TY  - CONF
AU  - Dobričić, Vladimir
AU  - Marodi, Marko
AU  - Marković, Bojan
AU  - Tomašič, Tihomir
AU  - Zidar, Nace
AU  - Peterlin Mašič, Lucija
AU  - Ilaš, Janez
AU  - Kikelj, Danijel
PY  - 2020
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5460
AB  - In this study, estimation of gastrointestinal absorption of thirteen selected dual DNA gyrase and topoisomerase IV
inhibitors was carried out using PAMPA test. Diffusion through artificial membrane, consisting of egg lecithin solution
in dodecane (first PAMPA model) and a mixture of hexadecane and hexane (second PAMPA model), was monitored
[1,2]. The starting solutions (pH 5.5) and the acceptor medium (pH 7.4) were prepared to contain 2% dimethyl
sulfoxide. Concentrations of tested compounds in starting solutions, donor and acceptor medium after incubation
were measured using LC-MS/MS method. Permeability coefficients were calculated and good correlation was
observed between results obtained using these two PAMPA models. Subsequently, the hexadecane/hexane model
was selected for the evaluation of gastrointestinal absorption of the remaining ten compounds.
Derivatives with the highest permeability in hexadecane/hexane model were TZS-34 and TCF-3a (logPe: -5.37 and
-4.93, respectively) whereas TLK-13 and NZ-97 had the lowest permeability (logPe: -9.91 and -9.85, respectively).
Therefore, the highest gastrointestinal absorption can be expected from TZS-34 and TCF-3a, and lowest from TLK-13
and NZ-97 (Figure 1). High membrane retention observed for compounds TEL-28 (72%) and TAZ-2b (30 %) might be a
reason for lower permeability than expected based on their lipophilicity.
PB  - MuTaLig COST ACTION CA15135
C3  - Fourth WG Meeting CA15135, Cost Action CA15135, 5 - 7. March, 2020. Bornova, Izmir, Book of the Abstracts
T1  - Estimation of gastrointestinal absorption of a series of dual DNA Gyrase and Topoisomerase IV inhibitors using Pampa technique
SP  - 41
EP  - 41
UR  - https://hdl.handle.net/21.15107/rcub_farfar_5460
ER  - 

@conference{
author = "Dobričić, Vladimir and Marodi, Marko and Marković, Bojan and Tomašič, Tihomir and Zidar, Nace and Peterlin Mašič, Lucija and Ilaš, Janez and Kikelj, Danijel",
year = "2020",
abstract = "In this study, estimation of gastrointestinal absorption of thirteen selected dual DNA gyrase and topoisomerase IV
inhibitors was carried out using PAMPA test. Diffusion through artificial membrane, consisting of egg lecithin solution
in dodecane (first PAMPA model) and a mixture of hexadecane and hexane (second PAMPA model), was monitored
[1,2]. The starting solutions (pH 5.5) and the acceptor medium (pH 7.4) were prepared to contain 2% dimethyl
sulfoxide. Concentrations of tested compounds in starting solutions, donor and acceptor medium after incubation
were measured using LC-MS/MS method. Permeability coefficients were calculated and good correlation was
observed between results obtained using these two PAMPA models. Subsequently, the hexadecane/hexane model
was selected for the evaluation of gastrointestinal absorption of the remaining ten compounds.
Derivatives with the highest permeability in hexadecane/hexane model were TZS-34 and TCF-3a (logPe: -5.37 and
-4.93, respectively) whereas TLK-13 and NZ-97 had the lowest permeability (logPe: -9.91 and -9.85, respectively).
Therefore, the highest gastrointestinal absorption can be expected from TZS-34 and TCF-3a, and lowest from TLK-13
and NZ-97 (Figure 1). High membrane retention observed for compounds TEL-28 (72%) and TAZ-2b (30 %) might be a
reason for lower permeability than expected based on their lipophilicity.",
publisher = "MuTaLig COST ACTION CA15135",
journal = "Fourth WG Meeting CA15135, Cost Action CA15135, 5 - 7. March, 2020. Bornova, Izmir, Book of the Abstracts",
title = "Estimation of gastrointestinal absorption of a series of dual DNA Gyrase and Topoisomerase IV inhibitors using Pampa technique",
pages = "41-41",
url = "https://hdl.handle.net/21.15107/rcub_farfar_5460"
}

Dobričić, V., Marodi, M., Marković, B., Tomašič, T., Zidar, N., Peterlin Mašič, L., Ilaš, J.,& Kikelj, D.. (2020). Estimation of gastrointestinal absorption of a series of dual DNA Gyrase and Topoisomerase IV inhibitors using Pampa technique. in Fourth WG Meeting CA15135, Cost Action CA15135, 5 - 7. March, 2020. Bornova, Izmir, Book of the Abstracts
MuTaLig COST ACTION CA15135., 41-41.
https://hdl.handle.net/21.15107/rcub_farfar_5460

Dobričić V, Marodi M, Marković B, Tomašič T, Zidar N, Peterlin Mašič L, Ilaš J, Kikelj D. Estimation of gastrointestinal absorption of a series of dual DNA Gyrase and Topoisomerase IV inhibitors using Pampa technique. in Fourth WG Meeting CA15135, Cost Action CA15135, 5 - 7. March, 2020. Bornova, Izmir, Book of the Abstracts. 2020;:41-41.
https://hdl.handle.net/21.15107/rcub_farfar_5460 .

Dobričić, Vladimir, Marodi, Marko, Marković, Bojan, Tomašič, Tihomir, Zidar, Nace, Peterlin Mašič, Lucija, Ilaš, Janez, Kikelj, Danijel, "Estimation of gastrointestinal absorption of a series of dual DNA Gyrase and Topoisomerase IV inhibitors using Pampa technique" in Fourth WG Meeting CA15135, Cost Action CA15135, 5 - 7. March, 2020. Bornova, Izmir, Book of the Abstracts (2020):41-41,
https://hdl.handle.net/21.15107/rcub_farfar_5460 .