Characterizing interspecies differences in gastric fluid properties to improve understanding of in vivo oral drug formulation performance: [Inkl. Corrigendum]
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Characterizing interspecies differences in gastric fluid properties to improve understanding of in vivo oral drug formulation performance : [Inkl. Corrigendum]. / Rivera, Kristina R.; Pessi, Jenni; Andersson, Vincent; Gustafsson, Henning; Gluud, Lise Lotte; Buckley, Stephen T.
I: European Journal of Pharmaceutical Sciences, Bind 183, 106386, 2023.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Characterizing interspecies differences in gastric fluid properties to improve understanding of in vivo oral drug formulation performance
T2 - [Inkl. Corrigendum]
AU - Rivera, Kristina R.
AU - Pessi, Jenni
AU - Andersson, Vincent
AU - Gustafsson, Henning
AU - Gluud, Lise Lotte
AU - Buckley, Stephen T.
N1 - Corrigendum: DOI 10.1016/j.ejps.2023.106426 Publisher Copyright: © 2023
PY - 2023
Y1 - 2023
N2 - An in-depth understanding of the properties of gastric fluid(s) prior to an in vivo pharmacokinetic investigation can vastly improve predictions of in vivo performance. Previously, properties of animal and human gastric fluids have been characterized with varying methods. Unfortunately, characterization has often not been thorough, and some properties, such as density and viscosity, have not been reported. Here, human, porcine and canine gastric fluids were harvested and characterized for pH, viscosity, surface tension, density, and osmolarity. We found that the variability of pH and surface tension between dogs was significantly higher than the variability between pigs, and, furthermore, gastric fluids collected from the same canine species (beagles) housed in two different countries (Denmark and China) had surprisingly different pH values. Next, an in vitro dissolution study in diluted gastric fluids from each species was performed using minitablets containing ibuprofen. Human gastric fluids and porcine gastric fluids showed similar dissolution profiles and corroborated well with biorelevant human Fasted State Simulated Gastric Fluid (FaSSGF). In contrast, differences in canine gastric fluids caused highly variable dissolution results. We systematically compared our findings to those in the literature and based on this evaluation, propose obtaining aspirates from the animals used for in vivo studies to ensure knowledge on the fluid properties affecting the performance of the formulated drug in question.
AB - An in-depth understanding of the properties of gastric fluid(s) prior to an in vivo pharmacokinetic investigation can vastly improve predictions of in vivo performance. Previously, properties of animal and human gastric fluids have been characterized with varying methods. Unfortunately, characterization has often not been thorough, and some properties, such as density and viscosity, have not been reported. Here, human, porcine and canine gastric fluids were harvested and characterized for pH, viscosity, surface tension, density, and osmolarity. We found that the variability of pH and surface tension between dogs was significantly higher than the variability between pigs, and, furthermore, gastric fluids collected from the same canine species (beagles) housed in two different countries (Denmark and China) had surprisingly different pH values. Next, an in vitro dissolution study in diluted gastric fluids from each species was performed using minitablets containing ibuprofen. Human gastric fluids and porcine gastric fluids showed similar dissolution profiles and corroborated well with biorelevant human Fasted State Simulated Gastric Fluid (FaSSGF). In contrast, differences in canine gastric fluids caused highly variable dissolution results. We systematically compared our findings to those in the literature and based on this evaluation, propose obtaining aspirates from the animals used for in vivo studies to ensure knowledge on the fluid properties affecting the performance of the formulated drug in question.
KW - Canine
KW - Density
KW - Dissolution
KW - Gastric fluid
KW - Human aspirates
KW - Ibuprofen
KW - In vitro models
KW - In vitro-in vivo correlation
KW - Oral drug
KW - Osmolarity
KW - pH
KW - Porcine
KW - Surface tension
KW - Viscosity
U2 - 10.1016/j.ejps.2023.106386
DO - 10.1016/j.ejps.2023.106386
M3 - Journal article
C2 - 36736067
AN - SCOPUS:85148965570
VL - 183
JO - European Journal of Pharmaceutical Sciences
JF - European Journal of Pharmaceutical Sciences
SN - 0928-0987
M1 - 106386
ER -
ID: 367477733