Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts

doi:10.1039/c8an01579a

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物质量控制与固体化学研究中心

	Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts
	Peng, Bo; Zhang, Zaiyong; Wang, Jian-Rong; Li, Meiqi; Zhang, Qi; Mei, Xuefeng
刊名	The Analyst
	2018-11-08
ISSN号	1364-5528
DOI	10.1039/c8an01579a
文献子类	Article
英文摘要	Discrimination of active pharmaceutical ingredients (APIs) existing as neutral molecules or salts is essential and complicated. However, the discrimination of pharmaceutical salts by confocal Raman micro-spectroscopy remains relatively poorly understood. In this paper, four new salts of triamterene (Tri) cocrystallized with nicotinic acid (NA), benzoic acid (BA), p-toluenesulfonic acid (TA), or isonicotinic acid (INA) were prepared and characterized comprehensively by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), polarized light microscopy (PLM), and dynamic vapor sorption (DVS). Ionized pteridine is identified by marker peaks in the confocal Raman micro-spectra that are characteristic of C[double bond, length as m-dash]N. The single crystal structures of Tri-NA·H2O and Tri-TA further demonstrate that a proton transfers from the carboxylic group of NA or TA to the pyrimidine N1 atom of Tri and their salts formation take place. The intrinsic dissolution rate (IDR) and apparent equilibrium solubility of these four salts are improved compared to the pure Tri component, especially for Tri-BA. This study provides a valuable insight into pharmaceutical salt discrimination by vibrational spectroscopy and presents that the combination of Tri with an acid can be a possible and promising alternative formulation of Tri.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/266263]
专题	药物质量控制与固体化学研究中心药物安全性评价中心
通讯作者	Peng, Bo; Zhang, Zaiyong; Wang, Jian-Rong; Li, Meiqi; Zhang, Qi; Mei, Xuefeng
作者单位	Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, P. R. China
推荐引用方式 GB/T 7714	Peng, Bo,Zhang, Zaiyong,Wang, Jian-Rong,et al. Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts[J]. The Analyst,2018.
APA	Peng, Bo,Zhang, Zaiyong,Wang, Jian-Rong,Li, Meiqi,Zhang, Qi,&Mei, Xuefeng.(2018).Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts.The Analyst.
MLA	Peng, Bo,et al."Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts".The Analyst (2018).