Absolute bioavailability of glyceryl trinitrate from a transdermal system, assessed by digital plethysmography
Isenschmid, M.; Müller, M.; Bührer, M.; Vorkauf, H.; Bircher, J.
International Journal of Clinical Pharmacology Therapy and Toxicology 23(7): 345-351
1985
ISSN/ISBN: 0174-4879 PMID: 3928505 Document Number: 243007
The absolute bioavailability of glyceryl trinitrate from a transdermal therapeutic system (Nitroderm TTS, 20 cm2) was assessed with a new method in 6 healthy volunteers. Instead of measuring plasma concentrations the pharmacological effects of glyceryl trinitrate were followed by digital plethysmography. Each experiment consisted of the establishment of an intravenous dose response curve which was followed by a 1-hour application of the transdermal system and a second intravenous dose response curve. The investigations were repeated after pretreatment of each subject with 0.4 mg pindolol i.v. The results show a satisfactory overall consistency of the data and indicate a release rate of 4.4 +/- SD 1.7 micrograms/min of bioavailable glyceryl trinitrate during the first hour of application of this transdermal system. This corresponds to 75 +/- 29% of the release rate obtained by analysis of residual amounts in the TTS.