Stability Study of the Antihistamine Drug Azelastine HCl along with a Kinetic Investigation and the Identification of New Degradation Products

Abstract

The first stability-indicating HPLC method was developed and validated for azelastine HCl (AZL). The separation of AZL from its degradation products was achieved on a C18 column using acetonitrile-0.04 M phosphate buffer of pH 3.5 (32:68, v/v) as a mobile phase with UV-detection at 210 nm and naftazone as an internal standard. The method was rectilinear over the range of 0.2 -20.0 μg mL -1 with a detection limit of 7.05 ng mL -1 . The degradation behavior of AZL was studied under different ICH-recommended stress conditions along with a kinetic investigation; also, degradation products were identified by mass spectrometry. The method was applied for the quality control and stability assessment of AZL in eye drops and nasal spray. The obtained results were favorably compared with those obtained by a comparison method.

Validated sensitive spectrofluorimetric method for determination of antihistaminic drug azelastine HCl in pure form and in pharmaceutical dosage forms: application to stability study

“…From an economic point of view, the proposed method seems to be so simple, sensitive and fast. Scheme is the expected proposal for the degradation of AZL, as illustrated by Rania et al .…”

“…Moreover, our method is one of the most sensitive reported for the determination of AZL, permitting determination of the drug at the ng level and facilitating its quantitation in metered dose nasal sprays. The proposed method has been found to be ~20–50 times more sensitive than the previously reported method ; in addition, the proposed method does not require complicated set‐up, unlike another method reported in the literature that needs a sophisticated LC–MS instrument .…”

“…A review of the literature revealed several analytical methods for the determination of AZL in either its pure or dosage forms, including spectrophotometry (3)(4)(5), electrochemical methods (6,7), thin-layer chromatography (TLC) (8) highperformance liquid chromatography (HPLC) (9)(10)(11)(12) and liquid chromatography-tandem mass spectrometry (LC/MS/MS) (13,14). However, all these methods use expensive instruments and tedious procedures.…”

Quantitative proton nuclear magnetic resonance method for simultaneous analysis of fluticasone propionate and azelastine hydrochloride in nasal spray formulation

“…Reviewing the literature revealed that different analytical methods were established for determination of FLP and AZH either alone or in combination. These methods include: spectrophotometry [5][6][7][8][9][10][11][12], spectrofluorometry [13,14], electrochemical methods [15][16][17], TLC [18,19], HPLC [5,11,[20][21][22][23][24][25][26][27][28][29]] HPTLC [30][31][32], LC/MS/MS [33][34][35][36][37][38][39] and capillary electrophoresis [40,41]. It was found that only two spectrophotometric methods [42,43] and two HPLC methods [44,45] were reported for quantification of the binary mixture of FLP and AZH.…”

Efficient UPLC and CE methods for the simultaneous determination of azelastine hydrochloride and its genotoxic impurity

“…Similarly, various chromatographic methods have been published for estimation of AZL, including high‐pressure thin‐layer chromatography (Dubey, Das, Roychowdhury, Pradhan, & Ghosh, ; Kumar, Dwivedi, Kushnoor, & Kushnoor, ; Salama, Abdel‐razeq, Abdel‐atty, & El‐kosy, ; Sane, Joshi, Francis, Khatri, & Hijli, ; Wyszomirska, Czerwińska, Kublin, & Mazurek, ), capillary electrophoresis (CE; Koppenhoefer, Epperlein, Xiaofeng, & Bingcheng, ; Koppenhoefer, Jakob, Zhu, & Lin, ; Suzuki, Ishihama, Kajima, & Asakawa, ), HPLC (EL‐Shaheny & Yamada, ; Rao et al, ; Thangabalan & Kumar, ) and LC/MS (Heinemann, Blaschke, & Knebel, ; Park et al, ; Zha & Shum, ). All of these published methods, are not concerned with resolution and determination of AZL in presence of both BC and AZL genotoxic impurity.…”