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[细粒棘球绦虫继发性囊肿对甲苯达唑、阿苯达唑及阿苯达唑亚砜的体外摄取与释放]

[Uptake and release of mebendazole, albendazole and albendazole sulfoxide by secondary cysts of Echinococcus granulosus in vitro].

作者信息

You J Q, Xiao S H, Guo H F, Jiao P Y

机构信息

Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai.

出版信息

Zhongguo Yao Li Xue Bao. 1991 Jul;12(4):367-71.

PMID:1807086
Abstract

Mebendazole (Meb), albendazole (Alb) or albendazole sulfoxide (AlbSO) were taken rapidly in vitro by secondary cysts of Echinococcus granulosus removed out from mice infected with protoscoleces 8-9 months previously. The amounts of the drugs taken by the cysts were apparently increased followed by exposure of the cysts to the drugs at 10 micrograms.ml-1. The Alb penetrated into the cysts was distributed mainly in cyst wall, whereas the content of Meb in cyst wall was twice as much as that in cyst fluid. The distributions of AlbSO in cyst wall and cyst fluid were similar. When the cysts in the medium were exposed to Alb, some AlbSO and albendazole sulphone were detected in both cyst wall and cyst fluid, indicating that a part of Alb was metabolized by the cysts. In another experiment cysts exposed to the drug for 2 h were transferred to the medium without the drug for another 24 h. The release rates of the 3 drugs from the cysts were alike. In 1-2 h after transfer about 65-70% of the drugs absorbed by the cysts previously were released. Twenty-four hours after exposure the release rates increased to 75-85%, and the release of the drugs from the cyst wall was somewhat faster than that from cyst fluid.

摘要

甲苯咪唑(Meb)、阿苯达唑(Alb)或阿苯达唑亚砜(AlbSO)可被迅速地从8-9个月前感染原头节的小鼠体内取出的细粒棘球绦虫继发性囊肿在体外摄取。将囊肿暴露于10微克·毫升-1的药物后,囊肿摄取的药物量明显增加。进入囊肿的阿苯达唑主要分布在囊肿壁中,而甲苯咪唑在囊肿壁中的含量是囊肿液中的两倍。阿苯达唑亚砜在囊肿壁和囊肿液中的分布相似。当培养基中的囊肿暴露于阿苯达唑时,在囊肿壁和囊肿液中均检测到一些阿苯达唑亚砜和阿苯达唑砜,这表明一部分阿苯达唑被囊肿代谢。在另一项实验中,将暴露于药物2小时的囊肿转移至不含药物的培养基中再培养24小时。这三种药物从囊肿中的释放速率相似。转移后1-2小时内,囊肿先前吸收的药物约有65-70%被释放。暴露24小时后,释放速率增至75-85%,且药物从囊肿壁的释放比从囊肿液的释放略快。

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