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出 处:《沈阳药科大学学报》1998年第1期13-17,共5页Journal of Shenyang Pharmaceutical University
基 金:国家自然科学基金
摘 要:建立了家兔尿中SFZ-47及其两种主要代谢产物SFZ-47羧基衍生物(M1)及该衍生物的酯型β-D-葡糖苷酸(M2)的 HPLC测定方法,并用该法对单剂量口服230mg SFZ-47的 3只家兔尿样进行了定量分析.结果表明:在0~24h内,SFZ-47,MI和M2的累积排泄量分别占给药剂量的(8.3±0.48)%,(18.93±2.66)%和(23.42±8.00)%.The major metabolites of 3H-l,2-dihydro-2-(4-methylphenylamino)methyl-1-pyrro- lizinone(SFZ-47) in rabbits, a new anti-inflammatory and analgesic agent are 4-(3H-1,2-dihy- dro-1-pyrrolizinone-2-methylamino) benzoic acid(M1) and its acyl β-D-glucuronide(M2).A HPLC method for the quantitative determination of SFZ-47 and its two major metabolites in rabbit urine was developed in terms of specificity,precision,and accuracy,and was found to be reliable and reproducible.In three rabbits after a 230 mg p.o. dose of SFZ-47,the analytical results showed that the excretion rate of the parent drug was (8.90±0.48)% of the total dose administrated in 24 h,while those of M1 and M2 were (18.93±2.66)% and (23.42±8 .00) %, respectively.
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