【摘要】 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。更多还原

【Abstract】 Objective: To study the pharmacokinetics and relative bioavailability of ciclosporin in rats. Method: The ciclosporin concentration of in whole blood was determined by HPLC. Single dose of CsA-SD po and that of Neoral po were given in two groups of rats respectively. The data was processed by the software 3P87. The pharmackinetic parameters were estimated by a statistic analysis of ANOVA. Result: The Cmax,tmax,AVC0→48 of Neoral and CsA-SD were (4029.7±405.8)ng·ml-1 and (3958±1455) ng·ml-1 , (1.54±0.57)h and (1.90±0.51)h, (75072±25453) ng·h·ml-1 and (84861±26392)ng·h·ml-1, respectively. The mean relative bioavailability of the CsA-SD vs Neoral was 113. 04% . The analyzed result showed that there were not a stastical difference between two groups. Conclusion: The results suggested that the ciclosporin solid dispersion had the similar bioavailability compared with Neoral.更多还原