Pharmacokinetic investigations of various levodopa formulations

  • M. Gerlach
  • W. Kuhn
  • H. Przuntek
Part of the Key Topics in Brain Research book series (KEYTOPICS)


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.


Parkinson Patient Motor Fluctuation Levodopa Therapy Standard Preparation Pharmacokinetic Investigation 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Cedarbaum JM, Breck L, Kutt H, McDowell FH (1987) Controlled-release levodopa/carbidopa. II Sinemet CR 4 treatment of response fluctuations in Parkinson’s disease. Neurology 37: 1607–1612PubMedGoogle Scholar
  2. Gerlach M, Klaunzer N, Przuntek H (1986) Determination of L-Dopa and 30-methyl-Dopa in human plasma by extraction using C18 cartridges followed by high-performance liquid chromatographic analysis with electrochemical detection. J Chromatogr 380: 379–385CrossRefGoogle Scholar
  3. Gerlach M, Gebhardt B, Kuhn W, Przuntek H (1988) Pharmacokinetic studies with sustained-release formulation of levodopa in healthy volunteers. J Neural Transm [Suppl] 27: 211–218Google Scholar
  4. Goetz CG, Tanner CM, Klawans HL, Shannon KM, Carroll VS (1987) Parkinson’s disease and motor fluctuations: Long-acting carbidopa/ levodopa (CR-4-Sinemet). Neurology 37: 875–878PubMedGoogle Scholar
  5. Gundert-Remy UR, Hildebrandt R, Stiehl A, Weber E, Zürcher G, Da Prada M (1983) Intestinal absorption of levodopa in man. Eur J Clin Pharmacol 25: 69–72PubMedCrossRefGoogle Scholar
  6. Juncos IL, Fabbrini G, Mouvadian MM, Serrati C, Kask AM, Chase TN (1987) Controlled release levodopa treatment of motor fluctuations in Parkinson’s disease. Neurol Neurosurg Psychiatr 50: 194–198CrossRefGoogle Scholar
  7. Marsden CD, Rinne UK, Koella WP, Dubius R (eds) (Madopar) HBS. International workshop on the “On-Off’-phenomenon in Parkinson’s disease: New possibilities for its management, Agno, 1985. Europ Neurol 27 [Suppl] 1Google Scholar
  8. Nutt IG, Fellman IH (1984) Pharmocokinetics of levodopa. Clin Neuropharmacol 7: 35–49PubMedCrossRefGoogle Scholar
  9. Nutt IG, Woodward WR, Carter IH (1986) Clinical and biochemical studies with controlled-release levodopa/carbidopa. Neurology 36: 1206–1211PubMedGoogle Scholar
  10. Pincus IH, Barry K (1987) Influence of dietary protein on motor fluctuations in Parkinson’s disease. Arch Neurol 44: 270–272PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag/Wien 1989

Authors and Affiliations

  • M. Gerlach
    • 1
  • W. Kuhn
    • 2
  • H. Przuntek
    • 3
  1. 1.Department of NeurologyUniversity of WürzburgFederal Republic of Germany
  2. 2.Department of PsychiatryUniversity of WürzburgFederal Republic of Germany
  3. 3.Department of NeurologyRuhr-Universität BochumFederal Republic of Germany

Personalised recommendations