COMBINATION OF SGLT2 HIBITORS AND MINERAL CORTICOID RECEPTOR MODULATORS
Patent Information
- Authority / Receiving Office
- DE · DE
- Patent Type
- Patents
- Current Assignee / Owner
- ASTRAZENECA AB
- Filing Date
- 2023-08-31
- Publication Date
- 2026-06-17
AI Technical Summary
Existing formulations of mineralocorticoid receptor (MR) modulators and sodium-glucose cotransporter 2 (SGLT2) inhibitors face challenges in achieving physicochemical compatibility, mechanical stability, and maintaining patient compliance due to differences in solubility and permeability, which affect in-vitro dissolution and in-vivo bioavailability.
A fixed dose combination (FDC) formulation is developed, comprising MR modulator AZD9977 and SGLT2 inhibitor dapagliflozin in separate pellets with tailored coatings and binders to ensure compatibility and optimal dissolution profiles, packaged in a size 0 or 1 gelatin capsule.
The FDC formulation achieves comparable in-vitro dissolution and in-vivo bioavailability to separate dosages, providing greater therapeutic benefit for treating heart failure and chronic kidney disease without significant adverse effects like hyperkalemia, hypotension, acute kidney injury, or gynecomastia.