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首页> 外文期刊>European journal of drug metabolism and pharmacokinetics >Enhanced bioavailability of orally administered flurbiprofen by combined use of hydroxypropyl-cyclodextrin and poly(alkyl-cyanoacrylate) nanoparticles
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Enhanced bioavailability of orally administered flurbiprofen by combined use of hydroxypropyl-cyclodextrin and poly(alkyl-cyanoacrylate) nanoparticles

机译:羟丙基-环糊精和聚(氰基丙烯酸烷基酯)纳米粒子联合使用可增强口服氟比洛芬的生物利用度

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摘要

Flurbiprofen was formulated into nanoparticle suspension to improve its oral bioavailability. Hydroxy-propyl-beta-cyclodextrin inclusion-flurbiprofen complex (HP-beta-CD-FP) was prepared, then incoiporating this complex into poly(alkyl-cyanoacrylate) (PACA) nanoparticles. HP-beta-CD-FP-PACA nanoparticle was prepared by the emulsion solvent polymerization method. The zeta potential was -26.8 mV, the mean volume particle diameter was 134 nm, drug encapsulation efficiency was 53.3 ± 3.6 % and concentration was 1.5 mg/mL. The bioavailability of flurbiprofen from optimized nanoparticles was assessed in male Wistar rats at a dose of 15 mg/kg. As compared to the flurbiprofen suspension, 211.6 % relative bioavailability was observed for flurbiprofen nanoparticles. The reduced particle size and increased surface area may contribute to improve oral bioavailability of flurbiprofen.
机译:将氟比洛芬制成纳米颗粒悬浮液,以提高其口服生物利用度。制备了羟丙基-β-环糊精包合物-氟比洛芬复合物(HP-β-CD-FP),然后将该复合物并入聚(氰基丙烯酸烷基酯)(PACA)纳米颗粒中。通过乳液溶剂聚合法制备HP-β-CD-FP-PACA纳米颗粒。 zeta电位为-26.8 mV,平均体积粒径为134 nm,药物封装效率为53.3±3.6%,浓度为1.5 mg / mL。在雄性Wistar大鼠中以15 mg / kg的剂量评估了来自优化纳米颗粒的氟比洛芬的生物利用度。与氟比洛芬悬浮液相比,氟比洛芬纳米颗粒的相对生物利用度为211.6%。减小的粒径和增加的表面积可有助于改善氟比洛芬的口服生物利用度。

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