目的:研究环孢素的全血浓度测定方法;以市售新山地明(Neoral)为参比制剂,研究自制环孢素固体分散体(CsA- SD)在大鼠体内的药动学和相对生物利用度。方法:两组SD雄性大鼠分别单剂量给予CsA-SD和Neoral,按设计采集48 h 内动态血标本,采用HPLC法测定血药浓度。应用3P87药动学程序对数据进行拟合计算药动学参数。结果:单次给药后Ne- oral和CsA-SD的主要药动学参数Cmax分别为(4 029.7±405.8)ng·ml-1和(3 958±1 455)ng·ml-1,tmax分别为(1.54±0.57) h和(1.90±0.51)h,AUC0→8分别为(75 072±25 453)ng·h·ml-1和(84 861±26 392)ng·h·ml-1。统计分析结果显示,各主要药动学参数均无显著性差异。以Neoral为参比制剂,单剂量给药时CsA-SD的相对生物利用度为113.04%。结论:环孢素固体分散体在大鼠体内显示与市售新山地明相近的生物利用度。 OBJECTIVE: To study the method of determining the concentration of cyclosporine in whole blood. To study the pharmacokinetics and relative pharmacokinetics of CsA-SD in rats by using the commercially available Neoral as reference formulation bioavailability. Methods: Two male Sprague-Dawley rats were given CsA-SD and Neoral, respectively. Dynamic blood samples were collected within 48 hours according to the design, and plasma concentrations were determined by HPLC. The 3P87 pharmacokinetics program was used to fit the data to calculate the pharmacokinetic parameters. RESULTS: The main pharmacokinetic parameters Cmax of Neal and CsA-SD were (4 029.7 ± 405.8) ng · ml-1 and (3 958 ± 1 455) ng · ml-1, respectively (1.54 ± 0.57) h and (1.90 ± 0.51) h, AUC0 → 8 were (75 072 ± 25 453) ng · h · ml-1 and (84 861 ± 26 392) ng · h · ml-1, respectively. Statistical analysis showed no significant difference in the main pharmacokinetic parameters. With Neoral as reference preparation, the relative bioavailability of CsA-SD in a single dose was 113.04%. CONCLUSION: The solid dispersion of cyclosporine shows similar bioavailability to the commercially available neohexithiam in rats.