%0 Journal Article %1 WOS:000424977500015 %A de Oliveira, Yara Santiago %A Oliveira, Alcemira Conceicao %A Ayala, Alejandro Pedro %C RADARWEG 29, 1043 NX AMSTERDAM, NETHERLANDS %D 2018 %I ELSEVIER %J EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES %K Amorphous; Crystalline; Grinding} Solvate; hydrochloride; {Raloxifene %P 146-154 %R 10.1016/j.ejps.2017.11.028 %T Mechanochemically induced solid state transformations: The case of raloxifene hydrochloride %V 114 %X Raloxifene hydrochloride is a benzothiophene derivative mainly used in the prevention and treatment of osteoporosis, but exhibits a low bioavailability hindered by its poor water solubility. In this study, a mechanochemical approach based on neat and liquid-assisted grinding was applied to produce new solid forms of raloxifene hydrochloride. The solids obtained were characterized by several solid-state techniques, such as powder X-ray diffraction, thermal analysis, infrared and Raman spectroscopy. These results showed that depending on the processing conditions solvated or amorphous forms can be produced. The thermal stability of the new forms was also investigated showing that the new forms convert back into the raw material form, as observed by Raman spectroscopy, which was successfully used to discriminate amorphous and crystalline forms, as well as, to monitor in situ the recrystallization process. Furthermore, the solubility of the new forms was evaluated, showing the clear advantage of the amorphous form, when compared with the currently marketed salt.

@article{WOS:000424977500015, abstract = {Raloxifene hydrochloride is a benzothiophene derivative mainly used in the prevention and treatment of osteoporosis, but exhibits a low bioavailability hindered by its poor water solubility. In this study, a mechanochemical approach based on neat and liquid-assisted grinding was applied to produce new solid forms of raloxifene hydrochloride. The solids obtained were characterized by several solid-state techniques, such as powder X-ray diffraction, thermal analysis, infrared and Raman spectroscopy. These results showed that depending on the processing conditions solvated or amorphous forms can be produced. The thermal stability of the new forms was also investigated showing that the new forms convert back into the raw material form, as observed by Raman spectroscopy, which was successfully used to discriminate amorphous and crystalline forms, as well as, to monitor in situ the recrystallization process. Furthermore, the solubility of the new forms was evaluated, showing the clear advantage of the amorphous form, when compared with the currently marketed salt.}, added-at = {2022-05-23T20:00:14.000+0200}, address = {RADARWEG 29, 1043 NX AMSTERDAM, NETHERLANDS}, author = {de Oliveira, Yara Santiago and Oliveira, Alcemira Conceicao and Ayala, Alejandro Pedro}, biburl = {https://www.bibsonomy.org/bibtex/275e2c228ae4c6bb2f6216b5f0e77af0a/ppgfis_ufc_br}, doi = {10.1016/j.ejps.2017.11.028}, interhash = {998c82dc4ef1c419d77f50221d4159d9}, intrahash = {75e2c228ae4c6bb2f6216b5f0e77af0a}, issn = {0928-0987}, journal = {EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES}, keywords = {Amorphous; Crystalline; Grinding} Solvate; hydrochloride; {Raloxifene}, pages = {146-154}, publisher = {ELSEVIER}, pubstate = {published}, timestamp = {2022-05-23T20:00:14.000+0200}, title = {Mechanochemically induced solid state transformations: The case of raloxifene hydrochloride}, tppubtype = {article}, volume = 114, year = 2018 }