Abstract
We investigated the single-dose pharmacokinetics of 5 different levodopa sustained-release (SR) formulations in healthy volunteers. All SR formulations showed a very different profile from that of a standard formulation. In all cases, the SR formulations prolonged the time to peak levodopa blood levels. The rate of absorption is reduced as evidenced by the peak levels being lower and smoother. In some cases there is a tendency to produce a plateau rather than a peak, which lasts for between 1 and 4 hours. On the basis of available pharmacokinetic parameters, we selected an SR formulation which would appear to be the most suitable candidate. A pilot trial with this formulation in 5 Parkinson patients with motor fluctuations confirmed the results of the volunteer studies.
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