Pharmacokinetics of proline-rich tripeptides in the pig Academic Article uri icon


  • Tripeptides may possess bioactive properties. For instance, blood pressure lowering is attributed to the proline-rich tripeptides Ile-Pro-Pro (IPP), Leu-Pro-Pro (LPP), and Val-Pro-Pro (VPP). However, little is known about their absorption, distribution, and elimination characteristics. The aim of this study was to characterize the pharmacokinetic behavior of IPP, LPP, and VPP in a conscious pig model. Synthetic IPP, LPP, and VPP were administered intravenously or intragastrically (4.0mgkg1 BW in saline) to 10 piglets (approximately 25kg body weight) in the postabsorptive state. After intravenous dosing, the elimination half-life for IPP was significantly higher (P<0.001) than for LPP and VPP (2.50.1, 1.90.1, and 2.00.1min, respectively). After intragastric dosing, however, the elimination half-lives were not significantly different between the peptides (91, 154, and 126min, respectively). Maximum plasma concentrations were about 10nmoll1 for the three tripeptides. The fraction dose absorbed was 0.0770.010, 0.0590.009, and 0.0730.015%, for IPP, LPP, and VPP, respectively. Proline-rich tripeptides reach the blood circulation intact, with an absolute bioavailability of about 0.1% when administered via a saline solution. Because half-lives of absorption and elimination were maximally about 5 and 15min, respectively, this suggests that under these conditions a bioactive effect of these tripeptides would be rather acute.

published proceedings

  • Peptides

altmetric score

  • 3

author list (cited authors)

  • van der Pijl, P. C., Kies, A. K., Ten Have, G., Duchateau, G., & Deutz, N.

citation count

  • 52

complete list of authors

  • van der Pijl, PC||Kies, AK||Ten Have, GAM||Duchateau, GSMJE||Deutz, NEP

publication date

  • December 2008