Cheng Zhongzhe, Ding Lian, Zhang Yang, Chen Guiying, Chen Chang, Cheng Yi-Qiang, Jiang Hongliang
Tongji School of Pharmacy, Huazhong University of Science & Technology, 13 Hangkong Road, Wuhan, Hubei 430030, China.
Bioanalysis. 2015;7(1):39-52. doi: 10.4155/bio.14.264.
Thailandepsin B (TDP-B) is a potent histone deacetylase inhibitor under development. A reliable bioanalytical method for the quantification of TDP-B in plasma samples is required.
The stabilizer mixture containing hydrochloric acid, formic acid and dichlorvos was applied to stabilize TDP-B in matrix samples. The method validation was conducted over the curve range of 1.00 to 1000 ng/ml. The intrabatch and interbatch precision and accuracy of the quality control samples showed ≤10.9% relative standard deviation and -6.7% to 15.0% relative error. Moreover, a possible metabolite M of TDP-B was tentatively characterized.
A reliable LC-MS/MS method was developed and validated for the quantification of TDP-B and was successfully applied to a rat pharmacokinetic study.
泰国蛋白酶B（TDP-B）是一种正在研发的强效组蛋白去乙酰化酶抑制剂。需要一种可靠的生物分析方法来定量血浆样本中的TDP-B。
应用含有盐酸、甲酸和敌敌畏的稳定剂混合物来稳定基质样本中的TDP-B。在1.00至1000 ng/ml的曲线范围内进行方法验证。质量控制样品的批内和批间精密度和准确度显示相对标准偏差≤10.9%，相对误差为-6.7%至15.0%。此外，初步鉴定了TDP-B的一种可能代谢物M。
开发并验证了一种可靠的LC-MS/MS方法用于定量TDP-B，并成功应用于大鼠药代动力学研究。
