纳米级雄黄粉体药代动力学研究

Study on pharmacokinetics of nanoparticle realgar powders in rabbit

目的 制备纳米级雄黄粉体 ,比较传统雄黄与纳米级雄黄的药代动力学行为。方法 两组家兔分别单剂量口服5 0mg ,比较纳米级雄黄粉体和传统雄黄在兔体内的药代动力学参数。结果 传统雄黄组家兔的药动学参数为 :A =0 .0 96 2±0 .0 0 93mg·L-1,Ke =0 .0 70 2± 0 .0 0 74l/h ,Ka =0 .4 72 3± 0 .0 712l/h ,Lagtime=0 .0 30 0± 0 .0 0 0 0H ,T1/ 2 (Ka) =0 .15 1± 0 .2 38H ,T1/ 2 (Ke) =10 .0 5 6± 0 .895H ,T(peak) =4 .80 6± 0 .4 0 1H ,C(max) =0 .0 6 0± 0 .0 0 0mg·L-1,AUC =1.16 8± 0 .0 84 (mg·L-1)h ,CL/F(s) =4 3.0 78± 3.4 95L/h ,V/F(c) =6 2 0 .6 96± 2 9.6 4 9L ;纳米雄黄组家兔的药动学参数为 :A =0 .2 4 4 3± 0 .0 0 5 2mg·L-1,Ke =0 .0 2 2 7±0 .0 0 5 2l/h ,Ka =0 .92 2 5± 0 .0 5 93l/h ,Lagtime =0 .0 30 0± 0 .0 0 0 0H ,T1/ 2 (Ka) =0 .75 4± 0 .0 4 9H ,T1/ 2 (Ke) =2 8.74 6± 1.0 0 7H ,T(peak) =4 .0 6 6± 0 .174H ,C(max) =0 .2 16± 0 .0 0 5mg·L-1,AUC =9.82 2± 0 .394 (mg·L-1)h ,CL/F(s) =5 .10 8± 0 .2 0 8L/h ,V/F(c) =2 11.5 6 6± 3.2 97L。结论 纳米级雄黄粉体与传统雄黄比较 ,其药代动力学发生显著变化 ,吸收相增大而消?

Aim To prepare nanopariticle realgar powlders and compare pharmacokinetics of nanometer realgar and traditional realgar.Methods The pharmacokinetics of As between nanometer realgar and traditional realgar were compared after single oral administration of 50mg in rabbits.Result The pharmacokinetics parameters of traditional realgar were:A=0.096 2±0.009 3mg·L -1 ,Ke=0.070 2±0.007 4l/h,Ka=0.472 3±0.071 2l/h,Lagtime=0.0300±0.0000H,T 1/2 (Ka)=0.151±0.238H,T 1/2 (Ke)=10.056±0.895H,T (peak) =4.806±0.401H,C (max) =0.060±0.000mg·L -1 ,AUC=1.168±0.084(mg·L -1 )h,CL/F(s)=43.078±3.495L/h,V/F(c)=620.696±29.649L;The pharmacokinetics parameters of nanometer realgar were:A=0.244 3±0.005 2mg·L -1 ,Ke=0.022 7±0.005 2l/h,Ka=0.922 5±0.059 3l/h,Lagtime=0.030 0±0.000 0H,T 1/2 (Ka)=0.754±0.049H,T 1/2 (Ke)=28.746±1.007H,T (peak) =4.066±0.174H,C (max) =0.216±0.005mg·L -1 ,AUC=9.822±0.394(mg·L -1 )h,CL/F(s)=5.108±0.208L/h,V/F(c)=211.566±3.297L.Conclusions The pharmacokinetics of As between nanometer realgar and traditional realgar were compared,there is notabily variety,absorb mutually increase and eliminate mutually decrease.