王学清, 戴俊东, 张强, 张涛, 夏桂民. 环孢素A-羟丙甲纤维素酞酸酯纳米粒的大鼠相对生物利用度J. 药学学报, 2004, 39(6): 463-466.
引用本文: 王学清, 戴俊东, 张强, 张涛, 夏桂民. 环孢素A-羟丙甲纤维素酞酸酯纳米粒的大鼠相对生物利用度J. 药学学报, 2004, 39(6): 463-466.
WANG Xue-qing, DAI Jun-dong, ZHANG Qiang, ZHANG Tao, XIA Gui-min. Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in ratsJ. Acta Pharmaceutica Sinica, 2004, 39(6): 463-466.
Citation: WANG Xue-qing, DAI Jun-dong, ZHANG Qiang, ZHANG Tao, XIA Gui-min. Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in ratsJ. Acta Pharmaceutica Sinica, 2004, 39(6): 463-466.

环孢素A-羟丙甲纤维素酞酸酯纳米粒的大鼠相对生物利用度

Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in rats

  • 摘要: 目的制备环孢素A-HPMCP(两种型号HP50与HP55)纳米粒,并与新山地明(Neoral)进行大鼠相对生物利用度与药物动力学行为的比较。方法以溶剂-非溶剂法制备CyA-HP50 NP与CyA-HP55 NP,用HPLC法测定其相对生物利用度,并用3P97程序计算药代动力学参数。结果3种制剂的血药浓度-时间数据均以2室模型拟合最佳。与Neoral相比,CyA-HP50 NP与CyA-HP55 NP的相对生物利用度分别为82.3%和119.6%,均无显著性差异;CyA-HP50 NP与CyA-HP55 NP的K10均较小(P<0.05),说明药物消除较慢。与CyA-HP50 NP相比,CyA-HP55 NP的相对生物利用度为145.3%,有显著性差异(P<0.01)。结论CyA-HPMCP NP 制备方法简便,生物利用度高,可望开发为一种新的制剂。

     

    Abstract: AimTo study the preparation of hydroxypropyl methylcellulose phthalate(HPMCP) nanoparticles and compare its pharmacokinetic characteristics with Neoral. MethodsHPMCP nanoparticles loaded cyclosporine A were prepared by solvent-nonsolvent method. CyA-HP50 nanoparticles, CyA-HP55 nanoparticles and Neoral were orally administered at the dosage of 15 mg·kg-1 to rats. The CyA concentration in blood were determined by HPLC. Pharmacokinetic parameters were calculated by 3P97 program. ResultsThe concentration-time data of the three preparations were best fit by two compartment model. The relative bioavailability of CyA-HP50 and CyA-HP55 nanoparticles calculated by the AUC0-72 were 82.3% and 119.6%, bioequivalent to the reference of Neoral. The relative bioavailability of CyA-HP55 nanoparticles was 145.3% of CyA-HP50 nanoparticles. Conclusion CyA HPMCP nanoparticles could be prepared easily and reproducibly. It was found that the oral absorption of CyA can be increased by using the HPMCP nanoparticles.

     

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