Selection of excipients for the formulation of varenicline tablet cores

V. Eremin, E. V. Blynskaya, S. Tishkov
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Abstract

The active pharmaceutical ingredient (APS) of varenicline is a tartrate with the chemical name 7,8,9,10‑Tetrahydro-6,10‑Methano-6H-pyrazino(2,3‑h) (3)benzazepine (as tartrate). Varenicline free base is an achiral molecule, however varenicline tartrate, which is formed by the reaction of varenicline free base and L-tartaric acid, is optically active and has an absolute counterion configuration of 2R, 3R. At the moment, only the drug Champix, produced by the pharmaceutical company Pfizer, is represented among direct analogues, so the development of a domestic analogue is an urgent topic of research. The purpose is to develop the optimal composition of varenicline tablet cores to create a finished dosage form.
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选择用于配制伐尼克兰片芯的辅料
伐伦克林的活性药物成分(APS)是酒石酸盐,化学名称为 7,8,9,10-四氢-6,10-甲桥-6H-吡嗪并(2,3-h) (3)苯并氮杂卓(酒石酸盐)。伐伦克林游离碱是一种非手性分子,但伐伦克林酒石酸盐是由伐伦克林游离碱和 L-酒石酸反应生成的,具有光学活性,其绝对反离子构型为 2R、3R。目前,直接类似物中只有辉瑞制药公司生产的药物 Champix,因此开发国产类似物是一项紧迫的研究课题。其目的是开发出最佳的伐尼克兰片芯成分,以制成成品剂型。
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