The disposition of thioperamide, a histamine H3-receptor antagonist, in rats.
An HPLC method using an ovomucoid-conjugated column has been developed for measurement of thioperamide, a histamine H3 antagonist, with a minimum quantitation limit of 0.05 micrograms mL-1. The assay was used to study the disposition of thioperamide in rats. After bolus intravenous administration of thioperamide (10 mg kg-1), the plasma concentration decreased monoexponentially with a half-life of 26.9 min. The apparent total body clearance of thioperamide from rat plasma was 74.6 mL min-1 kg-1. Although thioperamide was quickly transferred to various tissues, its concentrations in peripheral tissues were higher than that in the brain. However, the brain regional tissue/plasma ratios of thioperamide increased continuously after its injection.
Department of Pharmaceutics I, Tohoku College of Pharmacy, Sendai, Japan.
E
E
Sakurai
E
E
Gunji
Y
Y
Iizuka
N
N
Hikichi
K
K
Maeyama
T
T
Watanabe
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D006207:Half-Life; D006633:Histamine Antagonists; D007275:Injections, Intravenous; D008297:Male; D008954:Models, Biological; D010059:Ovomucin / Q000737:chemistry; D010880:Piperidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
D006633:Histamine Antagonists; D010880:Piperidines; D010059:Ovomucin; C052075:thioperamide