AQbD-guided development of a robust and green SI-RP-HPLC method for impurity profiling of an efonidipine hydrochloride ethanolate and chlorthalidone combination, with LC-MS and NMR-based identification of degradation product in efonidipine.
Pranav S Bang, Vishnu P Choudhari, Vikram S Gharge
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引用次数: 0
Abstract
Efonidipine Hydrochloride Ethanolate (EHE) and Chlorthalidone (CTD) are co-formulated for the management of hypertension owing to their complementary pharmacological actions. Ensuring accurate impurity profiling in such combination formulations is vital for maintaining drug stability, safety and regulatory compliance. However, conventional analytical techniques often face challenges related to sustainability and robustness. Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) remains a key analytical approach for impurity determination, yet the integration of Quality by Design (QbD) principles into its development is still evolving. The present study focuses on developing a novel, sustainable RP-HPLC method for impurity profiling of EHE and CTD tablets using a QbD approach and green chemistry. Chromatographic separation was achieved on a Zorbax SB C8 column (150 mm × 4.6 mm, 5 µm). Critical method parameters such as mobile phase composition and pH were systematically optimized through QbD to enhance method robustness. A photolytic degradation product of EHE was identified as Efonidipine Related Compound A, and a plausible photolytic degradation pathway was proposed. A photolytic degradation product was identified in the LC-MS and its structure was confirmed through NMR spectroscopy. The developed green method exhibited excellent resolution, precision and reproducibility across multiple batches, allowing for effective separation and quantification of impurities. This green QbD-optimized, environmentally sustainable RP-HPLC method provides a reliable and scalable solution for impurity profiling in complex pharmaceutical formulations, aligning with modern quality control and regulatory expectations.
盐酸乙炔地平乙醇酸酯(EHE)和氯噻酮(CTD)由于其互补的药理作用而被共同配制用于高血压的治疗。确保这种组合制剂中准确的杂质分析对于维持药物稳定性、安全性和法规遵从性至关重要。然而,传统的分析技术经常面临与可持续性和稳健性相关的挑战。反相高效液相色谱法(RP-HPLC)仍然是杂质测定的关键分析方法,但将设计质量(QbD)原则整合到其发展中仍在不断发展。本研究的重点是建立一种新的、可持续的RP-HPLC方法,利用QbD方法和绿色化学对EHE和CTD片进行杂质分析。色谱分离采用Zorbax SB C8色谱柱(150 mm × 4.6 mm, 5µm)。通过QbD对流动相组成、pH等关键方法参数进行了系统优化,提高了方法的鲁棒性。确定了EHE的光解降解产物为依福尼地平相关化合物A,并提出了一个合理的光解降解途径。通过LC-MS鉴定了一种光解降解产物,并通过NMR对其结构进行了表征。所开发的绿色方法在多个批次中具有出色的分辨率、精密度和重复性,可以有效地分离和定量杂质。这种绿色qbd优化,环境可持续的RP-HPLC方法为复杂药物配方中的杂质分析提供了可靠和可扩展的解决方案,符合现代质量控制和监管期望。
期刊介绍:
The Journal of Chromatography A provides a forum for the publication of original research and critical reviews on all aspects of fundamental and applied separation science. The scope of the journal includes chromatography and related techniques, electromigration techniques (e.g. electrophoresis, electrochromatography), hyphenated and other multi-dimensional techniques, sample preparation, and detection methods such as mass spectrometry. Contributions consist mainly of research papers dealing with the theory of separation methods, instrumental developments and analytical and preparative applications of general interest.