Original Article

Clinical Pharmacology and Therapeutics (1984) 36, 765–772; doi:10.1038/clpt.1984.255

Plasma nitroglycerin concentrations and hemodynamic effects of sublingual, ointment, and controlled-release forms of nitroglycerin

Supported in part by Kremers-Urban Company, Milwaukee, Wis. A preliminary report of this work has been presented.8

Stephen H Curry PhD, Hae-Ryun Kwon BS, John H Perrin PhD, John R Culp MD, Carl J Pepine MD, Wing C Yu MS and Jane L Stevens MS Gainesville, Fla., and Waltham, Mass.

Colleges of Pharmacy and Medicine, University of Florida, Gainesville, and Thermo Electron Corporation, Waltham

Correspondence: Stephen H Curry PhD, Box J-4, University of Florida, Gainesville, FL 32610.

Received 6 June 1984; Accepted 13 September 1984.

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Abstract

After a sublingual test dose, 12 healthy men aged 21 to 29 yr were treated with controlled-release transdermal nitroglycerin skin patches designed to deliver 10 mg/day nitroglycerin and with nitroglycerin ointment (2%) (1-in amount from the tube spread over 50 cm2) for 24 hr in a double-blind crossover study. Assessment was by measurement of nitroglycerin in plasma, blood pressure, and pulse rate. The mean plasma concentration of nitroglycerin during ointment dosing was approximately 200% to 400% that during skin patch dosing. Levels during ointment dosing were closer to those from sublingual dosing than were those during skin patch dosing. Blood pressure and pulse rate changes were much the same during both transdermal treatments. Calculations showed that delivery of nitroglycerin from the skin patches would have to be over 40 to 80 cm2 of the skin to achieve nitroglycerin exposure of the order of that induced by 1 in of ointment spread over 50 cm2 or from sublingual dosing.

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