Solid state of a new PDE-5 inhibitor DA-8159: characterization, dissolution, transformation.
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.
College of Pharmacy, Duksung Women's University, Seoul, Korea.
Ji Yoon
JY
Ryu
Young-Taek
YT
Sohn
D018938:Caco-2 Cells; D006801:Humans; D058986:Phosphodiesterase 5 Inhibitors / Q000737:chemistry* / Q000378:metabolism*; D011743:Pyrimidines / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility; D013449:Sulfonamides / Q000737:chemistry* / Q000378:metabolism*; D014961:X-Ray Diffraction; D000096926:Benzenesulfonamides
D058986:Phosphodiesterase 5 Inhibitors; D011743:Pyrimidines; D013449:Sulfonamides; C419664:udenafil; D000096926:Benzenesulfonamides