Development and application of a simple LC-MS method for the determination of plasma rilpivirine (TMC-278) concentrations

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  • Shibata Masaaki
    Department of Pharmacy, National Hospital Organization Nagoya Medical Center
  • Takahashi Masaaki
    Department of Pharmacy, National Hospital Organization Nagoya Medical Center
  • Yoshino Munehiro
    Department of Pharmacy, National Hospital Organization Osaka Medical Center
  • Kuwahara Takeshi
    Department of Pharmacy, National Cerebral and Cardiovascular Center Hospital
  • Nomura Toshiharu
    Department of Pharmacy, National Hospital Organization Nagoya Medical Center
  • Yokomaku Yoshiyuki
    Department of Clinical Research Center, National Hospital Organization Nagoya Medical Center
  • Sugiura Wataru
    Department of Clinical Research Center, National Hospital Organization Nagoya Medical Center

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Abstract

Rilpivirine (TMC-278) is a second-generation non-nucleoside reverse transcriptase inhibitor that is high potent against both wild-type and drug-resistant HIV-1 strains. Therefore, rilpivirine is expected to treat therapy-experienced patients who failed to use current drugs due to the emergence of drug-resistant HIV mutants. The quantification of rilpivirine in human plasma is important to support clinical studies and determine pharmacokinetic parameters of rilpivirine in HIV-1 infected patients. Consequently, simple and easy system to determine plasma rilpivirine concentrations has been required. In this study, we developed a conventional LC-MS method to quantify plasma rilpivirine. Subsequently the method was validated by estimating the precision and accuracy for inter- and intraday analysis in the concentration range of 18-715 ng/ml. The calibration curve was linear in this range. Average accuracy ranged from 100.0 to 100.6%. Relative standard deviations of both inter- and intraday assays were less than 3.3%. Recovery of rilpivirine was more than 82.0%. These results demonstrate that our LC-MS method provides a conventional, accurate and precise way to determine rilpivirine in human plasma. This method can be used in routine clinical application for HIV-1 infected patients, and permits management of drug interactions and toxicity for rilpivirine. J. Med. Invest. 60: 35-40, February, 2013

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