摘要
目的 研究环孢素A聚乳酸纳米粒胶体 (CyA NP)的制备处方与工艺 ,并以新山地明 (Neoral)为参比制剂 ,进行相对生物利用度考察。方法 以溶剂 非溶剂法制备CyA NP ,用HPLC法测定全血中的药物浓度 ,计算胶体的生物利用度。结果 胶体中的纳米粒均匀圆整 ,粒径为 5 7 5nm ,药物回收率大于 90 %。CyA NP的AUC0 - 72 为 2 9 0 6mg·h·L- 1 ,Neoral的AUC0 - 72 为 2 8 5 9mg·h·L- 1 ,与Neoral相比 ,CyA NP的相对生物利用度为 10 1 6 % ,峰浓度较小(P <0 0 5 ) ,吸收较慢 (P <0 0 5 ) ,消除亦较慢 (P <0 1)。结论 以溶剂 非溶剂法可以简便制得CyA NP ,其大鼠相对生物利用度与Neoral相比无显著性差异 。
Aim To develop a less toxic alternative for sandimmun neoral (Neoral). To study the preparation conditions and to compare its pharmacokinetic characteristics with Neoral. Methods 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. Results 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). Conclusion The nanoparticles (diamater<100 nm) with relative high bioavailability were prepared using solvent nonsolvent method. It is suitable for further study.
出处
《药学学报》
CAS
CSCD
北大核心
2004年第1期68-71,共4页
Acta Pharmaceutica Sinica
基金
8 63计划资助项目 (2 0 0 1AA2 180 61)
