title: Plasma pharmacokinetics and tissue distribution of bufotalin in mice following single-bolus injection and constant-rate infusion of bufotalin solution.
abstract: Bufotalin is one of the active antitumor components in Ch'an Su which is a widely used traditional Chinese medicine. However, there is insufficient information on the biopharmaceutical properties of bufotalin based on pharmacokinetic studies. To investigate the pharmacokinetics and tissue distribution of bufotalin, single-bolus injection and constant-rate infusion of bufotalin solution were performed in mice. After single intravenous administration, bufotalin was quickly distributed and eliminated from the plasma with a t1/2 of 28.6 min and an MRT of 14.7 min. Bufotalin concentrations in brain and lung were significantly higher than those in blood and other tissues at 30 min after dosing. The steady-state bufotalin plasma concentration and tissue distribution were determined using a novel constant-rate infusion device, and the distribution characteristics were similar to those of single-bolus injection. These results indicated that bufotalin could cross the blood-brain barrier and naturally target the lung. Bufotalin might be a promising antitumor candidate for lung cancer.
authors.affiliation: Shanghai Institute of Pharmaceutical Industry, National Pharmaceutical Engineering and Research Center, Shanghai, 201203, People's Republic of China.
authors.forename: Chui-liang
authors.initials: CL
authors.lastname: Yu
authors.forename: Hui-min
authors.initials: HM
authors.lastname: Hou
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism; D002018:Bufanolides / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D006207:Half-Life; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D008168:Lung / Q000378:metabolism; D008297:Male; D008516:Medicine, Chinese Traditional; D051379:Mice; D014018:Tissue Distribution
chemical_list: D000970:Antineoplastic Agents; D002018:Bufanolides; C004600:bufotalin