Abstract: This study is devoted to investigate the pattern of absorption, distribution and elimination of ¹⁴C-labeled gossypol (Spec. act. 0.3μci/mg). Single oral doses of 40, 15, 2 and 2 mg/kg were administered to mice, rats, dog and monkey, respectively. The results indicate that in the blood of mice and rats the peak of radioactivity appeared 6～9 br after the admnistration: the biological half-lifes of gossypol in each of these were 31 and 16.5 hr. Forty eight hours after ¹⁴C-gossypol administration radioactivity was found in all tissues determined, concentration of ¹⁴C in the contants of gastrointestinal tract was the highest, while that in the liver and kidneys were nextto ti. Radioactivity was higher in the testes of rats than in those of mice. The main route for ¹⁴C-gossypol elimination was in the feces, only a very small portion of the ingested ¹⁴C was eliminated via the urine. In similar experiments on one dog and one monkey, radioactivity in testes was found to be lower than in rats. The radioactivity of the dog heart was the highest while the rate of excretion of ¹⁴C via the gastrointestinal tract of the monkey was highest among all these 4 species The biological half-life of gossypol in blood were 11 and 45 hr in monkey and dog, respectively.The experimental data thus obtained suggest that the difference in antifertility activity and toxicity of gossypol among different animals might be attributed to the difference of distribution, rate of absorption and elimination among these animals.