Original Articles

Absorption, distribution and excretion of [14C] praziquantel in animals

He-sheng Shao, Shang-ren Pan, Xi-nan Jing, Nan-xing Xu, Lan-qin Ying, Hai-yan Zhu, Xie-ming Qian, Han-ying Yan, Quan-sheng Yao


The absorption, distribution and excretion of [14C]praziquantel in rats, mice and mice infected with Schistosoma japonicum were reported. 14C was labeled at the carbonyl group of the piperazinone ring.
After iv in rats, the t1/2alpha and t1/2beta were 1 and 7.5 h, respectively. After a po dosage the radioactivity in the blood reached its peak at 1 h.
At 4 h after po, 46% of the radioactivity was absorbed in the stomach, 90% in the jejunum and 92% in the ileum.
After po, im or iv, the radioactivity was highest in the liver, then kidneys and lungs.
The radioactivities excreted in the bile within 12 h after iv and po were 28% and 6%, respectively. The radioactivities in the urine within 96 h were 63% and 65%, respectively.
At 24 h after a single dosage the radioactivities in the organs approached their background levels. The radioactivities in the liver and kidneys were slightly increased after multiple dosages.
The bioavailability of the drug was higher after im than after po.
The rates of absorption and excretion of the drug were slower and the peak values lower in the mice infected with S. japonicum than in the healthy mice.

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