Development and Validation of a Method for Determining Deferasirox in Human Blood Plasma by HPLC-UV

Introduction. Deferasirox is one of the most well-known complexing drugs chelators and is successfully used in chelating therapy for the treatment of excess iron in the human body. Deferasirox is also included in the list of vital and essential medicines, which indicates the importance of this drug for Russian healthcare. In this document, there are drugs only from a foreign manufacturer, therefore, within the framework of the trend towards import substitution, the development of deferasirox preparations of domestic production is a necessary and promising direction. In this connection, there is a need to develop a method that allows quantifying deferasirox in human blood plasma with minimal time and resource costs as part of a pharmacokinetic study.

Aim. The aim of this study is to develop a method for quantitative determination of deferasirox in human blood plasma by high performance liquid chromatography coupled with ultraviolet detection (HPLC-UV) for further bioequivalence studies.

Materials and methods. Determination of the deferasirox in human blood plasma was carried out by HPLC-UV. The method of proteins precipitation by acetonitrile was used as a sample preparation. Erlotinib solution was used as an internal standard. Mobile phase: 0.3 % solution of orthophosphoric acid in water, brought to pH 3.0 (eluent A) and 0.1 % solution of formic acid in acetonitrile (eluent B). Column was Symmetry®, 75 × 4,6 mm (Waters, США). Analytical range of the technique for deferasirox was 0.25–70.00 µg/ml in human blood plasma. Detection was carried out using a UV detector at an absorption wavelength of 299 ± 2 nm.

Results and discussion. This method was validated by selectivity, calibration curve, accuracy, precision, spike recovery, the lower limit of quantification, carry-over effect and stability.

Conclusion. A method of quantitative determination of deferasirox in human blood plasma was developed and validated by HPLC-UV. The analytical range was 0.25–70.00 µg/ml in human blood plasma. This method was used as part of a study of the pharmacokinetics and bioequivalence of deferasirox drugs.

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