Irbesartan crystal forms: thermodynamic and dissolution properties study Artículo académico uri icon

Abstracto

  • Irbesartan is an anti-hypertensive drug practically insoluble in water and belongs to class II of the BCS. Solubility is a keyfactor in anti-hypertensive drugs because a rapid onset and increased extent of bioavailability after administration aredesirable [1]. It presents two crystal forms called A and B. However, in the Cambridge Structural Data Base onlycrystallographic data NOZWII: form B is reported [2]. Although commercial available products of this drug are formulatedwith polymorph A there are no reports related to its solubility properties and thermodynamic stability. Hence, in this workthe crystal structure of form A, the intrinsic dissolution rate and stability relationship between irbesartan polymorphs werestablished. Several crystallization methods and solid-state characterization techniques were applied to this drug.Crystal structure of irbesartan form A was determined through X-ray powder diffraction using synchrotron radiation. FormsA and B are related monotropically and form A showed more soluble than form B with an intrinsic dissolution rate of 0.017compared to 0.004 mg cm-2 min-1 of form B.

fecha de publicación

  • 2017