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Nasal absorption of alprenolol and metoprolol

1986; Elsevier BV; Volume: 34; Issue: 1-2 Linguagem: Inglês

10.1016/0378-5173(86)90019-0

1873-3476

Guus Duchateau, J. Zuidema, Willem M. Albers, F.W.H.M. Merkus,

Analytical Methods in Pharmaceuticals

In order to determine the importance of hydrophobicity in nasal drug absorption, we studied the bioavailability of the β-adrenoceptor blocking drugs, alprenolol 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.