Pharmacokinetics, Pharmacodynamics, and Safety of a Single Escalating Dose and Repeated Doses of Rasagiline Transdermal Patch in Healthy Chinese Subjects

Abstract A rasagiline transdermal patch can be used to offer continuous rasagiline to patients with Parkinson's disease who cannot take their usual oral medications. This was the first study to investigate the pharmacokinetics, pharmacodynamics, and safety of the rasagiline transdermal patch in healthy Chinese subjects. Thirty subjects were randomized to 3 groups with 10 subjects in each group. The 10 subjects of group 1 received a single 1‐mg dose of rasagiline as a tablet; the 20 subjects of groups 2 and 3 received a single transdermal patch (48‐hour patch‐on period) containing 1.25 mg and 2.5 mg rasagiline, respectively. After a 2‐week washout period, the subjects of group 1 were assigned to receive 1 mg of rasagiline tablets every 24 hours for 7 days, and the subjects of group 2 were assigned to receive 1.25‐mg rasagiline transdermal patches (48‐hour patch‐on period) every 72 hours for 5 time periods. The absorption of rasagiline from the transdermal patch was significantly improved, although the peak plasma concentration was obviously reduced. There was slight accumulation of rasagiline dose after multiple administrations. Inhibition of platelet monoamine oxidase‐B (MAO‐B) activity was dose dependent. The 80% inhibition maintained for at least 48 hours after multiple‐dose administration of 1 mg tablets, and for 72 hours after multiple‐dose administration of 1.25 mg/48 h patch. Compared with rasagiline tablets, the transdermal patch had a prolonged duration of 80% inhibition and increased maximal inhibition of MAO‐B activity. These characteristics permitted an interval of 3 days of dosing, which was convenient for patients to use.