College of Pharmacy, Duksung Women's University, Seoul, Korea.
Arch Pharm Res. 2012 May;35(5):861-6. doi: 10.1007/s12272-012-0511-2. Epub 2012 May 29.
The polymorphic forms of a new PDE-5 inhibitor DA-8159 were prepared and characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TG). Two crystal forms and one amorphous form of DA-8159 have been isolated by recrystallization and characterized by DSC, TG and PXRD. From the TG data it was confirmed that two crystal forms are neither solvates nor hydrates. The PXRD patterns of the two crystal forms were different. In the dissolution studies in simulated intestinal fluid at 37 ± 0.5°C, the solubility decreased in the order of amorphous form > Form 1 > Form 2. After storage of 60 days, Form 1 was transformed to Form 2. Form 2 was not transformed. The amorphous form was transformed to Form 2 at 52% R.H. and 95% R.H., but it did not transform at 0% R.H.
新型 PDE-5 抑制剂 DA-8159 的多晶型物通过差示扫描量热法（DSC）、粉末 X 射线衍射法（PXRD）和热重分析（TG）进行了制备和表征。通过重结晶分离得到了 DA-8159 的两种晶型和一种无定形物，并通过 DSC、TG 和 PXRD 进行了表征。从 TG 数据可以确认，两种晶型既不是溶剂化物也不是水合物。两种晶型的 PXRD 图谱不同。在 37±0.5°C 的模拟肠液中的溶解研究中，无定形物的溶解度>晶型 1>晶型 2。储存 60 天后，晶型 1转变为晶型 2。晶型 2未发生转变。无定形物在 52%RH 和 95%RH 下转化为晶型 2，但在 0%RH 下不发生转化。
