Direct Visualization of in Vitro Drug Mobilization from Lescol XL Tablets Using Two-Dimensional F-19 and H-1 Magnetic Resonance Imaging

作者：Chen Chen; Gladden Lynn F; Mantle Michael D^*

来源：Molecular Pharmaceutics, 2014, 11(2): 630-637.

DOI：10.1021/mp400407c

• magnetic resonance imaging F-19 MRI
• USP-IV dissolution
• radial FLASH
• RARE
• controlled release
• multinuclear coimaging

This article reports the application of in vitro multinuclear (F-19 and H-1) two-dimensional magnetic resonance imaging (Mm) to study both dissolution media ingress and drug egress from a commercial Lescol XL extended release tablet in a United States Pharmacopeia Type IV (USP-IV) dissolution cell under pharmacopoeial conditions. Noninvasive spatial maps of tablet swelling and dissolution, as well as the mobilization and distribution of the drug are quantified and visualized. Two-dimensional active pharmaceutical ingredient (API) mobilization and distribution maps were obtained via F-19 MRI. F-19 API maps were coregistered with H-1 T-2-relaxation time maps enabling the simultaneous visualization of drug distribution and gel layer dynamics within the swollen tablet. The behavior of the MRI data is also discussed in terms of its relationship to the UV drug release behavior.

• 出版日期2014-2