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Pharmacokinetics of a Rivastigmine Transdermal Patch Formulation in Healthy Volunteers: Relative Effects of Body Site Application

Gilbert Lefèvre, PhD, Greg Sdek, MD, PhD, Hsun-Lun Aaron Huang, PharmD, Marc Saltzman, MD, Mitchell Rosenberg, MD, Beate Kiese, MSc and Peter Fordham, PhD

From Novartis Pharma AG, Basel, Switzerland (Dr Lefèvre, Ms Kiese); Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Sdek, Dr Huang); Parkway Research Center, North Miami Beach, Florida (Dr Saltzman, Dr Rosenberg); and SGS Cephac Europe, Saint Benoit, France (Dr Fordham).

A patch formulation of rivastigmine, an inhibitor of acetylcholinesterase and butyrylcholinesterase, is under development. The current objective was to evaluate the pharmacokinetic profile and patch adhesiveness following application at the upper back, chest, abdomen, thigh, and upper arm. In a single-dose, open-label, crossover study with 40 (42.5% men) healthy subjects, a 10-cm² patch containing 18 mg rivastigmine was applied to each body site. Median t_max was 16 hours for all sites except the thigh (22 hours). Exposure levels and C_max were highest at the upper back, chest, and upper arm sites. Adhesiveness was greatest when applied to the thigh, followed by the abdomen, upper arm, chest, and upper back, although no statistically significant correlations with pharmacokinetic parameters were found, except at the chest (P = .02). Pharmacokinetic profiles and adhesiveness of the upper back, chest, and upper arm, coupled with low rates of erythema at these sites, suggest their suitability for clinical use.

Key Words: Adhesiveness • Alzheimer's disease • pharmacokinetics • rivastigmine • transdermal patch

Address for reprints: Dr Gilbert Lefèvre, Novartis Pharma AG, Exploratory Development, WSJ-210.4.25, CH-4002 Basel, Switzerland; e-mail: gilbert.lefevre{at}novartis.com.

This article has been cited by other articles:

				J. Cummings, G. Lefevre, G. Small, and S. Appel-Dingemanse Pharmacokinetic rationale for the rivastigmine patch Neurology, July 24, 2007; 69(4_suppl_1): S10 - S13. [Abstract] [Full Text] [PDF]