Pharmacokinetic study of radioactive antineoplaston A10 in rats and mice.
Fifteen Wistar rats were divided into three groups: low dose--150 mg/kg, medium dose--300 mg/kg and high dose--600 mg/kg. 3H-labelled antineoplaston A10 (3H-A10) was administered to the rats in all three groups. Blood was withdrawn from the tail vein, while urine and faeces were collected at different time intervals for the determination of radioactivity. The volume of distribution (Vd) was evaluated in the rats by intravenous dosage of 150 mg/kg of 3H-A10 dissolved in dimethyl sulfoxide. Thirty mice were divided into six groups and sacrificed at 1, 3, 6, 12, 24 and 36 h respectively after oral administration of H3-A10 for the study of radioactivity in various organs. It was observed that the concentration-time curves of A10 in the blood support a dicompartmental model of pharmacokinetics, and calculated values are very close to experimental values. The binding rate of A10 to plasma protein is 5.05% at 3 h after oral administration. Organ distribution studies indicated the highest accumulation of radioactivity in the bladder, followed by kidney, stomach, genitals and liver, whereas there was lower accumulation of radioactivity in the spleen, heart, brains and lungs.
Xu
W
W
Shandong Medical University, Department of Pharmacy, Jinan, China.
Wang
H
H
Yuan
Y
Y
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D044482:Benzeneacetamides; D004305:Dose-Response Relationship, Drug; D005260:Female; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D010880:Piperidines / Q000493:pharmacokinetics*; D010881:Piperidones; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution
D000970:Antineoplastic Agents; D044482:Benzeneacetamides; D010880:Piperidines; D010881:Piperidones; C052091:antineoplaston A10