title: Absorption enhancement of rectally infused insulin by sodium tauro-24,25-dihydrofusidate (STDHF) in rats.
abstract: The bile salt derivative sodium tauro-24,25-dihydrofusidate (STDHF) has been reported to promote nasal absorption of insulin. In the present study the effect of STDHF on rectal insulin absorption was investigated in rats. At concentrations of 1 and 4% (w/v) it enhanced insulin bioavailability from 0.2 +/- 0.2 (control) to 4.2 +/- 3.2 and 6.7 +/- 2.1%, respectively, as assessed by radioimmunoassay. Insulin preparations with STDHF reduced blood glucose concentrations considerably in a concentration-dependent way. Coadministration of STDHF with Na2EDTA (0.25%, w/v) tended to increase further insulin bioavailability and hypoglycemic response. Varying the site of rectal administration did not influence these parameters.
authors.affiliation: Division of Pharmacology, Sylvius Laboratories, State University of Leiden, The Netherlands.
authors.forename: E J
authors.initials: EJ
authors.lastname: van Hoogdalem
authors.forename: C D
authors.initials: CD
authors.lastname: Heijligers-Feijen
authors.forename: J C
authors.initials: JC
authors.lastname: Verhoef
authors.forename: A G
authors.initials: AG
authors.lastname: de Boer
authors.forename: D D
authors.initials: DD
authors.lastname: Breimer
mesh_terms: D000285:Administration, Rectal; D000818:Animals; D001682:Biological Availability; D001786:Blood Glucose / Q000378:metabolism; D004492:Edetic Acid / Q000494:pharmacology; D005672:Fusidic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D007262:Infusions, Intravenous; D007328:Insulin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013268:Stimulation, Chemical
chemical_list: D001786:Blood Glucose; D007328:Insulin; D005672:Fusidic Acid; C053824:tauro-24,25-dihydrofusidate; D004492:Edetic Acid