Najib Mohd Nadzri Mohd, Back Kevin, Edkins Katharina
School of Pharmacy, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, UK.
School of Medicine, Pharmacy and Health, Durham University, University Boulevard, Stockton-on-Tees, TS17 6BH, UK.
Chemistry. 2017 Dec 6;23(68):17339-17347. doi: 10.1002/chem.201703658. Epub 2017 Nov 14.
Pharmaceutical sodium salts are prone to incorporate water into their crystal structures. The model compound diatrizoic acid monosodium salt, an X-ray contrast agent, has been investigated in depth towards its interaction with water in the solid state. Five hydrates with water content ranging from 0.3 to 8 molar equivalents of water show a high degree of interconvertibility, stoichiometric and non-stoichiometric behaviour, and potential of amorphisation during release of water. A DMSO/water mixed solvate further highlights the high attraction of this salt to incorporate water. All incorporated solvent coordinates to the sodium cation and can further interact and stabilise the respective crystal forms by hydrogen bonding. DTS thus highlights the importance of an in-depth investigation of sodium salts used pharmaceutically to guarantee dose uniformity and stability of final formulation.
药用钠盐易于在其晶体结构中结合水。作为一种X射线造影剂的模型化合物泛影酸单钠盐，已对其在固态下与水的相互作用进行了深入研究。五种水合物的含水量从0.3到8摩尔当量的水，表现出高度的相互转化性、化学计量和非化学计量行为，以及在水释放过程中发生非晶化的可能性。一种二甲基亚砜/水混合溶剂化物进一步突出了这种盐结合水的高吸引力。所有结合的溶剂都与钠离子配位，并可通过氢键进一步相互作用并稳定各自的晶体形式。因此，DTS强调了深入研究药用钠盐以确保最终制剂剂量均匀性和稳定性的重要性。
