摘要
目的:研究2种环孢素A制剂的人体生物利用度.方法:采用两阶段、双交叉试验设计,20名健康志愿者单剂量口服500mg受试药(环孢素A口服溶液)和对照药(环孢素A胶囊)后采用高效液相色谱法测定全血中的药物浓度.结果:受试药与对照药的AUC0～24分别为(15 033.4±3 474.9)、(16 106.4±2 975.5)(ng·h)/ml,AUC0～∞分别为(16 755.5±3 827.5)、(17 488.5±3 233.89)(ng·h)/ml,tmax分别为(2.05±0.58)、(2.60±0.53)h,Cmax分别为(2 660.3±491.5)、(2 665.5±527.1)ng/ml,t1/2分别为(8.30±2.60)、(7.15±2.09)h;经统计分析,二者AUC 0～24、AUC0～∞、Cmax无显著性差异(P＞0.05),受试药tmax快于对照药;受试药的相对生物利用度为(93.83±15.21)%.结论:2种制剂的AUC 0～24、AUC0～∞、Cmax相似,而tmax差异较大.
OBJECTIVE： To study the bioavailability of 2 kinds of cyelosporin A preparations in human body. METHODS： Two-stage and two-way cross over was adopted in this determination, the whole blood concentrations of 20 healthy volunteers were determined by HPLC after a single oral dose of 500 mg cyclosporin A oral solution （the testing drug） and cyclosporin A capsule （the reference drug） . RESULTS： The main pharmacokinetic parameters of the testing drug and the reference drug were as follows,AUC0-24 were （15 033.4±3 474.9）（ng·h）/ml and （16 106.4±2 975.5）（ng · h）/ml; AUC0-∞ were （16 755.5±3 827.5） （ng·h）/ml and（ 17 488.5±3 233 89） （ng·h）/ml; t were （2.05±0.58） h and（2.60±0.53） h; C were（2 660.3±491.5）ng/ml and（2 665.5±527.1）ng/ml; t1/2 were（8.30±2.60）h and（7.15±2.09）h, respectively. The statistical analysis showed that the main pharmacokinetic parameters between the 2 preparations were of no great difference （P〉0.05） except that the tmax of the testing preparation was faster than that of the control drug, The relative bioavailability of the testing drug was （93.83± 15.21） %, CONCLUSION： The AUCσ-24, AUC0-∞ and Cmax of 2 preparations are similar, but there is a significant difference in tmax.
出处
《中国药房》
CAS
CSCD
北大核心
2005年第22期1723-1725,共3页
China Pharmacy
