An eco‐friendly direct spectrofluorimetric method for the determination of irreversible tyrosine kinase inhibitors, neratinib and pelitinib: application to stability studies

Abstract

A new rapid and simple stability-indicating spectrofluorimetric method has been developed for the determination of two irreversible tyrosine kinase inhibitors (TKIs), neratinib (NER) and pelitinib (PEL). The method is based upon measurement of the native fluorescence intensity of both drugs at λ 270 nm in aqueous borate buffer solutions (pH 10.5). The fluorescence intensity recorded at 545 nm (NER) and 465 nm (PEL) were rectilinear over the concentration range of 0.1-10 μg/mL for both drugs with a high correlation coefficient (r > 0.999). The proposed method provided low limits of detection and of quantitation of 0.07, 0.11 μg/mL (NER) and 0.02, 0.05 μg/mL (PEL), respectively. The method was successfully applied for the determination of NER and PEL in bulk powder. The proposed methods were fully validated as per the International Conference on Harmonisation (ICH) guidelines. The application of the method was extended to stability studies of both NER and PEL under different forced-degradation conditions (acidic-induced, base-induced, oxidative, wet heat, and photolytic degradation). Moreover, the kinetics of the base-induced and oxidative degradation of both drugs was investigated and the pseudo-first-order rate constants and half-lives were estimated at different temperatures. Also, an Arrhenius plot was applied to predict the stability behaviour of the two drugs at room temperature. Copyright © 2016 John Wiley & Sons, Ltd.

LC–MS/MS assay for the quantitation of the tyrosine kinase inhibitor neratinib in human plasma

“…More recently, one publication reports a fluorescence assay for neratinib in buffers with an LLQ of 100 ng/mL [18], and another reports an UPLC-MS/MS assay for bioanalytical purposes [19]. The latter assay utilized double the plasma volume for a 4-fold shorter assay range of 4-500 ng/mL, with a 2-step protein precipitation, had a shorter run-time, and utilized crizotinib as internal standard.…”

Micelle‐enhanced direct spectrofluorimetric method for the determination of linifanib: Application to stability studies

“…The degradation was found to follow pseudo-first order kinetics. The rate constant (k) and half-life (t 1/2 ) for the alkaline degradation of LNF were calculated using the following equations [26,[33][34][35][36] ; slope ¼ -k=2:303…”

“…Generally, spectrofluorimetric techniques are characterized by high sensitivity and selectivity, in addition to other advantages such as simplicity, low detectability, wide linear ranges and rapid analysis. Moreover, fluorescence spectroscopy is an adaptable analytical technique and is more sensitive than other detection systems such as classical ultraviolet (UV) absorption, is time‐saving compared with high‐performance liquid chromatography (HPLC), and is less expensive than LC–MS/MS detection . Thus, fluorescence spectroscopy was used in this study.…”

“…Moreover, fluorescence spectroscopy is an adaptable analytical technique and is more sensitive than other detection systems such as classical ultraviolet (UV) absorption, is time-saving compared with high-performance liquid chromatography (HPLC), and is less expensive than LC-MS/MS detection. [23][24][25][26] Thus, fluorescence spectroscopy was used in this study.…”

Spectrophotometric Investigations of Charge Transfer Complexes of Tyrosine Kinase Inhibitors with Iodine as a σ-Electron Acceptor: Application to Development of Universal High-Throughput Microwell Assay for Their Determination in Pharmaceutical Formulations

“…An appropriate analytical method is needed for TKI quality control (QC). Chromatographic methods including high-performance liquid chromatography (HPLC) [18][19][20][21][22][23] and high-performance thinlayer chromatography (HPTLC) [24][25][26][27] as well as other techniques such as voltammetry [28], spectrofluorimetry [29][30][31][32], and spectrophotometry [33][34][35][36][37][38][39][40][41][42][43][44] have all been reported as methodologies for the QC of TKIs in pharmaceutical formulations. Because of its simplicity, low cost, and widespread availability in QC laboratories, spectrophotometry is the most practical analytical method.…”