Xiao S H, Sun H L, Yang Y Q, Jiao P Y, You J Q, Guo H F
Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai.
Zhongguo Yao Li Xue Bao. 1990 Mar;11(2):176-80.
[3H]Praziquantel was absorbed rapidly by the cysts in mice infected with metacestodes of Echinococcus granulosus and treated with ig [3H]praziquantel 400 mg/kg (containing 3H 1.48 MBq). Within 24 h after treatment, 3H content in the ectocyst was 27.7-54.9% higher than that in cyst wall. The peak concentration of 3H in cyst wall and cyst fluid were 11.7-15.3% of those found in plasma. However, when the cysts were exposed to [3H]praziquantel 20 micrograms/ml (containing 3H 3.7 kBq), the 3H radioactivity in the cyst wall and cyst fluid reached equilibrium within 30 min-48 h after medication, corresponding to 45.5-63.3% of 3H radioactivity in the medium. Autoradiography showed that [3H]praziquantel entered into the germinal layer through ectocyst and laminated layer. The damage to germinal layer was related closely to deposition of the drug.
用含3H 1.48MBq的[3H]吡喹酮400mg/kg对感染细粒棘球绦虫囊尾蚴的小鼠进行灌胃处理后，[3H]吡喹酮被囊尾蚴迅速吸收。给药后24小时内，外囊中的3H含量比囊壁中的高27.7 - 54.9%。囊壁和囊液中3H的峰值浓度分别为血浆中浓度的11.7 - 15.3%。然而，当囊尾蚴暴露于含3H 3.7kBq的20μg/ml [3H]吡喹酮时，给药后30分钟至48小时内，囊壁和囊液中的3H放射性达到平衡，相当于培养基中3H放射性的45.5 - 63.3%。放射自显影显示，[3H]吡喹酮通过外囊和板层进入生发层。生发层的损伤与药物沉积密切相关。
