Research output: Contribution to journal › Article › peer-review
New water-soluble dosage forms of 1,2,4-thiadiazole derivative on the basis of inclusion complexes with cyclodextrins. / Brusnikina, Maria; Silyukov, Oleg; Chislov, Mikhail; Volkova, Tatyana; Proshin, Alexey; Terekhova, Irina.
In: Journal of Thermal Analysis and Calorimetry, Vol. 127, No. 2, 01.02.2017, p. 1815-1824.Research output: Contribution to journal › Article › peer-review
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TY - JOUR
T1 - New water-soluble dosage forms of 1,2,4-thiadiazole derivative on the basis of inclusion complexes with cyclodextrins
AU - Brusnikina, Maria
AU - Silyukov, Oleg
AU - Chislov, Mikhail
AU - Volkova, Tatyana
AU - Proshin, Alexey
AU - Terekhova, Irina
PY - 2017/2/1
Y1 - 2017/2/1
N2 - 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.
AB - 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.
KW - 1,2,4-Thiadiazole
KW - Cyclodextrin
KW - Inclusion complex
KW - Thermal analysis
KW - Thermodynamics
KW - Water-soluble dosage forms
UR - http://www.scopus.com/inward/record.url?scp=84996486486&partnerID=8YFLogxK
U2 - 10.1007/s10973-016-5955-z
DO - 10.1007/s10973-016-5955-z
M3 - Article
AN - SCOPUS:84996486486
VL - 127
SP - 1815
EP - 1824
JO - Journal of Thermal Analysis and Calorimetry
JF - Journal of Thermal Analysis and Calorimetry
SN - 1388-6150
IS - 2
ER -
ID: 37016598