Open Access
Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A
Тип публикации: Journal Article
Дата публикации: 1992-04-01
SCImago Q1
WOS Q1
БС1
SJR: 0.977
CiteScore: 10.1
Impact factor: 5.2
ISSN: 03785173, 18733476
Pharmaceutical Science
Краткое описание
The kinetics of degradation of isocyclosporin A (isoCyA) was studied in aqueous solution at pH 1–10 and in human plasma. At pH > 5 isoCyA was found to undergo a quantitative conversion to cyclosporin A (CyA) via a mechanism involving intramolecular aminolysis of the ester bond by the N-methyl amino group in the peptide. The pH-rate profile obtained for this O,N-acyl migration was accounted for in terms of spontaneous as well as hydroxide ion-catalyzed aminolysis. The half-life of the conversion of isoCyA to CyA was 21.7 h at pH 7.4 and 37°C and 12.1 h in 80% human plasma at 37°C. IsoCyA is suggested as a potential prodrug derivative of CyA which may be useful to improve the delivery characteristics of the parent drug.
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BUNDGAARD H., Friis G. J. Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A // International Journal of Pharmaceutics. 1992. Vol. 82. No. 1-2. pp. 85-90.
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BUNDGAARD H., Friis G. J. Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A // International Journal of Pharmaceutics. 1992. Vol. 82. No. 1-2. pp. 85-90.
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TY - JOUR
DO - 10.1016/0378-5173(92)90076-e
UR - https://doi.org/10.1016/0378-5173(92)90076-e
TI - Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A
T2 - International Journal of Pharmaceutics
AU - BUNDGAARD, HANS
AU - Friis, Gitte Juel
PY - 1992
DA - 1992/04/01
PB - Elsevier
SP - 85-90
IS - 1-2
VL - 82
SN - 0378-5173
SN - 1873-3476
ER -
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BibTex (до 50 авторов)
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@article{1992_BUNDGAARD,
author = {HANS BUNDGAARD and Gitte Juel Friis},
title = {Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A},
journal = {International Journal of Pharmaceutics},
year = {1992},
volume = {82},
publisher = {Elsevier},
month = {apr},
url = {https://doi.org/10.1016/0378-5173(92)90076-e},
number = {1-2},
pages = {85--90},
doi = {10.1016/0378-5173(92)90076-e}
}
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MLA
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BUNDGAARD, HANS, and Gitte Juel Friis. “Prodrugs of peptides. 16. Isocyclosporin A as a potential prodrug of cyclosporin A.” International Journal of Pharmaceutics, vol. 82, no. 1-2, Apr. 1992, pp. 85-90. https://doi.org/10.1016/0378-5173(92)90076-e.
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