Albendazole, an effective broad-spectrum anthelmintic agent, showed unpredictable therapeutic response caused by poor water solubility and slow dissolution rate. Then, novel binary and multicomponent supramolecular systems of two different solid forms of albendazole (I and II) with maltodextrin alone or with glutamic acid were studied as an alternative to improve the oral bioavailability of albendazole. The interactions and effects on the properties of albendazole were studied in solution and solid state. The solid systems were characterized using Raman and Fourier transform-infrared spectroscopy, thermal analysis, powder X-ray diffraction, and scanning electron microscopy. The solubility measurements, performed in aqueous and simulated gastric fluid, showed that albendazole (form II) was the most soluble form, while its supramolecular systems showed the highest solubility in simulated gastric fluid. On the other hand, the dissolution profiles of binary and multicomponent systems in simulated gastric fluid displayed pronounced increments of the dissolved drug and a faster dissolution rate compared to those of free albendazole forms. Thus, these supramolecular structures constitute an interesting alternative to improve the physicochemical properties of albendazole, with potential application for the preparation of pharmaceutical oral formulations.
ÁC 7 H 5 O 4 À , and BZMD-3,5-dihydroxybenzoic acid (3/1), 3C 13 H 13 N 3 O 4 ÁC 7 H 6 O 4 , and their crystalline structures elucidated, confirming the robustness of the selected synthon.
With the purpose
of enhancing the biopharmaceutical properties
of the furosemide, a pharmaceutical salt was obtained and characterized
by combining the drug and triethanolamine. The solid system was prepared
using different techniques such as kneading, grinding, and slow evaporation.
It was characterizated by X-ray powder diffraction, solid-state nuclear
magnetic resonance, infrared and Raman spectroscopy, thermal analysis,
and scanning electron microscopy. The results showed that the same
pharmaceutical compound in solid state was obtained through the different
preparation techniques. The crystalline structure was fully elucidated
by single-crystal X-ray diffraction. The salt formation was confirmed
by two-dimensional nuclear magnetic resonance experiments, which revealed
the transference of the OH proton of the drug to triethanolamine.
Besides, the solubility studies demonstrated an increase in the drug
solubility attributed not only to a pH change but also to a soluble
salt formation in solution. In addition, the combination of the drug
with triethanolamine produces an enhancement of the chemical photostability,
whereas the physical photostability and the hygroscopicity status
were not modified. Finally, this new solid form of furosemide constitutes
an interesting strategy to improve the biopharmaceutical properties
and stability of furosemide, with potential application in pharmaceutical
formulations.
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