Highly Crystalline Forms of Valsartan with Superior Physicochemical Stability

Single
crystal structures of blockbuster antihypertensive drug Valsartan
are revealed
the first time in this report. Two new highly crystalline forms, named
form E and an ethanol solvate form F, were discovered and fully characterized
by PXRD, Raman, IR, TG, DSC, and DVS. Conformational flexibility and
single crystal structures are discussed in detail. Physicochemical
properties, such as hygroscopicity, chemical stability, crystallinity,
and dissolution behaviors, are compared with the marketed solid-state
form (amorphous state). The results show that the newly discovered
highly crystalline form E presents a remarkably different dissolution
behavior and superior chemical stability.