Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation
Maria Promzeleva
1
,
A.D. Proshin
2
,
Oleg I Silyukov
1, 3
,
A. Mazur
3
,
Peter M. Tolstoy
3
,
Sergey Ivanov
4
,
Felix Kamilov
5
,
1
Тип публикации: Journal Article
Дата публикации: 2018-01-03
scimago Q1
wos Q2
БС2
SJR: 1.105
CiteScore: 9.7
Impact factor: 5.5
ISSN: 23739878
PubMed ID:
33418739
Biomaterials
Biomedical Engineering
Краткое описание
The synthesized 1,2,4-thiadiazole derivative displaying biological activity has low aqueous solubility and dissolution rate. Novel oral formulations of thiadiazole with β- and hydroxypropyl-β-cyclodextrins were obtained by grinding and freeze-drying methods with the purpose to improve the aqueous solubility. Complex formation of 1,2,4-thiadiazole derivative with cyclodextrins was confirmed by means of solid-state 13C MAS CP/TOSS NMR. Solubility, dissolution rate and permeability of the solid inclusion complexes were evaluated in different biorelevant media (SGF, FaSSGF, FaSSIF) simulating the conditions in the gastrointestinal tract. It was demonstrated that the content of biorelevant media affects the properties of the inclusion complexes. In particular, solubilizing effect of cyclodextrins became less pronounced when the micelles of taurocholic acid and lecithin are formed in the dissolution media. The inclusion of thiadiazole into cyclodextrin cavity is in competition with its partitioning into the mic...
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Promzeleva M. et al. Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation // ACS Biomaterials Science and Engineering. 2018. Vol. 4. No. 2. pp. 491-501.
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Promzeleva M., Volkova T. D., Proshin A., Silyukov O. I., Mazur A., Tolstoy P. M., Ivanov S., Kamilov F., Terekhova I. V. Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation // ACS Biomaterials Science and Engineering. 2018. Vol. 4. No. 2. pp. 491-501.
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TY - JOUR
DO - 10.1021/acsbiomaterials.7b00887
UR - https://doi.org/10.1021/acsbiomaterials.7b00887
TI - Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation
T2 - ACS Biomaterials Science and Engineering
AU - Promzeleva, Maria
AU - Volkova, Tatyana D.
AU - Proshin, A.D.
AU - Silyukov, Oleg I
AU - Mazur, A.
AU - Tolstoy, Peter M.
AU - Ivanov, Sergey
AU - Kamilov, Felix
AU - Terekhova, Irina V
PY - 2018
DA - 2018/01/03
PB - American Chemical Society (ACS)
SP - 491-501
IS - 2
VL - 4
PMID - 33418739
SN - 2373-9878
ER -
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@article{2018_Promzeleva,
author = {Maria Promzeleva and Tatyana D. Volkova and A.D. Proshin and Oleg I Silyukov and A. Mazur and Peter M. Tolstoy and Sergey Ivanov and Felix Kamilov and Irina V Terekhova},
title = {Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation},
journal = {ACS Biomaterials Science and Engineering},
year = {2018},
volume = {4},
publisher = {American Chemical Society (ACS)},
month = {jan},
url = {https://doi.org/10.1021/acsbiomaterials.7b00887},
number = {2},
pages = {491--501},
doi = {10.1021/acsbiomaterials.7b00887}
}
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MLA
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Promzeleva, Maria, et al. “Improved Biopharmaceutical Properties of Oral Formulations of 1,2,4-Thiadiazole Derivative with Cyclodextrins: In Vitro and in Vivo Evaluation.” ACS Biomaterials Science and Engineering, vol. 4, no. 2, Jan. 2018, pp. 491-501. https://doi.org/10.1021/acsbiomaterials.7b00887.
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