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Determination of the Bioavailability of [ 14 C]‐Hexaminolevulinate Using Accelerator Mass Spectrometry After Intravesical Administration to Human Volunteers
Author(s) -
Klem B.,
Lappin G.,
Nicholson S.,
Wetering J.,
Vries D. E.,
Oosterhuis B.,
Garner R. C.
Publication year - 2006
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270006286849
Subject(s) - bioavailability , systemic administration , absorption (acoustics) , pharmacology , medicine , route of administration , urology , chemistry , in vivo , materials science , microbiology and biotechnology , composite material , biology
Hexaminolevulinate (HAL) is a diagnostic agent that allows the visualization of tumor tissue in the bladder by fluorescence cystoscopy. It is administered intravesically via a catheter for 1 hour, followed by blue light bladder inspection to induce selective red tumor fluorescence. Hexaminolevulinate should ideally be confined to the bladder only, but it is likely that some absorption occurs during administration, and therefore the systemic bioavailability is of interest. The bioavailability of HAL was determined by intravesical and intravenous administration of [ 14 C]‐HAL hydrochloride to 8 human volunteers. To reduce the radiation dose as low as possible, the ultrasensitive analytical technique of accelerator mass spectrometry was used to measure [ 14 C]‐HAL. The bioavailability of [ 14 C]‐HAL after intravesical and intravenous administration was determined from the respective area under the curve based on total radioactivity and was determined to be 7% (range, 5%–10%; 90% confidence interval). The systemic absorption of [ 14 C]‐HAL after intravesical administration is low and supports previous clinical experience with HAL showing no systemic side effects.