The current research work reports a study on the degradation profile of tavaborole, which is an oxaborole antifungal drug used to treat infections in the toenails. This work also reports the chemical stability of tavaborole in different stress conditions along with the isolation and characterization of degradation products by high‐resolution mass spectrometry and two‐dimensional nuclear magnetic resonance techniques. A sensitive and reproducible stability‐indicating ultra‐performance liquid chromatography method was developed and validated for quantification of tavaborole bulk drug in the presence of degradation products. Significant degradation was observed during oxidative stress conditions using H₂O₂. It was observed that the drug was highly unstable under oxidation stress conditions and thus degradation profiles with various oxidizing reagents were studied. One unknown impurity (DP‐1) was formed during peroxide degradation, which was isolated by reverse‐phase preparative chromatography. The structure of this degradant was characterized by high‐resolution mass spectrometry and multidimensional nuclear magnetic resonance techniques. The structure of this novel impurity DP‐1 was identified as [4‐fluoro‐2‐(hydroxymethyl)phenol], which was not reported as a degradant in the literature. An Acquity BEH C₁₈, 100 × 2.1 mm, 1.7 μm column was used to achieve the desired separation within a shorter runtime of 4.0 min. The method was validated for specificity, precision, linearity and accuracy over the concentration range of 5.0–400 μg ml⁻¹ (r² −0.9999) and limit of quantitation 5.0 μg ml⁻¹. This method is compatible with LCMS analysis which enables to identify the unknown impurities formed in the process.

中文翻译：

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通过验证的稳定性证实了RP-UPLC方法对他巴硼烷的氧化降解曲线的研究：使用2D-NMR和HRMS分离和表征新型降解物

当前的研究工作报告了对他巴硼罗的降解情况的研究，后者是一种氧杂硼烷抗真菌药，用于治疗脚趾甲的感染。这项工作还报告了塔瓦伯络合物在不同应力条件下的化学稳定性，以及通过高分辨率质谱和二维核磁共振技术对降解产物的分离和表征。开发了灵敏且可重现的稳定性指示超高效液相色谱方法，并已验证该方法可在存在降解产物的情况下定量测定他波伯乐原料药的含量。在使用H ₂ O _2的氧化应激条件下，观察到明显的降解。观察到该药物在氧化应激条件下高度不稳定，因此研究了各种氧化剂的降解曲线。过氧化物降解期间形成了一种未知杂质（DP-1），该杂质通过反相制备色谱法分离。该降解物的结构通过高分辨率质谱和多维核磁共振技术表征。这种新型杂质DP-1的结构被鉴定为[4-氟-2-（羟甲基）苯酚]，在文献中没有报道其为降解物。无罪BEH C ₁₈使用100×2.1 mm，1.7μm的色谱柱，可在4.0分钟的较短运行时间内实现所需的分离。该方法进行了验证的特异性，精确度，线性度和精度在5.0-400微克毫升的浓度范围^-1（- [R ² -0.9999）和定量5.0微克毫升极限^-1。此方法与LCMS分析兼容，后者可以识别过程中形成的未知杂质。