Applicability of fluorescamine as a fluorogenic reagent for highly sensitive fluorimetric analysis of the tyrosine kinase inhibitor (avapritinib) in pharmaceuticals and biological samples

Abstract

Avapritinib (AVP) was the first precision drug to be approved by the US Food and Drug Administration (FDA) in 2020 for patients suffering from metastatic gastrointestinal stromal tumors (GISTs) and progressive systemic mastocytosis. The analysis of AVP in pharmaceutical tablets and human plasma was then carried out using a fast, efficient, sensitive, and simple fluorimetric method using a fluorescamine reagent. The procedure is based on the interaction between fluorescamine as a fluorogenic reagent and the primary aliphatic amine moiety in AVP using borate buffer solution at pH 8.8. The produced fluorescence was measured at 465 nm (Excitation at 395 nm). The calibration graph's linearity range was discovered to be 45.00–500.0 ng mL−1. Utilizing the International Council for Harmonization (ICH) and US‐FDA recommendations, the research technique was validated and bioanalytically validated. The proposed approach was effectively employed for determining the stated pharmaceuticals in plasma with a high percentage of recovery ranging from 96.87 to 98.09 and pharmaceutical formulations with a percentage of recovery equal to 102.11% ± 1.05%. In addition, the study was extended to a pharmacokinetic study of AVP with 20 human volunteers as a step for AVP management in therapeutic cancer centers.

A new green fluorimetric micelle complexation approach for reduction of the consumed solvent and quantification of avapritinib in biological fluids

“…The rate of recovery ± SD was 102.57 ± 0.45, with t -value and F -value equal to 1.21 and 2.43, respectively, compared with the detailed strategy. 8 …”

“…The spiked human plasma was subjected to the following procedure: using specific amounts of the cited drug standard working solution (0.50–4.0 μg mL −1 ), 1.0 mL of the drug-free plasma was spiked. As a protein precipitator, one millilitre of acetonitrile was included in mixture, 8 which was then diluted with distilled water to 10.0 mL and centrifuged at 4000 rpm for approximately 15 minutes. The analytical technique used one millilitre of the supernatant.…”