PHYSICOCHEMICAL CHARACTERIZATION OF FUROSEMIDE MODIFICATIONS
PHYSICOCHEMICAL CHARACTERIZATION OF FUROSEMIDE MODIFICATIONS
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DOI：
10.1016/0378-5173(90)90185-7
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发表时间：
1990-04-20
影响因子：
5.8
通讯作者：
TATSUMI, E
中科院分区：
文献类型：
--
作者：
MATSUDA, Y;TATSUMI, E
采用X射线粉末衍射仪、差示扫描量热法、红外和傅立叶变换红外光谱、元素分析、热台显微镜和扫描电子显微镜对呋塞米的多晶型进行了研究和表征。Doherty和York(1988)报告的结果与目前的数据进行了高精度的比较分析，以确定两项研究之间的共同点和差异。前述作者只研究了两种晶型(一种稳定晶型和一种亚稳晶型)，与我们在晶型之外的五种新类型的修饰(两种晶型、两种溶剂型和一种非晶型)的研究结果形成了对比。在7种修饰中，在加热时观察到两种稳定形式(低温和高温稳定形式)之间的对映异向性，两种亚稳定形式直接转变为高温稳定形式，而在溶剂酸盐的情况下，情况涉及通过低温稳定形式的中间阶段进行。讨论了这四种晶型的热力学稳定性与活化能和转变热的关系。在这些修饰中，明显不同程度的物理化学光稳定性(显色)；虽然稳定晶型即使在强光照射下也不表现出明显的显色，但其他晶型非常容易着色。其中一种亚稳形式(形式(III))在溶解性能上远远超过任何其他晶体形式。
The polymorphism of furosemide has been extensively investigated and characterized using X-ray powder diffractometry, differential scanning calorimetry, infrared and Fourier transform infrared spectroscopy, elemental analysis, hot-stage microscopy and scanning electron microscopy. Comparative analysis of the results reported by Doherty and York (1988) with the present data were performed to a high degree of precision in order to determine the points of agreement and difference between the two studies. The aforementioned authors investigated only two polymorphs (one stable and one metastable from), contrasting with our findings of five new types of modification (two polymorphs, two solvates and one amorphous form) in addition to the crystal forms. Among the seven modifications, enantiotropism was observed between two stable forms (low- and high-temperature-stable forms) On heating, the two metastable forms underwent transformation directly to the high-temperature-stable form whereas the situation in the case of the solvates involved progression via the intermediate stage of the low-temperature-stable form. The thermodynamic stability of these four polymorphs is discussed in relation to the activation energy and heat of transformation. A distinctly different degree of physicochemical photostability (coloration) was evident among the modifications; although the stable form did not show significant coloration even when irradiated with intense light, the other crystal forms were very susceptible to coloration. One of the metastable forms (form (III)) far surpassed any of the other crystal forms in dissolution properties.