Summary
Scalp hair samples were obtained every month for three months after administration from healthy male volunteers who participated in the phase I study of a new antimicrobial fluoroquinolone derivative (Q-35). Hairs were cut into 1 cm long pieces successively from the scalp end. Corresponding pieces of 5 hair strands were dissolved in 1M NaOH and assessed for Q-35 by HPLC. The drug was detectable in the hairs of all subjects taking either a single (400 mg,n = 6) or repeated oral doses of Q-35 (400 mg/day for 6.5 days, total 2600 mg,n = 6). The hair portions containing the drug were shown in most subjects to move outwards along the hair shafts month by month in proportion to the hair growth rate of about 1 cm/month. Q35 (600 mg/day) was also given to 6 healthy male volunteers for 6.5 days (total 3900 mg) and hair samples were obtained 1 and 3 months after administration. When Q-35 was analyzed along a single hair shaft, the drug was detectable only in 1–2 consecutive 1 cm long pieces, which were also shown to move outwards along the hair shaft with time. A detailed analysis revealed that the drug was contained only in 2–4 consecutive 2.5 mm long pieces of a single hair collected after 3 months, showing that there was no significant axial diffusion of the drug along the hair shaft with time. These findings indicate the utility of measuring this fluoroquinolone derivative in human scalp hair as an index of drug exposure and as a time marker for analyzing other drug(s) in hair.
Zusammenfassung
Kopfhaarproben wurden über einen Zeitraum von 3 Monaten monatlich von gesunden männlichen freiwilligen Versuchspersonen erhalten, welche in Verbindung mit einer Phase I-Studie ein neues antimikrobielles Fluorochinolon-Derivat (Q-35) erhalten hatten. Die Haare wurden sukzessive in 1 cm lange Stücke zerschnitten. Korrespondierende Teile von insgesamt 5 Haarsträngen wurden in 1M NaOH gelöst und mittels einer HPLC-Methode auf Q-35 untersucht. Die Verbindung war erkennbar in den Haaren aller Versuchspersonen nachzuweisen, welche entweder eine einzelne (400 mg,n = 6) oder wiederholte orale Dosen von Q-35 (400 mg/Tag für 6,5 Tage, insgesamt 2.600 mg,n = 6) erhalten hatten. Die Haarabschnitte, welche die Substanz enthielten, erwiesen sich bei den meisten Versuchspersonen als auswärts wandernde Haarschäfte, welche entsprechend zur Haarwuchsgeschwindigkeit ungefähr 1 cm pro Monat nach außen wuchsen. Q-35 (600 mg/Tag) wurde auch 6 gesunden männlichen freiwilligen Probanden für die Dauer von 6,5 Tagen gegeben (insgesamt 3.900 mg) und Haarproben über einen Zeitraum von 1–3 Monaten nach der Gabe gesammelt. Wurde Q-35 entlang eines einzelnen Haarschaftes analysiert, war die Substanz nur in 1-2 konsekutiven, 1 cm langen Stücken detektierbar; auch diese zeigten eine Auswärtsbewegung des Haarschafts über die Zeit. Weitergehende Analysen zeigten, daß die Droge nur in 2–4 konsekutiven, 2,5 mm langen Stücken des Haares enthalten war, welches 3 Monate gesammelt worden war; hierdurch wird gezeigt, daß keine bedeutsame zeitabhängige axiale Diffusion der Substanz entlang des Haarschafts stattfindet. Diese Befunde zeigen die Anwendbarkeit dieses Fluorochinolon-Derivats in menschlichen Kopfhaarproben als Index für eine Substanzaufnahme und als Zeitmarker für die Analyse anderer Drogen im Haar an.
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Uematsu, T., Ohsawa, Y., Mizuno, A. et al. Analysis of a new fluoroquinolone derivative (Q-35) in human scalp hair as an index of drug exposure and as a time marker in hair. Int J Leg Med 106, 237–243 (1994). https://doi.org/10.1007/BF01225412
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DOI: https://doi.org/10.1007/BF01225412