Abstract：
Background: A chiral HPLC technique was developed to determine sitagliptin phosphate enantiomers in rat plasma in compliance with US FDA regulations. Methods & results: The technique used a Phenomenex column with a mobile phase consisting of a 60:35:5 (v/v/v) blend of pH4, 10-mM ammonium acetate buffer, methanol and 0.1% formic acid in Millipore water. The precision for both (R) and (S) sitagliptin phosphate varied between 0.246 and 1.246%, while the accuracy was 99.6-100.1%. A glucose uptake assay was used to assess enantiomers in 3T3-L1 cell lines through flow cytometry. Conclusion: Investigation of the pharmacokinetic impacts of sitagliptin phosphate racemic enantiomers in rat plasma revealed notable contrasts in R and S enantiomers in female albino Wistar rats, suggesting enantioselectivity for sitagliptin phosphate.
摘要：
背景：开发了一种手性HPLC技术来测定大鼠血浆中的磷酸西格列汀对映体，符合美国FDA的规定。方法和结果：该技术使用Phenomenex柱，流动相由60:35:5（v/v/v）的pH4，10mM乙酸铵缓冲液，甲醇和0.1%甲酸的Millipore水溶液。磷酸（R）和（S）西格列汀的精密度在0.246和1.246%之间变化，而准确度为99.6-100.1%。葡萄糖摄取测定用于通过流式细胞术评估3T3-L1细胞系中的对映异构体。结论：研究磷酸西格列汀外消旋对映体在大鼠血浆中的药代动力学影响显示，雌性白化病Wistar大鼠的R和S对映体存在明显差异，提示磷酸西格列汀的对映选择性。
