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Development and Validation of a LC-MS/MS Assay for the Quantification Of Efavirenz In Different Biological Matrices


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.

Acceptance Date Sep 9, 2016
Publication Date Oct 1, 2016
Journal Bioanalysis
Print ISSN 1757-6180
Publisher Future Science
Pages 2125-2134
Keywords LC–MS/MS, brain tissue, efavirenz, plasma, protein binding
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