Else Laura J, Tjia John, Jackson Akil, Penchala Sujan Dilly, Egan Deirdre, Boffito Marta, Khoo Saye H, Back David J
Liverpool Bioanalytical Facility, Department of Molecular & Clinical Pharmacology, University of Liverpool, Liverpool, UK.
Bioanalysis. 2014;6(14):1907-21. doi: 10.4155/bio.14.59.
A sensitive, specific and robust liquid chromatography-tandem mass spectrometry method has been developed and validated for the quantification of rilpivirine in human plasma, genital/rectal biofluids and mucosal tissues.
Plasma and tissue samples were extracted using protein precipitation (acetonitrile/water; 5:1 v/v), and genital/rectal biofluids absorbed onto ophthalmic swabs were extracted using liquid-liquid extraction (hexane/ethyl acetate; 80:20 v/v). A stable isotope-labeled internal standard ((13)C-d4-RPV) was used, and the assay was validated over a concentration range of 0.5-400 ng/ml.
Inter- and intra-assay precision and accuracy met the acceptance as per US FDA bioanalytical guidelines. The validated assay has been used for the determination of rilpivirine concentrations in these matrices as part of an exploratory pharmacokinetic study investigating the suitability of a long-acting formulation of rilpivirine for pre-exposure prophylaxis.
已开发并验证了一种灵敏、特异且稳健的液相色谱-串联质谱法，用于定量测定人血浆、生殖器/直肠生物流体及黏膜组织中的利匹韦林。
血浆和组织样本采用蛋白沉淀法（乙腈/水；5:1 v/v）提取，吸附在眼科拭子上的生殖器/直肠生物流体采用液-液萃取法（己烷/乙酸乙酯；80:20 v/v）提取。使用稳定同位素标记的内标物（(13)C-d4-RPV），该测定法在0.5 - 400 ng/ml的浓度范围内进行了验证。
批间和批内精密度及准确度符合美国食品药品监督管理局生物分析指南的验收标准。作为一项探索性药代动力学研究的一部分，该经过验证的测定法已用于测定这些基质中的利匹韦林浓度，该研究旨在调查长效利匹韦林制剂用于暴露前预防的适用性。
