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In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique

Authorized Users Only
2017
Authors
Savić, Jelena
Dobričić, Vladimir
Nikolić, Katarina
Vladimirov, Sote
Dilber, Sanda
Brborić, Jasmina
Article (Published version)
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Abstract
Prediction of gastrointestinal absorption of thirteen newly synthesized beta-hydroxy-beta-arylalkanoic acids (HAA) and ibuprofen was performed using PAMPA test The highest values of PAMPA parameters (%Tand P-app) were calculated for 1C, 1B and 2C and these parameters were significantly lower in comparison to ibuprofen. QSPR analysis was performed in order to identify molecular descriptors with the highest influence on %Tand-logP(app) and to create models which could be used for the design of novel HAA with improved gastrointestinal absorption. Obtained results indicate that introduction of branched side chain, as well as introduction of substituents on one phenyl ring (which disturb symmetry of the molecule) could have positive impact on gastrointestinal absorption. On the basis of these results, six novel HAA were designed and PAMPA parameters %Tand-logP(app) were predicted by use of selected QSPR models. Designed derivatives should have better gastrointestinal absorption than HAA tes...ted in this study.

Source:
European Journal of Pharmaceutical Sciences, 2017, 100, 36-41
Publisher:
  • Elsevier Science BV, Amsterdam
Funding / projects:
  • Development of molecules with antiinflammatory and cardioprotective activity: structural modifications, modelling, physicochemical characterization and formulation investigations (RS-172041)

DOI: 10.1016/j.ejps.2017.01.005

ISSN: 0928-0987

PubMed: 28077276

WoS: 000397373900005

Scopus: 2-s2.0-85009360414
[ Google Scholar ]
6
5
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/2923
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Savić, Jelena
AU  - Dobričić, Vladimir
AU  - Nikolić, Katarina
AU  - Vladimirov, Sote
AU  - Dilber, Sanda
AU  - Brborić, Jasmina
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2923
AB  - Prediction of gastrointestinal absorption of thirteen newly synthesized beta-hydroxy-beta-arylalkanoic acids (HAA) and ibuprofen was performed using PAMPA test The highest values of PAMPA parameters (%Tand P-app) were calculated for 1C, 1B and 2C and these parameters were significantly lower in comparison to ibuprofen. QSPR analysis was performed in order to identify molecular descriptors with the highest influence on %Tand-logP(app) and to create models which could be used for the design of novel HAA with improved gastrointestinal absorption. Obtained results indicate that introduction of branched side chain, as well as introduction of substituents on one phenyl ring (which disturb symmetry of the molecule) could have positive impact on gastrointestinal absorption. On the basis of these results, six novel HAA were designed and PAMPA parameters %Tand-logP(app) were predicted by use of selected QSPR models. Designed derivatives should have better gastrointestinal absorption than HAA tested in this study.
PB  - Elsevier Science BV, Amsterdam
T2  - European Journal of Pharmaceutical Sciences
T1  - In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique
VL  - 100
SP  - 36
EP  - 41
DO  - 10.1016/j.ejps.2017.01.005
ER  - 
@article{
author = "Savić, Jelena and Dobričić, Vladimir and Nikolić, Katarina and Vladimirov, Sote and Dilber, Sanda and Brborić, Jasmina",
year = "2017",
abstract = "Prediction of gastrointestinal absorption of thirteen newly synthesized beta-hydroxy-beta-arylalkanoic acids (HAA) and ibuprofen was performed using PAMPA test The highest values of PAMPA parameters (%Tand P-app) were calculated for 1C, 1B and 2C and these parameters were significantly lower in comparison to ibuprofen. QSPR analysis was performed in order to identify molecular descriptors with the highest influence on %Tand-logP(app) and to create models which could be used for the design of novel HAA with improved gastrointestinal absorption. Obtained results indicate that introduction of branched side chain, as well as introduction of substituents on one phenyl ring (which disturb symmetry of the molecule) could have positive impact on gastrointestinal absorption. On the basis of these results, six novel HAA were designed and PAMPA parameters %Tand-logP(app) were predicted by use of selected QSPR models. Designed derivatives should have better gastrointestinal absorption than HAA tested in this study.",
publisher = "Elsevier Science BV, Amsterdam",
journal = "European Journal of Pharmaceutical Sciences",
title = "In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique",
volume = "100",
pages = "36-41",
doi = "10.1016/j.ejps.2017.01.005"
}
Savić, J., Dobričić, V., Nikolić, K., Vladimirov, S., Dilber, S.,& Brborić, J.. (2017). In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique. in European Journal of Pharmaceutical Sciences
Elsevier Science BV, Amsterdam., 100, 36-41.
https://doi.org/10.1016/j.ejps.2017.01.005
Savić J, Dobričić V, Nikolić K, Vladimirov S, Dilber S, Brborić J. In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique. in European Journal of Pharmaceutical Sciences. 2017;100:36-41.
doi:10.1016/j.ejps.2017.01.005 .
Savić, Jelena, Dobričić, Vladimir, Nikolić, Katarina, Vladimirov, Sote, Dilber, Sanda, Brborić, Jasmina, "In vitro prediction of gastrointestinal absorption of novel beta-hydroxy-beta-arylalkanoic acids using PAMPA technique" in European Journal of Pharmaceutical Sciences, 100 (2017):36-41,
https://doi.org/10.1016/j.ejps.2017.01.005 . .

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