14-6113 concentrations in the skin were 4-10 times higher than for Ro 15-0778 within the initial 48 h. The concentrations of both compounds in the skin were higher than concentrations in plasma.
Fenina
N
N
Laboratoire Hospitalo-Universitaire de Pharmacocinétique et Toxicocinétique, Faculté de Pharmacie et CHU Timone, Marseille, France.
Bun
H
H
Durand
A
A
D000284:Administration, Oral; D000818:Animals; D007166:Immunosuppressive Agents / Q000032:analysis* / Q000097:blood; D008297:Male; D051381:Rats; D011923:Rats, Nude; D012176:Retinoids / Q000008:administration & dosage / Q000032:analysis* / Q000097:blood; D012867:Skin / Q000737:chemistry
D007166:Immunosuppressive Agents; D012176:Retinoids; C072381:Ro 14-6113; C053595:temarotene