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International Journal of Otolaryngology
Volume 2009, Article ID 495186, 4 pages
Clinical Study

Concentrations of H1-Receptor Antagonist in the Human Nasal Mucosa

Department of Otolaryngology, Head and Neck Surgery, Nagasaki University Graduate School of Biomedical Sciences, 1-7-1 Sakamoto, Nagasaki 852-8501, Japan

Received 5 June 2009; Accepted 16 September 2009

Academic Editor: Fuad Baroody

Copyright © 2009 Kenji Takasaki et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Aims. To measure blood and tissue concentrations of the H1-receptor antagonist, bepotastine besilate (BB). Methods. Participants included 14 men and six women, whose age ranged from 13 to 76 years, with chronic rhinosinusitis, who underwent endoscopic sinus surgery at our university hospital. Among them, 10 participants had allergic rhinitis (AR) (Group I), and others did not have AR (Group II). Nasal mucosa and blood were collected 55 to 130 minutes after oral administration of BB 10 mg. Concentrations of the agent in the serum and nasal mucosa were measured by high-performance liquid chromatography. Results. Concentrations of BB of the serum in Group I and II were 9 8 ± 3 2  ng/mL and 1 1 2 ± 3 9  ng/mL. Those of the nasal mucosa tissue in Groups I and II were 1 0 1 ± 3 6  ng/g and 1 3 2 ± 4 4  ng/g. There was no significant difference in the values of concentration of BB between the serum and the nasal mucosa in either Group I or II ( 𝑃 = . 7 5 7 and 𝑃 = . 2 6 6 2 , resp., Paired t-test). Conclusion. This preliminary study is considered the first report on the concentration of H1-receptor antagonists in nasal mucosa. The prompt absorption and transition to the nasal mucosa of BB seems to have an effect on allergic rhinitis.