title: Whole-body tissue distribution of total radioactivity in rats after oral administration of [¹⁴C]-bilastine.
abstract: This study evaluated the tissue distribution of total radioactivity in male albino, male pigmented, and time-mated female albino rats after oral administration of a single dose of [¹⁴C]-bilastine (20 mg/kg). Although only 1 animal was analyzed at each time point, there were apparent differences in bilastine distribution. Radioactivity was distributed to only a few tissues at low levels in male rats, whereas distribution was more extensive and at higher levels in female rats. This may be a simple sex-related difference. In each group and at each time point, concentrations of radioactivity were high in the liver and kidney, reflecting the role of these organs in the elimination process. In male albino rats, no radioactivity was measurable by 72 hours postdose. In male pigmented rats, only the eye and uveal tract had measurable levels of radioactivity at 24 hours. Measureable levels of radioactivity were retained in these tissues at the final sampling time point (336 hours postdose), indicating a degree of melanin-associated binding. In time-mated female rats, but not in albino or pigmented male rats, there was evidence of low-level passage of radioactivity across the placental barrier into fetal tissues as well as low-level transfer of radioactivity into the brain.
authors.affiliation: Faes Farma, SA, R&D and Innovation Department, Leioa, Spain. mlucero@faes.es
authors.forename: María Luisa
authors.initials: ML
authors.lastname: Lucero
authors.forename: Andrew B
authors.initials: AB
authors.lastname: Patterson
mesh_terms: D000818:Animals; D001345:Autoradiography; D001562:Benzimidazoles / Q000378:metabolism / Q000493:pharmacokinetics*; D005123:Eye; D005260:Female; D039563:Histamine H1 Antagonists, Non-Sedating / Q000378:metabolism / Q000493:pharmacokinetics*; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008297:Male; D008431:Maternal-Fetal Exchange; D008543:Melanins / Q000378:metabolism; D010858:Pigmentation; D010880:Piperidines / Q000378:metabolism / Q000493:pharmacokinetics*; D011247:Pregnancy; D011849:Radioactive Tracers; D051381:Rats; D011919:Rats, Inbred Strains; D017207:Rats, Sprague-Dawley; D012727:Sex Characteristics; D014018:Tissue Distribution; D051598:Whole Body Imaging
chemical_list: D001562:Benzimidazoles; D039563:Histamine H1 Antagonists, Non-Sedating; D008543:Melanins; D010880:Piperidines; D011849:Radioactive Tracers; C445659:bilastine