Development and validation of an LC-MS/MS assay for the quantification of efavirenz in different biological matrices

作者：Curley Paul; Siccardi Marco^*; Moss Darren M; Owen Andrew

来源：Bioanalysis, 2016, 8(20): 2125-2134.

DOI：10.4155/bio-2016-0021

• brain tissue
• efavirenz
• LC-MS/MS
• plasma
• protein binding

Aim: The non-nucleoside reverse transcriptase inhibitor efavirenz is one of the most prescribed antiretroviral therapeutics. Efavirenz-containing therapy has become associated with the occurrence of CNS side effects, including sleep disturbances, depression and even psychosis. Results: The investigation of efavirenz distribution required the development of a versatile and sensitive method. In addition to plasma, quantification was required in brain tissue and phosphate-buffered saline. The assay presented here was linear from 1.9 to 500 ng/ml. Accuracy and precision ranged between 93.7 and 99.5%, and 1.5 and 5.6%, respectively. Discussion: The method developed here represents a versatile, sensitive and easy-to-use assay. The assay has been applied to in vitro and in vivo samples demonstrating reliable efavirenz quantification in multiple matrices.

• 出版日期2016-10