Pharmacokinetics of nitroglycerin and its metabolites after administration of sustained-release tablets.
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.
Kwon
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College of Pharmacy, University of Florida, Gainesville 32610.
Green
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Curry
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D000284:Administration, Oral; D000286:Administration, Sublingual; D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D006207:Half-Life; D006801:Humans; D008297:Male; D005996:Nitroglycerin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics*; D013607:Tablets
D003692:Delayed-Action Preparations; D013607:Tablets; C014509:dinitroglycerol; D005996:Nitroglycerin