13-甲基豆蔻酸在大鼠体内的药代动力学研究

目的　研究 1 3 -甲基豆蔻酸在大鼠体内的药代动力学。方法　用毛细管柱气相色谱法测定生物样品中的原形药物浓度 ,在大鼠体内进行血浆药代动力学、分布、排泄及血浆蛋白结合实验。结果　大鼠 ig1 3 -甲基豆蔻酸 40 0 ,80 0 ,1 2 0 0 mg· kg-1后 ,拟合的血药浓度 -时间曲线符合二室模型 ,t1/2α 为 2 .3 1 3～ 2 .843 h,t1/2β 为5 .0 99～ 6 .3 3 9h;tpeak 为 2 .2 1 5～ 2 .76 6 h;血浆蛋白结合率大于 85 .80 %。药物在大鼠体内分布广泛 ,其中心、肺、脾、肝等组织浓度较高 ,肌肉、脂肪等组织相对较低。 2 4 h粪、尿、胆汁原形药物排泄量分别为给药量的1 3 .77% ,0 .0 0 3 2 %和 0 .0 2 1 4%。结论　 1 3 -甲基豆蔻酸在大鼠体内吸收快 ,达峰时间短 ,组织分布广泛 ,血浆蛋白结合率高 ;有部分原形药物从粪便排泄

Study on pharmacokinetics of 13-methyltetradecanoic acid in rats

Objective To study the pharmacokinetics, absorption, distribution, excretion and plasma protein binding ratio of 13-MTD in rats. Methods The concentration of 13-MTD in biological specimens was determined by a gas chromatography method. Results The disposion was conformed to a two compartment model with t 1/2α=2.313～2.843 h,t 1/2β=5.099～6.339 h, t peak=2.215～2.766 h at the dosages of 400, 800 and 1 200 mg·kg -1. The plasma protein binding ratio of the drug was above 85.8%. 13-MTD was shown to be widely distributed to the various tissues. There was a relatively higher drug concentration in heart, lung, speen and liver,and relatively lower in fat and muscle. 13-MTD excrected in feces, urine and bile within 24 h was 13.77%, 0.003 2% and 0.021 4% respectively. Conclusions 13-MTD was absorbed and eliminated at a rapid rate and widely distributed in rats. The plasma protein binding ratio was found to be high. About 15% of unchanged 13-MTD was excreted in feces, only trace amount of 13-MTD was excreted in bile and almost no excretion was found in urine.