Nasal absorption of Alprenolol (cas 13655-52-2) and metoprolol

Add time:09/10/2019    Source:sciencedirect.com

In order to determine the importance of hydrophobicity in nasal drug absorption, we studied the bioavailability of the β-adrenoceptor blocking drugs, Alprenolol (cas 13655-52-2) and metoprolol, in volunteers, after nasal administration. The results were related to the oral and sublingual administration. The intranasal bioavailability, Tmax-, MRT- and MATcorr-values of the hydrophilic metoprolol after intranasal administration did not differ significantly from the oral and sublingual administration (n = 4). Metoprolol is probably swallowed after intranasal and sublingual administration and absorbed in the gastrointestinal tract. In contrast, great differences were found in the intranasal bioavailability, Tmax-, MRT-, and MATcorr-values of the hydrophobic alprenolol, related to the oral dose (n = 5). Nasal absorption of alprenolol was fast and showed a high bioavailability (Tmax = 0.45 ± 0.11 h). MRT-values after intranasal administration were significantly different from the other two administrations (MRTin = 3.0 ± 0.5 h, MRTsl = 3.9 ± 0.9 h, MRTor = 3.5 ± 0.6, P = 0.047 and P = 0.022, respectively). The results of this study indicate that hydrophobicity may be an important factor in nasal membrane passage.

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