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通过在聚乙烯吡咯烷酮中制备固体分散体来提高阿苯达唑对旋毛虫肠道期而非肠外期的疗效。

Improvement of albendazole efficacy against enteral, but not against parenteral stages of Trichinella spiralis by preparing solid dispersions in polyvinylpyrrolidone.

作者信息

Lopez M L, Torrado S, Torrado S, Martínez A R, Bolás F

机构信息

Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense, Madrid, España.

出版信息

Chemotherapy. 1997 Nov-Dec;43(6):430-5. doi: 10.1159/000239602.

Abstract

A comparison was made, in the Trichinella/mouse model, of the anthelmintic effects of albendazole (ABZ) and ricobendazole (RBZ) formulated as solid dispersions in polyvinylpyrrolidone with regard to ABZ formulated as a suspension in carboxymethylcellulose. A solid dispersion significantly increased (p < 0.01) the efficacy of the drugs against intestinal preadult but not against migrating and muscle stages of the parasite. The anthelmintic efficacy of RBZ given as a solid dispersion was equivalent to (against preadult and encysted larvae) or significantly lower than (against migrating larvae) that of ABZ with the same formulation. The pharmacokinetic profiles of ABZSO as measured by HPLC showed no significant differences in the Cmax and AUC following administration of ABZ formulated as a suspension or solid dispersion although the Tmax was significantly lower for the dispersion.

摘要

在旋毛虫/小鼠模型中,将阿苯达唑(ABZ)和利可苯达唑(RBZ)制成聚乙烯吡咯烷酮固体分散体的驱虫效果,与制成羧甲基纤维素混悬液的ABZ进行了比较。固体分散体显著提高了(p < 0.01)药物对肠道未成熟虫体的疗效,但对寄生虫的移行期和肌肉期无效。以固体分散体形式给药的RBZ的驱虫效果与相同制剂的ABZ相当(针对未成熟虫体和包囊幼虫)或显著低于(针对移行幼虫)ABZ。通过高效液相色谱法测定的阿苯达唑亚砜(ABZSO)药代动力学曲线显示,给予混悬液或固体分散体形式的ABZ后,其Cmax和AUC无显著差异,尽管固体分散体的Tmax显著降低。

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