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研究盐酸他可林（ＴＨＡ）在大鼠体内的药物动力学。方法大鼠分别ｉｖ和ｉｇＴＨＡ４、８、１６ｍｇ．ｇ－１后，用反相高效液相色谱法测定其血药浓度，以ＣＡＰＰ软件拟合其房室模型。用平衡透析法测定血浆蛋白结合率。结果血药浓度—时间关系符合二室模型。静注低、中、高３个剂量后，ｔ１／２（分别为７２、６０、６５ｍｉｎ；曲线下面积（ＡＵＣ）分别为２０、３４、４７ｇｍｉｎ·Ｌ－１；清除率（ＣＬ）分别为０．０５３、０．０６２、０．０９０Ｌ·ｋｇ－１·ｍｉｎ－１，灌胃后ｔ１／２分别为６０、６３、６２ｍｉｎ；ＡＵＣ分别为７、１２、２１ｇｍｉｎ－１；ＣＬ分别为０．１５３、０．１５２、０．２４０Ｌ·ｋｇ－１·ｍｉｎ－１。血浆蛋白结合率为５２％。结论盐酸他可林在大鼠体内的消除较快，个体差异较大。
Pharmacokinetics of tacrine hydrochloride (THA) in rats was studied. Methods The rats were iv and igTHA4,8,16mg. g-1, the plasma concentration was determined by RP-HPLC, and the CAPP software was used to fit the atrioventricular model. Plasma protein binding rate was measured by equilibrium dialysis. Results plasma concentration - time relationship with the two-compartment model. After three doses of intravenous injection, t1 / 2 (72,60,65min, respectively); the area under the curve (AUC) were 20,34,47gmin · L-1; clearance rate (CL) .053,0.062,0.090L · kg-1 · min-1, respectively. The t 1/2 was 60, 63 and 62 min after instillation, respectively. The AUC values were 7, 12 and 21 gmin-1, respectively. , 0.152,0.240L · kg-1 · min-1, respectively.The plasma protein binding rate was 52% .Conclusion Tacrolimus hydrochloride is rapidly eliminated in rats, and the individual differences are large.