关键词: ［14C］CT-707, 放射性同位素, 液体闪烁计数法, 吸收, 排泄

Abstract: AIM: To study the absorption and excretion of CT-707 in healthy male subjects. METHODS: Six healthy male subjects received a single 300 mg (120 μCi) oral dose of radio-labeled CT-707 as a suspension in a fasted state. Blood, urine and feces were collected. Radioactivity concentrations were measured by liquid scintillation counting (LSC). The pharmacokinetic parameters of total radioactivity in plasma were calculated by WinNonlin (Pharsight version 8.1) software according to the non-compartment model. The recovery rate of total radioactivity in urine and feces was calculated according to the weight and radioactivity concentration of urine and feces collected at each time interval. RESULTS: After a single 300 mg oral of radio-labeled CT-707 552 h (23 d) as a suspension in a fasted state, the mean AUC0-t, AUC0-∞, Cmax, Tmax and t1/2 values for CT-707 in plasma were (1 049.15±589.38) ng·Equ.g-1·h, (2 288.64±511.05) ng·Equ.g-1·h, (229.00±63.66) ng/Equ.g, (2.83±1.47) h and (6.17±2.43) h, respectively. Excretion test results showed that CT-707 was mainly excreted from feces with a mean cumulative recovery of about (76.24±3.43)%, and partial excreed from urine with a mean cumulative recovery of about (3.41±1.00)%, and a total mean cumulative recovery of about (79.65±3.26)%. CT-707 was well tolerated and no serious adverse events were reported. CONCLUSION: In healthy male subjects, CT-707 suspension preparation can be absorbed quickly and eliminated quickly after a single oral in a fasted state. Most of the suspension preparation can be recovered through feces, showing good safety and tolerated.

Key words: ［14C］CT-707, radioactive isotopes, liquid scintillation counting, absorption, excretion