Fei Fei, Yang Hailing, Peng Ying, Wang Pei, Wang Shuyao, Zhao Yuqing, Huang Jingqiu, Yu Xiaoyi, Feng Siqi, Sun Runbin, Yang Na, Wang Hongbo, Aa Jiye, Wang Guangji
Jiangsu Province Key Laboratory of Drug Metabolism and Pharmacokinetics, Jiangsu Key laboratory of drug design and optimization, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Tongjiaxiang 24, Nanjing 210009, PR China.
Lansen Pharmaceutical Holdings Co. Ltd, Ningbo 315174, PR China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jun 1;1022:30-37. doi: 10.1016/j.jchromb.2016.04.005. Epub 2016 Apr 2.
A sensitive and reliable method using liquid chromatography tandem mass spectrometry (LC-MS/MS) was established for the simultaneous assay of paeoniflorin and albiflorin in bio-samples of rats after liquid-liquid extraction with ethylacetate. For the first time, the developed method was validated and successfully applied to the pharmacokinetics study of paeoniflorin and albiflorin after oral administration of Total Glucosides Of White Paeony Capsule (TGP). Relative to the intravenous injection, the absolute bio-availabilities of paeoniflorin and albiflorin were 2.8 and 1.7%, while their excretion in feces was 43.06 and 40.87%, respectively. Both paeoniflorin and albiflorin showed dose-dependent exposure in plasma, with a half-life of approximately 1.8h. No significant differences were observed between a single equal dose of paeoniflorin or albiflorin and that of TGP for the pharmacokinetic parameters, including AUC, T1/2 and Cmax. Paeoniflorin and albiflorin were exposed at high levels in immune relevant organ/tissues, such as the spleen, thymus and bone, which could facilitate immuno-regulatory activities.
建立了一种灵敏可靠的液相色谱串联质谱法(LC-MS/MS),用于在大鼠生物样品经乙酸乙酯液液萃取后同时测定芍药苷和 albiflorin。首次对所建立的方法进行了验证,并成功应用于白芍总苷胶囊(TGP)口服给药后芍药苷和 albiflorin 的药代动力学研究。相对于静脉注射,芍药苷和 albiflorin 的绝对生物利用度分别为 2.8%和 1.7%,而它们在粪便中的排泄率分别为 43.06%和 40.87%。芍药苷和 albiflorin 在血浆中均呈现剂量依赖性暴露,半衰期约为 1.8 小时。对于包括 AUC、T1/2 和 Cmax 在内的药代动力学参数,单剂量相等的芍药苷或 albiflorin 与 TGP 之间未观察到显著差异。芍药苷和 albiflorin 在免疫相关器官/组织(如脾脏、胸腺和骨骼)中高水平暴露,这可能有助于免疫调节活性。