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用高效液相色谱法测定了维胶酸(RⅡ)在大鼠体内的吸收,分布,排泄,生物利用度及蛋白结合率等药代动力学特性,RⅡ30mg·kg-1iv,血清中药物浓度经两次加权的二室模型拟合,T1/2β为20.71h,CLs为0.34L·kg-1·h-1,Vc为0.99L·kg-1.RⅡ100及200mg·kg-1po,经一室开放模型拟合,T1/2Ke分别为11.92及13.01h,CLs为0.87及0.77L·kg-1·h-1,体内绝对生物利用度为39.7%及46.4%。RⅡ200mg·kg-1po7h后,肠,胃组织中RⅡ含量囊高,血,肝,卵巢,肾次之,心,脾,肺,睾丸,肌肉,脂肪含量较少,脑,副睾,骨组织含量极微;24h后,各组织含量明显下降,说明RⅡ不易在体内蓄积。120h内主要经粪便排出,累积排出率为34.4±s2.0%,经尿液,胆汁排泄较少,累积排泄率仅分别为1.1±s0.6%及0.024±s0.01%。经超滤法测定,RⅡ血药浓度在45.94-103.22mg·L-1内,RⅡ血浆蛋白结合率为46.6%一52.4%。
The pharmacokinetic characteristics of vicinal acid (RⅡ) in rats were determined by high performance liquid chromatography (RⅡ) in the absorption, distribution, excretion, bioavailability and protein binding rate. RⅡ30mg · kg- Two-fold weighted two-compartment model fitting showed that T1 / 2β was 20.71 h, CLs was 0.34 L · kg-1 · h-1 and Vc was 0.99 L · kg-1. R Ⅱ 100 and 200 mg · kg-1po, respectively, and fitted by a one-compartment open model with T1 / 2Ke of 11.92 and 13.01 h, CLs of 0.87 and 0.77 L · kg -1 · h -1, Utilization was 39.7% and 46.4%. After RⅡ200mg · kg-1po7h, the content of RⅡ in intestine and stomach tissue was high, the content of RⅡ in blood, liver, ovary, kidney, heart, spleen, lung, testis, muscle and fat were less, After 24 hours, the content of each tissue decreased obviously, which indicated that RⅡis not easy to accumulate in the body. 120h mainly excreted via feces, the cumulative discharge rate of 34.4 ± s2.0%, less urine, bile excretion less cumulative excretion rates were only 1.1 ± s0.6% and 0.024 ± s0. 01%. The results of ultrafiltration showed that RⅡ plasma concentration was in the range of 45.94-103.22 mg · L-1, and R Ⅱ plasma protein binding rate was 46.6% -52.4%.