In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound
Аутори
Krstevska, AleksandraNedelkov, Ivana
Petrović, Maša
Ibrić, Svetlana
Mirković, Dušica
Cvijić, Sandra
Конференцијски прилог (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Precipitation of a drug substance in the small intestine
is a phenomenon relevant to weak bases due to their pH-
dependent solubility. Because of the low solubility at
higher pH, upon entry in the small intestine, a weak base
may get into a supersaturated state, which is
thermodynamically unstable and tends to precipitate
(Makitalo, 2019). Consequently, precipitation in the
gastrointestinal (GI) tract may significantly limit oral
bioavailability (BA) of poorly soluble, weak bases.
Several in vitro and in silico tools are available for
assessing the precipitation kinetics of weakly basic
compounds (Kou et al., 2018). The dynamic nature of
physiologically based in silico models and their ability to
treat drug dissolution and precipitation as variables
affecting concomitant drug bioperformance make in silico
models a powerful tool to assess the impact of these
variables on drug absorption.
The aim of this work was to in silico evaluate the
influence of possible variation...s in the values of GI
physiological parameters on the potential precipitation and
absorption of a weakly basic, poorly soluble and highly
permeable compound. ...
Извор:
Macedonian Pharmaceutical Bulletin, 2023, 69, Suppl 1, 127-128Издавач:
- Macedonian Pharmaceutical Association
- Ss. Cyril and Methodius University in Skopje, Faculty of Pharmacy
Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200161 (Универзитет у Београду, Фармацеутски факултет) (RS-MESTD-inst-2020-200161)
Напомена:
- 14th Central European Symposium on Pharmaceutical Technology, 28th - 30th September, Ohrid, N. Macedonia, 2023
Институција/група
PharmacyTY - CONF AU - Krstevska, Aleksandra AU - Nedelkov, Ivana AU - Petrović, Maša AU - Ibrić, Svetlana AU - Mirković, Dušica AU - Cvijić, Sandra PY - 2023 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/5053 AB - Precipitation of a drug substance in the small intestine is a phenomenon relevant to weak bases due to their pH- dependent solubility. Because of the low solubility at higher pH, upon entry in the small intestine, a weak base may get into a supersaturated state, which is thermodynamically unstable and tends to precipitate (Makitalo, 2019). Consequently, precipitation in the gastrointestinal (GI) tract may significantly limit oral bioavailability (BA) of poorly soluble, weak bases. Several in vitro and in silico tools are available for assessing the precipitation kinetics of weakly basic compounds (Kou et al., 2018). The dynamic nature of physiologically based in silico models and their ability to treat drug dissolution and precipitation as variables affecting concomitant drug bioperformance make in silico models a powerful tool to assess the impact of these variables on drug absorption. The aim of this work was to in silico evaluate the influence of possible variations in the values of GI physiological parameters on the potential precipitation and absorption of a weakly basic, poorly soluble and highly permeable compound. ... PB - Macedonian Pharmaceutical Association PB - Ss. Cyril and Methodius University in Skopje, Faculty of Pharmacy C3 - Macedonian Pharmaceutical Bulletin T1 - In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound VL - 69 IS - Suppl 1 SP - 127 EP - 128 DO - 10.33320/maced.pharm.bull.2023.69.03.062 ER -
@conference{ author = "Krstevska, Aleksandra and Nedelkov, Ivana and Petrović, Maša and Ibrić, Svetlana and Mirković, Dušica and Cvijić, Sandra", year = "2023", abstract = "Precipitation of a drug substance in the small intestine is a phenomenon relevant to weak bases due to their pH- dependent solubility. Because of the low solubility at higher pH, upon entry in the small intestine, a weak base may get into a supersaturated state, which is thermodynamically unstable and tends to precipitate (Makitalo, 2019). Consequently, precipitation in the gastrointestinal (GI) tract may significantly limit oral bioavailability (BA) of poorly soluble, weak bases. Several in vitro and in silico tools are available for assessing the precipitation kinetics of weakly basic compounds (Kou et al., 2018). The dynamic nature of physiologically based in silico models and their ability to treat drug dissolution and precipitation as variables affecting concomitant drug bioperformance make in silico models a powerful tool to assess the impact of these variables on drug absorption. The aim of this work was to in silico evaluate the influence of possible variations in the values of GI physiological parameters on the potential precipitation and absorption of a weakly basic, poorly soluble and highly permeable compound. ...", publisher = "Macedonian Pharmaceutical Association, Ss. Cyril and Methodius University in Skopje, Faculty of Pharmacy", journal = "Macedonian Pharmaceutical Bulletin", title = "In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound", volume = "69", number = "Suppl 1", pages = "127-128", doi = "10.33320/maced.pharm.bull.2023.69.03.062" }
Krstevska, A., Nedelkov, I., Petrović, M., Ibrić, S., Mirković, D.,& Cvijić, S.. (2023). In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound. in Macedonian Pharmaceutical Bulletin Macedonian Pharmaceutical Association., 69(Suppl 1), 127-128. https://doi.org/10.33320/maced.pharm.bull.2023.69.03.062
Krstevska A, Nedelkov I, Petrović M, Ibrić S, Mirković D, Cvijić S. In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound. in Macedonian Pharmaceutical Bulletin. 2023;69(Suppl 1):127-128. doi:10.33320/maced.pharm.bull.2023.69.03.062 .
Krstevska, Aleksandra, Nedelkov, Ivana, Petrović, Maša, Ibrić, Svetlana, Mirković, Dušica, Cvijić, Sandra, "In silico assessment of intestinal precipitation: Case study of a poorly soluble, weakly basic compound" in Macedonian Pharmaceutical Bulletin, 69, no. Suppl 1 (2023):127-128, https://doi.org/10.33320/maced.pharm.bull.2023.69.03.062 . .