摘要
目的对脑血宁注射液的血清药物化学及药动学进行初步研究。方法建立脑血宁注射液及其静脉给药后人血清HPLC指纹图谱的分析方法,鉴定给药后血清中的主要药物化学成分及来源生药,并对主要化学成分的药物动力学进行研究。结果静脉滴注脑血宁注射液后,从人血清中检测到3种化合物,其中2种为脑血宁注射液所含原形成分,分别为丹皮酚和栀子苷;1种为新产生的代谢产物。丹皮酚和栀子苷人体内的药物动力学研究显示,静脉注射给药后,栀子苷在人体内血药浓度迅速下降,其药时过程符合一室模型,给药后70%以原型由肾脏清除;丹皮酚在人体的血浆药物浓度时间曲线过程符合二室模型,给药后,在体内广泛代谢,只有占给药量0.04%的丹皮酚以原形从尿液排出。结论血中所含化学成分为脑血宁注射液体内直接作用物质,对其进行深入的研究将有助于阐明脑血宁注射液的有效成分及作用机制。
Objective To study the serum pharmacochemistry and pharmacokinetics of Naoxuening Injection（NXI）. Methods Based on the established HPLC fingerprint of NXI, analysis and comparison were carried out among the HPLC profiles of NXI, blank plasma and human serum samples obtained after intravenous administration of NXI. and the main compounds were identified and then the pharmacokinetics of the main compounds were studied. Results Three compounds were i- dentified from the serum after intravenous administration of NXI. Two were the compounds containing in NXI, which were named after geniposide and paeonol, respectively. The other one was identified as metabolic product. The concentration-time curve of geniposide in blood accorded with one - compartment model of pharmacokinetics, and 70 % of geniposie was cleared from the kidney. The concentration - time curve of paenol in blood accorded with two - compartment model of pharmacoki- netics, and 0. 04 % of geniposie was cleared from the kidney. Conclusion The compounds contained in the blood and their metabolites are the effective constituents, and the further serum pharmacochemical research will be beneficial to the pharmacol- ogy and the therapeutic mechanism of of NXI.
出处
《中药新药与临床药理》
CAS
CSCD
2008年第5期376-379,共4页
Traditional Chinese Drug Research and Clinical Pharmacology
