In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs. / Holm, René; Meng-Lund, Emil; Andersen, Morten B. ; Jespersen, Mads L.; Karlsson, Jens-Jacob; Garmer, Mats; Jørgensen, Erling B.; Jacobsen, Jette.

In: European Journal of Pharmaceutical Sciences, Vol. 49, No. 2, 13.05.2013, p. 117-124.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Holm, R, Meng-Lund, E, Andersen, MB, Jespersen, ML, Karlsson, J-J, Garmer, M, Jørgensen, EB & Jacobsen, J 2013, 'In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs', European Journal of Pharmaceutical Sciences, vol. 49, no. 2, pp. 117-124. https://doi.org/10.1016/j.ejps.2013.02.024

APA

Holm, R., Meng-Lund, E., Andersen, M. B., Jespersen, M. L., Karlsson, J-J., Garmer, M., Jørgensen, E. B., & Jacobsen, J. (2013). In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs. European Journal of Pharmaceutical Sciences, 49(2), 117-124. https://doi.org/10.1016/j.ejps.2013.02.024

Vancouver

Holm R, Meng-Lund E, Andersen MB, Jespersen ML, Karlsson J-J, Garmer M et al. In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs. European Journal of Pharmaceutical Sciences. 2013 May 13;49(2):117-124. https://doi.org/10.1016/j.ejps.2013.02.024

Author

Holm, René ; Meng-Lund, Emil ; Andersen, Morten B. ; Jespersen, Mads L. ; Karlsson, Jens-Jacob ; Garmer, Mats ; Jørgensen, Erling B. ; Jacobsen, Jette. / In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs. In: European Journal of Pharmaceutical Sciences. 2013 ; Vol. 49, No. 2. pp. 117-124.

Bibtex

@article{43c420572185433bb1384bdcf769ffb4,
title = "In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and G{\"o}ttingen minipigs",
abstract = "This work studied the buccal absorption of metoprolol in vitro, ex vivo and in vivo as a function of buffered pH at 7.4, 8.5, 9.0 and 9.5. Permeability studies showed a correlation (r(2)=0.92) between in vitro TR146 cell culture and ex vivo porcine buccal mucosa in a modified Ussing chamber. A higher apparent permeability was observed at higher pH values, i.e. the more compound that was unionised the higher the permeability. In vivo studies were conducted in anaesthetised G{\"o}ttingen mini-pigs. A clear influence of pH on the absorption was seen and a significant higher absolute bioavailability was obtained after buccal dosing (58-107%) compared to oral (3%) administration, ranging 58-107% and 3%, respectively. Macroscopically, no local toxic effects were observed by visual inspection of mini-pig cheeks. A very clear level C in vitro in vivo correlation (r(2)=0.98) was obtained between the observed in vitro permeabilities and the bioavailability observed in vivo, suggesting that the two in vitro models have good predictive power for drug delivery, which could be a useful tool for future formulation developments intended for buccal delivery.",
author = "Ren{\'e} Holm and Emil Meng-Lund and Andersen, {Morten B.} and Jespersen, {Mads L.} and Jens-Jacob Karlsson and Mats Garmer and J{\o}rgensen, {Erling B.} and Jette Jacobsen",
year = "2013",
month = may,
day = "13",
doi = "10.1016/j.ejps.2013.02.024",
language = "English",
volume = "49",
pages = "117--124",
journal = "Norvegica Pharmaceutica Acta",
issn = "0928-0987",
publisher = "Elsevier",
number = "2",

}

RIS

TY - JOUR

T1 - In vitro, ex vivo and in vivo examination of buccal absorption of metoprolol with varying pH in TR146 cell culture, porcine buccal mucosa and Göttingen minipigs

AU - Holm, René

AU - Meng-Lund, Emil

AU - Andersen, Morten B.

AU - Jespersen, Mads L.

AU - Karlsson, Jens-Jacob

AU - Garmer, Mats

AU - Jørgensen, Erling B.

AU - Jacobsen, Jette

PY - 2013/5/13

Y1 - 2013/5/13

N2 - This work studied the buccal absorption of metoprolol in vitro, ex vivo and in vivo as a function of buffered pH at 7.4, 8.5, 9.0 and 9.5. Permeability studies showed a correlation (r(2)=0.92) between in vitro TR146 cell culture and ex vivo porcine buccal mucosa in a modified Ussing chamber. A higher apparent permeability was observed at higher pH values, i.e. the more compound that was unionised the higher the permeability. In vivo studies were conducted in anaesthetised Göttingen mini-pigs. A clear influence of pH on the absorption was seen and a significant higher absolute bioavailability was obtained after buccal dosing (58-107%) compared to oral (3%) administration, ranging 58-107% and 3%, respectively. Macroscopically, no local toxic effects were observed by visual inspection of mini-pig cheeks. A very clear level C in vitro in vivo correlation (r(2)=0.98) was obtained between the observed in vitro permeabilities and the bioavailability observed in vivo, suggesting that the two in vitro models have good predictive power for drug delivery, which could be a useful tool for future formulation developments intended for buccal delivery.

AB - This work studied the buccal absorption of metoprolol in vitro, ex vivo and in vivo as a function of buffered pH at 7.4, 8.5, 9.0 and 9.5. Permeability studies showed a correlation (r(2)=0.92) between in vitro TR146 cell culture and ex vivo porcine buccal mucosa in a modified Ussing chamber. A higher apparent permeability was observed at higher pH values, i.e. the more compound that was unionised the higher the permeability. In vivo studies were conducted in anaesthetised Göttingen mini-pigs. A clear influence of pH on the absorption was seen and a significant higher absolute bioavailability was obtained after buccal dosing (58-107%) compared to oral (3%) administration, ranging 58-107% and 3%, respectively. Macroscopically, no local toxic effects were observed by visual inspection of mini-pig cheeks. A very clear level C in vitro in vivo correlation (r(2)=0.98) was obtained between the observed in vitro permeabilities and the bioavailability observed in vivo, suggesting that the two in vitro models have good predictive power for drug delivery, which could be a useful tool for future formulation developments intended for buccal delivery.

U2 - 10.1016/j.ejps.2013.02.024

DO - 10.1016/j.ejps.2013.02.024

M3 - Journal article

C2 - 23500040

VL - 49

SP - 117

EP - 124

JO - Norvegica Pharmaceutica Acta

JF - Norvegica Pharmaceutica Acta

SN - 0928-0987

IS - 2

ER -

ID: 46280072