Pharmacokinetic evaluation of indomethacin nanocapsules.

Drug design and delivery Pub Date : 1989-06-01
V Andrieu, H Fessi, M Dubrasquet, J P Devissaguet, F Puisieux, S Benita
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引用次数: 0

Abstract

Indomethacin-loaded polyisobutylcyanoacrylate nanocapsules were prepared by interfacial polymerization of the alkylcyanoacrylate monomer. Mean particle size of the nanocapsules ranged from 200 to 300 nm. Comparison of the results following intravenous infusion of indomethacin solution and nanocapsules to rats revealed that nanoencapsulation accelerated the extravascular distribution of indomethacin due partly to enhanced uptake of the colloidal carrier by the liver reticuloendothelial system. Following intragastric administration, the oral bioavailability of indomethacin in solution was 90%--indicating complete absorption of this drug from the gastrointestinal tract of the rat. Absorption of indomethacin nanocapsules by this route was more rapid. This was attributed either to an increase in the intensity and/or the duration of contact of the encapsulated drug with the gut wall, or to a more efficient absorption process involving paracellular pathways.

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吲哚美辛纳米胶囊的药动学评价。
采用氰基丙烯酸烷基酯单体界面聚合法制备了负载吲哚美辛的聚氰基丙烯酸异丁酯纳米胶囊。纳米胶囊的平均粒径为200 ~ 300 nm。对大鼠静脉滴注吲哚美辛溶液和纳米胶囊的结果进行比较发现,纳米胶囊加速了吲哚美辛在血管外的分布,部分原因是纳米胶囊增强了肝网状内皮系统对胶体载体的摄取。灌胃后,吲哚美辛溶液的口服生物利用度为90%,表明该药物从大鼠胃肠道完全吸收。该方法吸收吲哚美辛纳米胶囊的速度较快。这可能是由于包裹药物与肠壁接触的强度和/或持续时间增加,或者是由于涉及细胞旁途径的更有效的吸收过程。
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