Wang Xue-qing, Zhang Tao, He Ying, Zhang Liang, Zhang Qiang
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Yao Xue Xue Bao. 2004 Jan;39(1):68-71.
To develop a less toxic alternative for sandimmun neoral (Neoral). To study the preparation conditions and to compare its pharmacokinetic characteristics with Neoral.
Polylactide nanoparticles loaded cyclosporine A was prepared by solvent-nonsolvent method. Polylactide nanoparticles were administered by oral in a dosage of 15 mg.kg-1. The CyA concentration in whole blood sample was determined by HPLC.
The quantities of CyA, PLA and volume of acetone added had significant influence on the NP diameters. Under proper condition, the nanoparticles with diameters of 57.5 nm were obtained. The relative bioavailability in rats was 101.6%, with a smaller absorption rate (P < 0.05) and a smaller elimination rate (P < 0.1).
The nanoparticles (diamater < 100 nm) with relative high bioavailability were prepared using solvent-nonsolvent method. It is suitable for further study.
开发一种毒性较低的新山地明（Neoral）替代物。研究其制备条件，并将其药代动力学特征与新山地明进行比较。
采用溶剂-非溶剂法制备聚丙交酯纳米粒载环孢素A。聚丙交酯纳米粒以15mg·kg-1的剂量口服给药。采用高效液相色谱法测定全血样品中环孢素A的浓度。
环孢素A的用量、聚丙交酯的用量和丙酮加入量对纳米粒粒径有显著影响。在合适的条件下，可得到粒径为57.5nm的纳米粒。大鼠体内相对生物利用度为101.6%，吸收速率较小（P<0.05），消除速率较小（P<0.1）。
采用溶剂-非溶剂法制备了具有较高相对生物利用度的纳米粒（粒径<100nm）。适合进一步研究。
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