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用高效液相色谱法对家兔单剂量ig750mg新抗炎镇痛剂3H-1,2二氢-2-(4-甲基苯胺基)-甲基-1-吡咯里嗪酮(Z-47)后尿中的代谢物进行了分离、检测。根据代谢物的色谱行为及与Z-47结构有关的其它药物的代谢途径,推测Z-47羧基衍生物[4-(3H-1,2-二氢-1-吡咯里嗪酮-2-甲基胺基)苯甲酸]是一可能的代谢产物,遂用化学方法合成了该衍生物。利用色谱保留值、紫外双波长吸收比值等对代谢物和标准品进行比较,并对尿样的酶水解产物进行色谱分析,证实Z-47羧基衍生物及其酯型β-D-葡糖苷酸结合物是Z-47在家兔体内的主要代谢产物。
The high-performance liquid chromatography (HPLC) was used to evaluate the effect of a single dose of ig750mg rabbit anti-inflammatory analgesic 3H-1,2-dihydro-2- (4-methylanilino) ) After urinary metabolites were isolated and tested. According to the chromatographic behavior of metabolites and the metabolic pathways of other drugs related to the structure of Z-47, it is presumed that the Z-47 carboxyl derivative [4- (3H-1,2-dihydro-1-pyrrolizinone- Amino) benzoic acid] is a possible metabolite, then the chemical synthesis of the derivative. The metabolites and standards were compared by the chromatographic retention and ultraviolet dual-wavelength absorption ratio, and the enzymatic hydrolyzate of urine samples was analyzed by chromatography to confirm that the Z-47 carboxyl derivative and its ester β-D-glucuronide The conjugate is the major metabolite of Z-47 in rabbits.