PMID: 7545750Jun 1, 1995Paper

Absorption enhancement of a hydrophilic model compound by verapamil after rectal administration to rats

The Journal of Pharmacy and Pharmacology
A B NoachD D Breimer

Abstract

The use of verapamil as an absorption enhancer for the paracellular route in-vivo was studied using FITC-labelled dextran (molecular weight 4000) (FD-4) as a hydrophilic model compound for transport enhancement. The kinetics of FD-4 after intravenous doses of 1 or 10 mg could be described by a two-compartment model with a systemic clearance of approximately 2 mL min-1 and a terminal plasma half-life of approximately 36 min. Rectal administration to rats, performed as a rectal infusion of 10 mg FD-4 together with 7 mM verapamil, resulted in a 10-fold increase in the percentage of the dose absorbed over a 5-h period compared with the control and a 6-fold increase compared with a bolus administration, although the total amount absorbed remained relatively low (approx. 3% maximum). Large inter-animal variation in effect values were noted. The data indicate that although verapamil is able to enhance the absorption of hydrophilic compounds in-vivo, practical application of verapamil for this purpose doses not seem feasible.

References

May 1, 1978·Journal of Pharmaceutical Sciences·D P Vaughan, M Dennis
Oct 15, 1977·European Journal of Pharmacology·J Wróbel, L Michalska
Sep 1, 1992·Journal of Pharmaceutical Sciences·R Mehvar, T L Shepard
Sep 1, 1990·Pharmaceutical Research·A R HilgersP S Burton
Jan 1, 1989·Pharmacology & Therapeutics·E J van HoogdalemD D Breimer
May 1, 1988·The Journal of Pharmacy and Pharmacology·E J van HoogdalemD D Breimer
Oct 1, 1985·Gastroenterology·M DonowitzH Cheng
Jan 1, 1987·The Journal of Membrane Biology·J L Madara, J R Pappenheimer
Sep 15, 1994·Biochemical Pharmacology·M SakaiD D Breimer

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Citations

Apr 7, 2006·The Journal of Pharmacy and Pharmacology·Naoko TanakaKazumasa Shinozuka

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