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Identification, synthesis, and characterization of potential genotoxic impurities of sildenafil citrate drug substance
Future Journal of Pharmaceutical Sciences ( IF 3.4 ) Pub Date : 2020-11-10 , DOI: 10.1186/s43094-020-00095-1
P. Rajesh Reddy , Sivanadh Musunuri , D. Rama Sekhara Reddy , V. Subrahmanyam Chittala , V. N. S. Murthy P , K. Krishnamohan

Sildenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specifil phophodiesterase type 5 (PDE5). Sildenafil enhances the effect of nitric oxide by inhibiting phosphodiesterase type 5, which is responsible for the degradation of cGMP in the corpus cavernosum. The possible genotoxic impurities of sildenafil were synthesized, i.e., sildenafil sulfonyl methyl ester, sildenafil sulfonyl ethyl ester, and sildenafil sulfonyl isopropyl ester. The present work describes the synthesis and characterization of these sulfonyl ester compounds related to sildenafil. All the synthesized sildenafil sulfonyl esters have proved to be beneficial for the pharmaceutical industry in view of the regulatory importance. A simple, efficient, and repeatable method was developed for the preparation of sildenafil sulfonyl esters in view of the regulatory importance of the potential genotoxic impurities in the active pharmaceutical ingredient. A detailed study of various impurities in sildenafil was conducted. Different process-related sulfonyl esters in sildenafil were identified, synthesized, and characterized by using various spectroscopic techniques like liquid chromatography-mass spectrometry (LCMS), mass, 1H NMR, and FT-IR. These efforts to synthesize and characterize them effectively have proved to be beneficial.

中文翻译:

枸sil酸西地那非原料药的潜在遗传毒性杂质的鉴定,合成和表征

西地那非是5型环鸟苷单磷酸(cGMP)-specifil磷酸二酯酶(PDE5)的选择性抑制剂。西地那非通过抑制5型磷酸二酯酶来增强一氧化氮的作用,5型磷酸二酯酶负责海绵体中cGMP的降解。合成了西地那非的可能的遗传毒性杂质,即西地那非磺酰基甲基酯,西地那非磺酰基乙基酯和西地那非磺酰基异丙基酯。本工作描述了与西地那非有关的这些磺酰基酯化合物的合成和表征。考虑到法规的重要性,所有合成的西地那非磺酰基酯都被证明对制药业是有益的。简单,高效,鉴于活性药物成分中潜在的遗传毒性杂质的管理重要性,开发了一种可重复的方法来制备西地那非磺酰基酯。对西地那非中的各种杂质进行了详细研究。西地那非中与过程相关的不同磺酰基酯已通过使用各种光谱技术(如液相色谱-质谱(LCMS),质量,1H NMR和FT-IR)进行鉴定,合成和表征。这些有效地合成和表征它们的努力被证明是有益的。并通过使用各种光谱技术进行表征,例如液相色谱-质谱(LCMS),质量,1H NMR和FT-IR。这些有效地合成和表征它们的努力被证明是有益的。并通过使用各种光谱技术进行表征,例如液相色谱-质谱(LCMS),质量,1H NMR和FT-IR。这些有效地合成和表征它们的努力被证明是有益的。
更新日期:2020-11-12
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