Rapid fluorometric determination of ticagrelor in tablets and rat plasma: Application to pharmacokinetics study.

Abstract

The new antiplatelet drug ticagrelor has been determined based on its native fluorescence properties. These properties were studied and optimized to develop fast, simple and sensitive spectrofluorimetric method. The study included two approaches. The first approach is depending on measuring the native fluorescence at 300nm after excitation at 222nm. While the second approach combined synchronous and derivative scanning modes to measure ticagrelor at 286nm using Δ λ=100nm. Ticagrelor was measured in aqueous solution starting from the concentration of 200 to 5000ng/mL in both native and first derivative synchronous approaches. The developed methods were validated in accordance with ICH guidelines to be acceptable for quality control laboratories. Lowest concentrations that could be quantitated using the native and first derivative synchronous methods were 189 and 151ng/mL while lowest detectable concentrations were 63 and 50ng/mL, respectively. Moreover, the derivative synchronous fluorimetric approach was utilized to determine ticagrelor at 286nm in presence of other commonly co- administered drugs and the results demonstrate the enhanced selectivity of the proposed method. The same approach was also used to determine ticagrelor in rat plasma with acceptable recoveries. A preliminary pharmacokinetic study in rats was conducted and could be used to monitor plasma ticagrelor levels in humans.