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Gasco MR, Trotta M, Eandi M. The influence of bile salts on the absorption in vitro and in vivo of propranolol. J Pharm Biomed Anal. 1984;2(3):425-39doi: 10.1016/0731-7085(84)80046-1.
Gasco, M. R., Trotta, M., & Eandi, M. (1984). The influence of bile salts on the absorption in vitro and in vivo of propranolol. Journal of pharmaceutical and biomedical analysis, 2(3), 425-39. https://doi.org/10.1016/0731-7085(84)80046-1
Gasco, M R, et al. "The influence of bile salts on the absorption in vitro and in vivo of propranolol." Journal of pharmaceutical and biomedical analysis vol. 2,3 (1984): 425-39. doi: https://doi.org/10.1016/0731-7085(84)80046-1
Gasco MR, Trotta M, Eandi M. The influence of bile salts on the absorption in vitro and in vivo of propranolol. J Pharm Biomed Anal. 1984;2(3):425-39. doi: 10.1016/0731-7085(84)80046-1. PMID: 16867723.
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J Pharm Biomed Anal. 1984;2(3):425-39. doi: 10.1016/0731-7085(84)80046-1.

The influence of bile salts on the absorption in vitro and in vivo of propranolol.

Journal of pharmaceutical and biomedical analysis

M R Gasco, M Trotta, M Eandi

Affiliations

  1. Istituto di Chimica Farmaceutica e Tossicologica dell'Università, Corso Raffaello 31, Torino, Italy.

PMID: 16867723 DOI: 10.1016/0731-7085(84)80046-1

Abstract

The lipophilicity of propranolol is increased by some bile salts which form ion-pairs. In the presence of taurodeoxycholate, the logarithm of the apparent partition coefficient (log P) of propranolol is increased. Moreover, the apparent diffusion constants in vitro of propranolol as ion-pairs at pH 3.0-6.0 are about 5-6 times higher than those of propranolol alone. The area under the curve values of plasma concentration-time profiles of propranolol, following its oral administration to rabbits together with taurodeoxycholate, are about 1.4 times higher than those after administration of propranolol alone. Moreover, after the administration of propranolol with taurodeoxycholate the plasma concentration rises more rapidly, with a point of inflection between 0.5 and 1.5 h, than after administration of propranolol alone. Taurodeoxycholate does not modify the first-pass effect of propranolol in rabbits following intravenous and intraportal administration. The absorption of an oral dose of propranolol in the presence of taurodeoxycholate increases from 70% to 100%, due to the higher lipophilicity of the ion-pair. The plasma concentration-time curves suggest the hypothesis that greater absorption of the ion-pair occurs mainly in the upper region of the gastrointestinal tract.

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