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通过制备阿苯达唑-环糊精复合物提高阿苯达唑的生物利用度和驱虫活性。

Improving bioavailability and anthelmintic activity of albendazole by preparing albendazole-cyclodextrin complexes.

作者信息

García-Rodriguez J J, Torrado J, Bolás F

机构信息

Departmento de Parasitología, Facultad de Farmacia, Universidad Complutense, Spain.

出版信息

Parasite. 2001 Jun;8(2 Suppl):S188-90. doi: 10.1051/parasite/200108s2188.

Abstract

The bioavailability and anthelmintic activity of albendazole-cyclodextrin complexes (ABZ-CDC) compared to albendazole suspensions in carboxymethylcellulose (ABZ-CMC) was assessed in a mouse model for Trichinella infections. Swiss CD-1 mice experimentally infected with T. spiralis were treated with both formulations against enteral (adult worms) and parenteral (migrating and encysted larvae). Oral bioavailability was assessed in age matched mice treated with 50 mg/kg of both formulations. The anthelmintic effects and plasma concentration of the active metabolite albendazole-sulphoxide (ABZSO) enantiomer (-) were significantly increased following administration of ABZ-CDC in relation to ABZ-CMC.

摘要

在旋毛虫感染的小鼠模型中,评估了阿苯达唑 - 环糊精复合物(ABZ - CDC)与羧甲基纤维素阿苯达唑混悬液(ABZ - CMC)相比的生物利用度和驱虫活性。用这两种制剂对实验感染旋毛虫的瑞士CD - 1小鼠进行治疗,以对抗肠道(成虫)和肠外(迁移和包囊化幼虫)感染。在用50 mg/kg的两种制剂治疗的年龄匹配小鼠中评估口服生物利用度。与ABZ - CMC相比,给予ABZ - CDC后,活性代谢物阿苯达唑亚砜(ABZSO)对映体(-)的驱虫效果和血浆浓度显著增加。

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