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Published on: November 14, 2018
Bioavailability of propranolol after oral, sublingual, and intranasal administration
G S Duchateau1, J Zuidema, F W Merkus
1Department of Biopharmaceutics, University of Amsterdam, Plantage Muidergracht 14, 1018 TV, Amsterdam, The Netherlands.
Abstract:
The bioavailability of propranolol was compared after oral, sublingual, and intranasal administration in eight healthy male volunteers. Relative to the bioavailability after intranasal (in) administration, which was previously shown to be nearly complete (F relin = 100%), the sublingual (sl) administration of a standard 10-mg tablet gave a bioavailability of F relsl = 63 ± 22%, while the oral (or) administration yielded only F relor = 25 ± 8%. The serum concentration-time curves of propranolol after sublingual administration resembled those of a sustained-release preparation. This sustained-release phenomenon after the sublingual route is reflected in the mean residence times (MRTs) of propranolol in the body (MRTor = 5.7 ± 1.3 hr, MRTsl - 6.4 ± 1.3 hr, MRTin = 4.6 ± 1.0 hr; mean ± SD; N = 8). MRTs after sublingual administration were significantly longer than after the oral and the intranasal doses (P < 0.05 and P < 0.002, respectively).
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