灯盏花素脉冲控释片在家兔体内的药物动力学研究

Study on Pharmacokinetics of Breviscapine Pulsatile Controlled-Release Tablets in Rabbits

目的研究灯盏花素脉冲控释片在家兔体内的药物动力学。方法采用液-液萃取法制备血样供试品,应用HPLC法测定制剂中灯盏乙素的血药浓度并进行药动学研究。结果灯盏花素脉冲控释片在家兔体内呈二室模型分布,其主要药动学参数:k a=1.4230 h-1,α=1.2042 h-1,β=0.5546 h-1,t1/2(a)=0.49 h,t1/2(α)=0.58 h,t1/2(β)=1.25 h,k21=1.0387 h-1,k12=0.0771 h-1,k10=0.6430 h-1,V c=2.71 L,V=3.14 L,CL=1.74 L/h,AUC0→∞=34.46μg·h/mL,T lag=1.06 h,MRT=4.20 h。结论灯盏花素脉冲控释片在兔体内经过一定时间以脉冲式释放药物,达到了延时释药的设计要求,且体内外释药过程具有一定的相关性。

Objective To study pharmacokinetics of Breviscapine pulsatile controlled-release tablets in rabbits.Methods Lc/Lc extract was used to prepare blood test samples,HPLC was used to determine scutellarin and conducted pharmacokinetic research.Results Breviscapine pulsatile controlled-release tablets were fitted to double-department model in rabbits.The main parameters were：ka =1.4230 h-1,α =1.2042 h-1,β =0.5546 h-1,t1/2（a） =0.49 h,t1/2（a） =0.58 h,t1/2（β） =1.25 h,k21 =1.0387 h-1,k12 =0.0771 h-1,k10 =0.6430 h-1,Vc =2.71 L,V =3.14 L,CL =1.74 L/h,AUC0→∞ =34.46 ug · h/mL,Tlag =1.06 h,MRT =4.20 h.Conclusions After a certain period,breviscapine pulsatile controlled-release tablets in rabbits release drugs by pulse,reached the design requirements of delay release,and vivo and in vitro delayed release time has a certain correlation.