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Apricot extract inhibits the P‐gp–mediated efflux of talinolol

Within the framework of developing strategies to enhance the intestinal absorption of P‐glycoprotein (P‐gp) substrates, the modulatory effect of a standardized apricot extract on P‐gp–related efflux carriers was investigated in the Caco‐2 system, Ussing chambers and the rat in situ perfusion model using talinolol as a model substrate. Using the Caco‐2 system, polarity in transport of talinolol could be observed, the absorptive transport being much lower than the secretory transport (Papp‐abs = 1.08 ± 0.29 × 10−6 cm/s and Papp‐secr = 11.74 ± 0.80 × 10−6 cm/s). Inclusion of apricot extract (1%) in the apical medium resulted in a statistically significantly diminished polarity (Papp‐abs = 4.88 ± 0.96 × 10−6 cm/s and Papp‐secr = 9.39 ± 0.58 × 10−6 cm/s, p < 0.05). In addition, the inhibitory effect of apricot extract on P‐gp related efflux mechanisms was shown to be concentration (0% ≈ 0.1% < 0.3% < 1%) and pH dependent. Experiments performed with the Ussing chambers resulted in similar observations. In the rat in situ perfusion model, inclusion of apricot extract (1%) in the perfusion medium resulted in a threefold increase of the amount of talinolol appearing in the collected blood compared to the reference condition (23.6 ± 5.53 pmol/cm · min and 7.13 ± 1.08 pmol/cm · min, respectively; p < 0.05). Coadministration of this standardized apricot extract might be a safe and useful strategy to enhance the intestinal absorption of P‐gp substrates. The nature and structure of the compound(s) responsible for this inhibiting effect on P‐gp–related efflux carriers remain to be elucidated, as well as the exact mechanism by which apricot extract exerts its inhibitory function. © 2002 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:2539–2548, 2002 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Pharmaceutical Science Wiley

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