Solubilization and Solid‐State Characterization of a Poorly Soluble 5‐α Reductase Inhibitor

January 2004 in “ Drug Development and Industrial Pharmacy ”

Haijian Zhu, Mark Sacchetti

5-alpha reductase inhibitor androgenetic alopecia GI197111X

TLDR GI197111X is best dissolved in Capmul MCM for trials.

GI197111X, a 5-alpha reductase inhibitor intended for treating androgenetic alopecia, was found to have low solubility at 25°C in all tested solvents suitable for animal and human use, with a solubility of 6.4 mg/mL in Capmul MCM being the only viable option for a soft gel dosage form in phase I/II trials. The study involved determining equilibrium solubilities, conducting a polymorph screen, and analyzing the crystal structure using a Bruker SMART diffractometer. The crystal structure was orthorhombic with specific unit cell dimensions and a calculated density of 1.248 g/cc. The molecule featured seven chiral centers, and single-crystal analysis confirmed the expected conformation or its enantiomer. The study also simulated and observed the crystal morphology, which matched closely with the calculated model.

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