救必应酸琥珀酰酯在大鼠体内的药动学和绝对生物利用度研究

摘要

OBJECTIVE:To study the pharmacokinetics and absolute bioavailability of succinyl rotundic acid (SRA) in rats. METHODS:Wistar rats were randomly divided into intragastric injection(ig)group(30 mg/kg)and tail intravenous injection(iv) group (15 mg/kg),with 10 rats in each group. They were given SRA with relevant usage and dosage. The blood sample of tail vein 0.2 ml was respectively taken after 5,10,20,30,40,60,90,150,210,270,390,510 min of administration. The plasma concen-tration of SRA was determined by RP-HPLC using tanshinone ⅡA as internal standard. The pharmacokinetic parameters and abso-lute bioavailability were calculated by using 3p97 software. RESULTS:The pharmacokinetic parameters of ig group were that cmax was(1.02±0.27)μg/ml,tmax was(26.64±2.74)min,t1/2 was(42.79±3.46)min and AUC0-510 min was(92.27±9.26)μg·min/ml;those of tail iv group were that t1/2 was(17.21±1.58)min,and AUC0-510 min was(320.50±11.89)μg·min/ml. Oral obsolute bioavail-ability of SRA was 14.40%. CONCLUSIONS:The pharmacokinetic characteristics of SRA in rats conform to one-compartment model,and the absolute bioavailability is high.%目的：研究救必应酸琥珀酰酯（SRA）在大鼠体内的药动学和绝对生物利用度。方法：将Wistar大鼠随机分成ig组（30 mg/kg）和尾iv组（15 mg/kg），每组10只，按相应给药方法和剂量给予SRA，于给药后5、10、20、30、40、60、90、150、210、270、390、510 min尾静脉取血0.2 ml。以丹参酮ⅡA为内标，采用反相-高效液相色谱法测定其血药浓度，3p97软件计算药动学参数和绝对生物利用度。结果：ig组大鼠的cmax为（1.02±0.27）μg/ml，tmax为（26.64±2.74）min，t1/2为（42.79±3.46）min，AUC0-510 min为（92.27±9.26）μg·min/ml；尾iv组大鼠的t1/2为（17.21±1.58）min，AUC0-510 min为（320.50±11.89）μg·min/ml。SRA口服绝对生物利用度为14.40％。结论：SRA在大鼠体内的药动学特征符合单室模型；口服绝对生物利用度较高。