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

✍ Scribed by Hae-Ryun Kwon; Preston Green; Dr Stephen H. Curry

• Publisher: John Wiley and Sons
• Year: 1992
• Tongue: English
• Weight: 638 KB
• Volume: 13
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510130208

✦ Synopsis

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.