粉防己碱在体内的代谢转化

粉防已碱有多种药理作用,近年我国又发现它可以防治矽肺。薄层层析及高压液相层析结果表明,粉防己碱进入大鼠及人体内,大部分以原形存在,少部分被转化,在大鼠的肝、肺、尿及人尿中,代谢产物可能有两个粉防己碱-N-2′-氧化物异构体和N-2′-去甲基粉防己碱。在两个粉防己碱-N-2′-氧化物中,其一前人已有报道,另一个为新化合物,根据核磁共振谱、质谱以及它能还原成粉防己碱,确定了其化学结构。本文给出了粉防己碱的气相层析及高压液相层析的实验条件。

BIOTRANSFORMATION OF TETRANDRINE IN RATS AND IN MEN

Tetrandrine is a new antisilicosis drug used in this country. We have studied further its biotransformationAs standards, two tetrandrine-N-2'-oxide epimers and N-2'-nor-tetrandrine were prepared, one of the two oxide epimers is a new compound. Its structure was elucidated on the basis of chemical and spectral data (NMR, MS). The metabolites of tetrandrine in liver, lung and urine of rats and in urine of patients after oral administration of tetrandrine were compared with the standards by TLC and HPLC. The results showed that, in addition to tetrandrine itself, the above-mentioned metabolic products of tetrandrine were probably present in the organs and in urine. The content of tetrandrine-N-2'-oxide was about 9% of that of tetrandrine in rat liver, while the content of N-2'-nor-tetrandrine was about 7%.In this paper, the experimental conditions of GC and HPLC for tetrandrine were reported.