抗风湿涂膜剂的体内药物动力学研究

考察抗风湿涂膜剂中辣椒素和乌头类总生物碱在生物体内药动学特征,以获得药动学参数为临床应用提供参考依据.方法为给家兔背部按一定面积涂抹抗风湿涂膜剂后,于不同时间采取血样.分别用高效液相色谱仪和紫外可见分光光度计测定血药质量浓度,通过3P97药动学软件对所得的数据自动拟合获得药动学参数,得辣椒素药动学行为符合一室模型,主要药动学参数为Ka=1.160 013h-1t、1/2(Ka)=0.597 534 h、Ke=0.219 206 2 h-1t、1/2(Ke)=3.162 079 h、AUC=22.084 286(μg/mL)h;乌头类总生物碱药动学行为符合一室模型,主要药动学参数为Ka=0.300 004 9 h-1t、1/2(Ka)=2.310 453 h、Ke=0.185 421t、1/2(Ke)=3.738 234 h、AUC=22.389984(μg/mL).h.药代动力学实验表明,本制剂中辣椒素在动物体内吸收分布速率较快,而代谢消除速率较慢;而乌头类总生物碱吸收与代谢均较慢.二者吸收程度均较好.

Study of pharmacokinetics in vivo on anti-rheumatism film

To study pharmacokinetical properties of capsaicin and the total alkaloids in Radix Aconiti on anti-rheumatism film in vivo so that to provide reference for the clinical application.The blood samples at different times were taken after to smeare anti-rheumatism film on the rabbit.The concentration data were analyzed with HPLC and UV.The pharmacokinetical parameters were obtained through automatic fitting data by 3P97 pharmacokinetic software.From the results the capsaicin pharmacokinetical behaviors accord with 1-compartment model.The pharmacokinetical parameters of the capsaicin were Ka as 1.160 013 h-1,t1/2(Ka) as 0.597 534 h,Ke as 0.219 206 2 h-1,t1/2(Ke) as 3.162 079 h,AUC as 22.084 286(μg/mL)h.The total alkaloids in Radix Aconitic,accord with 1-compartment model.The pharmacokinetic parameters were Ka as 0.300 004 9 h-1,t1/2(Ka)as 2.310 453 h,Ke as 0.185 421,t1/2(Ke) as 3.738 234 h,AUC as 22.389 984(μg/mL)·h.The results indicated that the absorption and distribution of capsaicin were fast and it’s elimination was slow.But the absorption and elimination of the total alkaloids in Radix Aconiti all were slow.At the same time it showed that the relative bioavailability may be very high and so it had a good effect.