Summary
We have studied the pharmacokinetics of tulobuterol given transdermally or by aerosol inhalation in healthy male volunteers.
Tulobuterol was rapidly absorbed after inhalation, with a tmax of 0.8–1.5 h. The Cmax and the AUC increased linearly with dose.
Tulobuterol was well absorbed after transdermal administration, with an absorption lag-time of about 4 h. The Cmax and AUC increased linearly with dose and the tmax was about 9–12 h. The mean percentage of drug absorbed during the application of a patch for 24 h was 82–90% after a single dose and 82–85% during repeated dosing.
The mean urinary recoveries as unchanged drug after a single inhalation and patch application were 3–4% and 5–6% respectively.
Tulobuterol did not accumulate during repeated inhalation or transdermal application. It was well tolerated, except for an increase in heart rate of 10–20 beats · min−1 after five repeated applications of a 4 mg patch.
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Uematsu, T., Nakano, M., Kosuge, K. et al. The pharmacokinetics of the β2-adrenoceptor agonist, tulobuterol, given transdermally and by inhalation. Eur J Clin Pharmacol 44, 361–364 (1993). https://doi.org/10.1007/BF00316473
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DOI: https://doi.org/10.1007/BF00316473