楼雅卿, 张宏, 曹霞, 陈孟来. 磷酸川芎嗪在狗和大鼠的药代动力学和体内命运J. 药学学报, 1986, 21(7): 481-487.
引用本文: 楼雅卿, 张宏, 曹霞, 陈孟来. 磷酸川芎嗪在狗和大鼠的药代动力学和体内命运J. 药学学报, 1986, 21(7): 481-487.
LOU Ya-Qing, ZHANG Hong, CAO Xia , CHEN Meng-Lai, . THE PHARMACOKINETICS AND DISPOSITION OF TETRAMETHYLPYRAZINE PHOSPHATE IN DOGS AND RATSJ. Acta Pharmaceutica Sinica, 1986, 21(7): 481-487.
Citation: LOU Ya-Qing, ZHANG Hong, CAO Xia , CHEN Meng-Lai, . THE PHARMACOKINETICS AND DISPOSITION OF TETRAMETHYLPYRAZINE PHOSPHATE IN DOGS AND RATSJ. Acta Pharmaceutica Sinica, 1986, 21(7): 481-487.

磷酸川芎嗪在狗和大鼠的药代动力学和体内命运

THE PHARMACOKINETICS AND DISPOSITION OF TETRAMETHYLPYRAZINE PHOSPHATE IN DOGS AND RATS

  • 摘要: 本文研究犬一次静注、肌注和口服磷酸川芎嗪的药代动力学和生物利用度并与盐酸川芎嗪进行比较。观察到磷酸川芎嗪属一级消除动力学,按一房室开放模型计算其各项动力学参数。证明静注、肌注和口服磷酸川芎嗪吸收较快、消除迅速。但肌注磷酸川芎嗪比盐酸川芎嗪吸收较好,血浆清除较慢,半衰期较长,肌注的生物利用度为81.68%。磷酸川芎嗪口服吸收较规律。大鼠ig磷酸川芎嗪吸收良好,组织分布广泛,以肝组织中含量最高。36 h内原形药从粪便和尿中共排出剂量的1.40%。

     

    Abstract: Studies on the pharmacokineties and bioavailability of tetramethylpyrazine phosphate (TMPP) after intravenous, intramuscular and oral administrations were carried out in comparision with tetramethylpyrazine hydrochloride (TMPH) in dogs. The drug concentration-time curves of both drugs were shown to fit a one compartment open model. The pharmacokinetic parameters were shown in tables 1~3. Better absorption, slower elimination, longer T 1/2 and greater absolute bioavailability of TMPP than those of TMPH were observed after IM administration of the drugs. The absorption of TMPP was more regular than that of TMPH when the drugs were given orally in small doses.TMPP was absorbed relatively completely and distributed in various tissues, especially in the liver. The excretion of unchanged drug in urine and feces was about 1.40% within 36 h after oral administration in rats.

     

/

返回文章
返回