New water-soluble dosage forms of 1,2,4-thiadiazole derivative on the basis of inclusion complexes with cyclodextrins
| Autor: | Maria Brusnikina, Oleg I. Silyukov, Mikhail Chislov, Irina V. Terekhova, Alexey N. Proshin, Tatyana Volkova |
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| Rok vydání: | 2016 |
| Předmět: |
chemistry.chemical_classification
Aqueous solution Cyclodextrin 010405 organic chemistry 010402 general chemistry Condensed Matter Physics 01 natural sciences Dosage form 0104 chemical sciences chemistry.chemical_compound Crystallography chemistry Dissolution testing Physical and Theoretical Chemistry Fourier transform infrared spectroscopy Thermal analysis Dissolution Derivative (chemistry) Nuclear chemistry |
| Zdroj: | Journal of Thermal Analysis and Calorimetry. 127:1815-1824 |
| ISSN: | 1588-2926 1388-6150 |
| DOI: | 10.1007/s10973-016-5955-z |
| Popis: | Effect of cyclodextrins on aqueous solubility of 1-[5-(3-chloro-phenylamino)-1,2,4-thiadiazol-3-yl]-propan-2-ol (I), which was synthesized and proposed for the treatment of Alzheimer’s disease, was studied. First of all, inclusion complex formation of I with different cyclodextrins was studied in aqueous solutions. Formation of more stable complexes with β- and hydroxypropyl-β-cyclodextrins was revealed. Next, solid inclusion complexes of I with β- and hydroxypropyl-β-cyclodextrins were prepared by the mechanical grinding, and their existence in the solid state was confirmed by powder X-ray diffraction, FTIR spectroscopy, microscopy, and thermochemical methods. Dissolution testing of the tablets of pure I and its complexes with β- and hydroxypropyl-β-cyclodextrins in the aqueous buffered solutions simulated the biological environment was carried out. The observed drastic enhancement of dissolution extent and dissolution rate of the complexes was attributed to the inclusion complex formation. |
| Databáze: | OpenAIRE |
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