Studies on the bioavailability of glyceryl trinitrate after sublingual administration of spray and tablet
Jensen, K.M.; Mikkelsen, S.
Arzneimittel-Forschung 47(6): 716-718
1997
ISSN/ISBN: 0004-4172 PMID: 9239449 Document Number: 1226
The plasma profiles of nitroglycerin (glyceryl trinitrate, GTN, CAS 55-63-0) were estimated after two sublingual puffs of 0.4 mg GTN from a fluorochlorohydrocarbon (FCH)-free oral spray and one sublingual tablet of 0.5 mg GTN (Nitromex). The study was carried out in an open, randomized, two-phase, cross-over design with 24 volunteers. Eighteen blood samples were taken within 30 minutes after administration, and the plasma concentrations of GTN were determined by a specific gas chromatographic method with electron capture detection. The pharmacokinetic parameters, C-max, t-max, and AUC, were determined for each volunteer. After correction-of the AUC and C-max values of the oral spray by dividing by two, the ratios (spray/tablet) of the AUC and C-max and the 90 % confidence intervals were estimated. The plasma concentrations of GTN (mean) after the spray (dose: 0.8 mg GTN) reached a maximum of 3.96 ng/ml (range: 0.99-10,86) at 3.5 minutes (range: 2-5). The plasma concentrations of GTN (mean) after the tablet (dose: 0.5 mg GTN) reached a maximum of 1.97 ng/ml (range: 0.57-4.33) at 4.9 minutes (range: 3-7). The corrected ratios (spray/tablet) of AUC and C-max were 1.02 and 0.97 with the 90 % confidence intervals (0.80, 1.30), respectively (0.77, 1.24). The results indicate that the oral spray in a dose of 0.4 mg is equivalent to the sublingual tablet in a dose of 0.5 mg.
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