Pharmacokinetic studies with a dual-release formulation of levodopa, a novel principle in the treatment of Parkinson's disease

Eur Neurol. 1998;39(2):119-24. doi: 10.1159/000007918.

Abstract

The objectives of the two studies reported here were the investigation of the influence of tablet breaking and food on the pharmacokinetics of levodopa and 3-O-methyldopa (3-OMD) after administration of a new levodopa/benserazide formulation with a biphasic drug delivery profile (Madopar DR). Both studies had an open-label, randomised, two-way crossover design and were conducted in 12 healthy young subjects. The pharmacokinetics of levodopa and 3-OMD after one intact or two halved tablets were very similar with average Cmax and tmax 1.9 mg x l(-1) and 1.2 h, respectively. Administration of the formulation after a standard breakfast did not influence the extent of levodopa absorption but increased the absorption rate. Cmax and tmax were on average 2.1 mg x l(-1) and 1.3 h, respectively, in the fed condition and 1.5 mg x l(-1) and 2.5 h in the fasted condition. The presence of food did not markedly affect the plateau in levodopa levels between about 1 and 3 h after intake. In conclusion, the release characteristics in healthy subjects of the new levodopa/benserazide formulation are influenced only to a minor extent by concomitant intake of food or by tablet breaking.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Antiparkinson Agents / adverse effects
  • Antiparkinson Agents / pharmacokinetics
  • Antiparkinson Agents / therapeutic use*
  • Cross-Over Studies
  • Delayed-Action Preparations
  • Female
  • Food
  • Humans
  • Levodopa / adverse effects
  • Levodopa / pharmacokinetics
  • Levodopa / therapeutic use*
  • Male
  • Parkinson Disease / drug therapy*
  • Parkinson Disease / metabolism
  • Tablets
  • Tyrosine / analogs & derivatives*
  • Tyrosine / pharmacokinetics

Substances

  • Antiparkinson Agents
  • Delayed-Action Preparations
  • Tablets
  • Tyrosine
  • Levodopa
  • 3-methoxytyrosine