Pharmacokinetics of oxatomide given percutaneously to healthy volunteers.
The percutaneous absorption of oxatomide gel at 5 per cent concentration was studied after single and repeated administration (85 mg b.i.d.) in six male and six female healthy volunteers, aged 25.7 +/- 0.8 years (mean +/- SEM) weighing 64.4 +/- 4.5 kg and the results compared with those obtained following a single oral dose (30 mg). The measurement of oxatomide was by means of a new sensitive and specific HPLC assay with limits of detection of 0.2 ng ml-1 in plasma and 1.0 ng ml-1 in urine. Poor percutaneous absorption was confirmed by the peak plasma concentrations which were 5.03 +/- 0.79 ng ml-1 following application of the gel for 7 days and 10.08 +/- 1.29 ng ml-1 following oral administration; the corresponding amounts of unchanged oxatomide recovered from 24 h urine collections were 1.42 +/- 0.39 micrograms and 3.93 +/- 0.92 micrograms.
Benvenuti
C
C
Medical Department, Puropharma, Milan-Italy.
Broggini
M
M
Botta
V
V
Valenti
M
M
Broccali
G
G
Dal Bo
L
L
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000328:Adult; D004334:Drug Administration Schedule; D005260:Female; D005782:Gels; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D010879:Piperazines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D012015:Reference Standards; D015203:Reproducibility of Results; D012869:Skin Absorption
D005782:Gels; D006634:Histamine H1 Antagonists; D010879:Piperazines; C015408:oxatomide