Comparative single- and multiple-dose pharmacokinetics of levodopa and 3-O-methyldopa following a new dual-release and a conventional slow-release formulation of levodopa and benserazide in healthy subjects
| Autor: | J. Dingemanse, U.E. Gasser, Ch. Crevoisier, M Ouwerkerk, G. Lankhaar |
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| Rok vydání: | 1998 |
| Předmět: |
Levodopa
Time Factors Parkinson's disease Metabolic Clearance Rate Biological Availability Pharmaceutical Science Pharmacology Drug Administration Schedule Benserazide chemistry.chemical_compound Pharmacokinetics Oral administration medicine Humans Methyldopa Cross-Over Studies Chemistry Fasting General Medicine medicine.disease Bioavailability Drug Combinations Delayed-Action Preparations Tyrosine 3-O-Methyldopa Biotechnology medicine.drug |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 46:223-228 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/s0939-6411(98)00022-8 |
| Popis: | A multiple-dose study was performed to assess the pharmacokinetic profile of a new levodopa/benserazide dual-release formulation (DRF) in comparison with a conventional slow-release formulation (SRF). The study was of an open label, randomized, two-way cross-over design and was conducted in 18 subjects. Assessment of the two formulations was at day 1 (single-dose) and at day 7 after a 5-day t.i.d. pre-treatment (100 mg levodopa and 25 mg benserazide) in fasting state. The pharmacokinetic parameters reflecting bioavailability, accumulation and metabolism of levodopa were determined. The levodopa pharmacokinetics of the new DRF showed rapid absorption ( t max =1.1 h), followed by sustained levodopa plasma concentrations, similar to the SRF. Following multi-dose administration, the peak plasma concentration of the new DRF was 90% higher compared to the SRF ( C max =2.1 and 1.1 μ g/ml, respectively). The bioavailability was significantly increased by 40% (AUC 0–∞ =6.1 and 4.3 μ g×h/ml, respectively). The new DRF was well tolerated as shown by the low incidence of mild side effects. In conclusion, the results of this study confirmed the levodopa dual-release properties of this new levodopa/benserazide formulation. |
| Databáze: | OpenAIRE |
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