Disposition of radiolabelled suppositories in humans

Author:

Jay Michael1,Beihn Robert M1,Digenis George A1,Deland Frank H1,Caldwell Larry2,Mlodozeniec Arthur R2

Affiliation:

1. Colleges of Pharmacy and Medicine, University of Kentucky, Lexington, Kentucky, USA, 40536−0053

2. INTERx, Merck, Sharp and Dohme Research Laboratories, Lawrence, Kansas, USA, 66044

Abstract

Abstract The disposition of Witepsol H 15 suppositories radiolabelled with [99m Tc] technetium hydroxymethyldiphosphonate was studied after rectal administration in volunteers. The migration of the radiolabel was monitored continuously by external scintigraphy. The resulting scintiphotos were superimposed on lower GI radiographs to determine the extent of spreading of the dosage form in the rectum. The dosage form migrated approximately 5−7 cm into the rectum in nearly all of the studies and was, in general, confined to the lower and middle regions of the rectum. Since the venous supply to the lower rectum leads primarily to the inferior vena cava, the data presented here indicate that the metabolism of drugs sensitive to the ‘first-pass’ effect may be partially avoided by their rectal administration.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

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