摘要
目的 研究环孢素(CyA)微乳剂的药动学和相对生物利用度。方法 2 0名健康志愿者单剂量口服CyA微乳剂和普通乳剂,用HPLC法测定血药浓度。结果 微乳剂的相对生物利用度为(2 2 9.2 8±95 .0 0 ) % ,微乳剂和普通乳剂的药动学参数分别为AUC0→2 4:(10 76 4 .32±2 6 6 9.4 4 )、(5 187.35±1913.80 ) μg·h·L-1,cmax:(194 8.0 1±35 0 .0 7)、(890 .0 1±2 73.6 4 ) μg·L-1;tmax:(1.6 8±0 .5 9)、(2 .98±0 .77)h。2种制剂的主要药动学参数AUC0→2 4、cmax和tmax经方差分析显示差异均具显著性意义(P <0 .0 5 )。双单侧t检验结果显示2种制剂不具生物等效性。
AIM To study the pharmacokinetics and relative bioavailability of ciclosporin microemulsion in Chinese healthy volunteers. METHODS A single dose of ciclosporin microemulsion and emulsion were crossover given to 20 healthy volunteers and whole blood levels were determined by HPLC. RESULTS The relative bioavailability of ciclosporin microemulsion was (229.28±95.00)%. Pharmacokinetic parameters of the microemulsion and emulsion preparation were AUC 0→24:(10 764.32±2 669.44) and (5 187.35±1 913.80) μg·h·L -1,c max:(1 948.01±350.07) and (890.01±273.64) μg·L -1;t max:(1.68±0.59) and (2.98±0.77)h,respectively. There were significant difference in the pharmacokinetic parameters between the 2 preparations. CONCLUSION The bioavailability of cyclosporin A microemulsion is better than the emulsion preparation.
出处
《中国临床药学杂志》
CAS
2005年第2期94-97,共4页
Chinese Journal of Clinical Pharmacy
