期刊
JOURNAL OF CHROMATOGRAPHIC SCIENCE
卷 57, 期 10, 页码 874-880出版社
OXFORD UNIV PRESS INC
DOI: 10.1093/chromsci/bmz078
关键词
bioanalytical method; UHPLC; pharmacokinetics; efavirenz; AIDS
资金
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2011/11239-9, 2015/23843-9]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- National Institute of Science and Technology-Pharmaceutical Innovation (INCT-if)
- PADC-Programa de Apoio ao Desenvolvimento Cientifico da Faculdade de Ciencias Farmaceuticas (UNESP)
A simple and rapid ultra-high-performance liquid chromatography (UHPLC) method for determination of efavirenz (EFV) in plasma was developed and applied in a preclinical pharmacokinetic study. The method involves only addition of acetonitrile to precipitation of plasma proteins followed by solvent evaporation. The mobile phase consisted of methanol, acetonitrile and 0.1 M formic acid (20:50:30) at a flow rate of 0.3 mL/min with run time of 5 min. A CSH C18 column and a UHPLC-UV system operating at 245 nm were used. There was a linear response in the range of 0.078 to 10 mu g/mL, and the equation was obtained by weighting (1/x(2)) with r(2) = 0.9965. The pharmacokinetic disposition of EFV was investigated in rabbits (two groups, n = 7) following a single intravenous administration (IV group) at a dose of 2.7 mg/kg and a single oral administration (oral group) of EFV co-administered with lamivudine (3TC) and tenofovir (TNF) at a dose of 50, 25 and 25 mg, respectively. The study demonstrated the applicability of the method for determination of EFV in plasma without interference from other co-administered drugs, and the pharmacokinetic parameters were calculated. The method showed advantages over other methods in the literature, such as simplicity of sample processing and fast results.
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