在小鼠体内具有改善药代动力学性能的阿苯达唑纳米晶体。
Albendazole nanocrystals with improved pharmacokinetic performance in mice.
作者信息
Paredes Alejandro J, Bruni Sergio Sánchez, Allemandi Daniel, Lanusse Carlos, Palma Santiago D
机构信息
Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET & Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba. Ciudad Universitaria, X5000HUA-Córdoba, Argentina.
Laboratorio de Farmacología, Centro de Investigación Veterinaria de Tandil (CIVETAN), UNCPBA-CICPBA-CONICET, Facultad de Ciencias Veterinarias, UNCPBA, Tandil, Argentina.
出版信息
Ther Deliv. 2018 Feb;9(2):89-97. doi: 10.4155/tde-2017-0090.
AIM
Albendazole (ABZ) is a broad-spectrum antiparasitic agent with poor aqueous solubility, which leads to poor/erratic bioavailability and therapeutic failures. Here, we aimed to produce a novel formulation of ABZ nanocrystals (ABZNC) and assess its pharmacokinetic performance in mice. Results/methodology: ABZNC were prepared by high-pressure homogenization and spray-drying processes. Redispersion capacity and solid yield were measured in order to obtain an optimized product. The final particle size was 415.69±7.40 nm and the solid yield was 72.32%. The pharmacokinetic parameters obtained in a mice model for ABZNC were enhanced (p < 0.05) with respect to the control formulation.
CONCLUSION
ABZNC with improved pharmacokinetic behavior were produced by a simple, inexpensive and potentially scalable methodology.
目的
阿苯达唑（ABZ）是一种水溶性差的广谱抗寄生虫药，这导致其生物利用度低/不稳定以及治疗失败。在此，我们旨在制备一种新型阿苯达唑纳米晶体（ABZNC）制剂，并评估其在小鼠体内的药代动力学性能。结果/方法：通过高压均质和喷雾干燥工艺制备ABZNC。测量再分散能力和固体产率以获得优化产品。最终粒径为415.69±7.40纳米，固体产率为72.32%。在小鼠模型中获得的ABZNC药代动力学参数相对于对照制剂有所提高（p<0.05）。
结论
通过一种简单、廉价且具有潜在可扩展性的方法制备了药代动力学行为得到改善的ABZNC。
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