• Home
  • Search Results
  • Pharmacokinetics of nitroglycerin and its metabolites after administration of sustained-release tablets.

Pharmacokinetics of nitroglycerin and its metabolites after administration of sustained-release tablets.

Biopharmaceutics & drug disposition (1992-03-01)
H R Kwon, P Green, S H Curry
ABSTRACT

Nitroglycerin was administered to eight healthy volunteers in the form of sublingual tablets, oral sustained-release tablets, and an oral solution. Blood samples were collected for measurement of nitroglycerin and its two isomeric glyceryl dinitrate metabolites. Blood pressure and pulse rate were monitored; subjective evaluations of headache, dizziness, facial flushing, skin irritation, and gastrointestinal upset were made. Nitroglycerin itself was virtually undetectable after the solution and tablet preparations; the metabolites were consistently detectable from a few minutes after dosing to 24 h later. Mean total (nitroglycerin plus metabolite) concentrations were comparable in the 15 min following sublingual administration, and the 8 h following tablet administration. The relative bioavailability of the tablets in comparison with the oral solution was 70 per cent based on metabolite concentrations. Nitroglycerin sustained-release tablets appear to exert their beneficial effects in the prolonged prophylaxis of angina through active metabolites.

MATERIALS
Product Number
Brand
Product Description

Supelco
1,3-Dinitroglycerin solution, 1.0 mg/mL in acetonitrile, ampule of 1 mL, certified reference material, Cerilliant®
Supelco
1,3-Dinitroglycerin solution, 100 μg/mL in acetonitrile, ampule of 1 mL, certified reference material, Cerilliant®