曾衍霖, 张昌绍. 防治血吸虫病药物的研究 ⅩⅩⅩ.酒石酸锑钾在体内的分解J. 药学学报, 1963, 10(9): 519-524.
引用本文: 曾衍霖, 张昌绍. 防治血吸虫病药物的研究 ⅩⅩⅩ.酒石酸锑钾在体内的分解J. 药学学报, 1963, 10(9): 519-524.
ZENG YAN-LIN AND JANG CHANG-SHAW, . STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅩⅩ. THE CLEAVAGE OF POTASSIUM ANTIMONY TARTRATE IN ANIMAL BODYJ. Acta Pharmaceutica Sinica, 1963, 10(9): 519-524.
Citation: ZENG YAN-LIN AND JANG CHANG-SHAW, . STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅩⅩ. THE CLEAVAGE OF POTASSIUM ANTIMONY TARTRATE IN ANIMAL BODYJ. Acta Pharmaceutica Sinica, 1963, 10(9): 519-524.

防治血吸虫病药物的研究 ⅩⅩⅩ.酒石酸锑钾在体内的分解

STUDIES ON ANTIBILHARZIAL DRUGS ⅩⅩⅩ. THE CLEAVAGE OF POTASSIUM ANTIMONY TARTRATE IN ANIMAL BODY

  • 摘要: 酒石酸锑钾(PAT)分子中锑及酒石酸是等当量的。如果它们在体内过程中变为不相等,便可证明PAT已有分解。本文根据这一设想,测定了PAT经尿与胆汁排泄以及进、出血细胞过程中锑及酒石酸的定量关系。兔静脉注射PAT后,6小时内尿中锑的排泄率为18%而酒石酸的排泄率则高达91%以上。给药后1小时内胆汁中排出酒石酸极少,但锑的排出量很高,达给药量的29%。尿及胆汁排泄过程中,锑与酒石酸当量间变为明显的不相等,可以说明PAT在体内已部分发生分解。狗血加PAT体外恒温1小时后,血浆锑量下降约一半,血细胞锑量相应增高,而血浆中酒石酸量则几无改变。狗血加PAT温孵1(1/2)小时后,以Locke液代替血浆让锑再出血细胞,结果Locke液中锑量为酒石酸量的5.7倍。锑与酒石酸两部分的数量变化缺乏平行关系,说明在进、出血细胞的过程中,也有部分PAT发生分解;并提示血液或为PAT分解的重要器官之一。

     

    Abstract: The PAT molecule consists of Sb and tartaric acid components in equimolar amounts.If the equimolarity no longer exists after metabolism, it can be inferred that a cleavage of PAT must have taken place. From the view point of the chemistry of complex compounds, an in vivo cleavage of PAT molecules is quite a possibility as a result of the new equilibrium established between the ligands and centric ions in the serum. This paper deals with the quantitative relationship between the Sb and tartaric acid components of PAT during excretion into urine and bile, and during their influx into and efflux from the blood cells. Our results all showed that the molar concentration of Sb was not equal to that of tartaric acid, indicating the occurrence of an in vivo cleavage of PAT. After a single dose of 30 mg of PAT was administered intravenously to rabbits, tartaric acid elimination in urine was almost complete in about 6 hours, while the Sb excretion was so low that it amounted to only 18% of the total dose administered. On the other hand, the biliary excretion of tartaric acid was very low during the first hour after PAT administration, meanwhile as much as 29% of the administered Sb appeared in the bile. In the experiments of the influx into the blood cells, dog's blood was incubated in vitro with PAT. The amount of Sb remaining in the serum decreased to about half of the original level at one hour after the addition of PAT, and the Sb contents of the blood cells rose correspondingly, but the quantity of tartaric acid in the serum remained nearly unchanged. In the experiments of the efflux from the blood cells, serum was removed after dog's blood was incubated with PAT for 1(1/2) hours, then Locke solution was added instead of serum. It was found that the ratio of Sb and tartaric acid molarities in Locke solution was 5.7±2.5 at the end of the second 1(1/2) hour period. The fact that the quantitative changes of Sb and tartaric acid did not run parallel to each other during the above processes, revealed that the cleavage of PAT molecule could also take place in vitro and suggested that the blood might be one of the important tissues in which the in vivo cleavage occurred.

     

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