Investigating a Soluble Pharmaceutical Salt: Albendazole Hydrochloride
CRYSTAL GROWTH & DESIGN, 19 (8):
4538-4545 (2019)DOI: 10.1021/acs.cgd.9b00348
Abstract
Albendazole is an effective antihelmintic drug, which has an
unpredictable therapeutic response due to its low solubility in
biological fluids that limits its oral absorption. In an attempt to
improve solubility, albendazole hydrochloride, a soluble pharmaceutical
salt, was obtained and characterized by X-ray diffraction together with
magic angle spinning solid-state nuclear magnetic resonance
spectroscopy, Raman and Fourier transform infrared spectroscopies,
thermal analysis, energy-dispersive X-ray spectroscopy, and scanning
electron microscopy. These studies revealed that the crystalline habit
of albendazole hydrochloride is different from that of the albendazole
solid forms previously reported. The full structure was elucidated by
performing single-crystal X-ray diffraction. The characterization
studies showed the participation of the carbamate moiety in the salt
formation. In addition, the solubility studies showed a significant
increase in the solubility with respect to forms I and II of
albendazole. In conclusion, our results indicate that albendazole
hydrochloride can be an auspicious salt to be used as a new product in
an attempt to counteract unfavorable pharmaceutical properties.