In-vivo evaluation of prolonged release bilayer tablets of anti-Parkinson drugs in Gottingen minipigs

• Type: Article in International Scientific Journal
• Date: 2011

Authors

Jose Paulo S E Sousa e Silva (Author) FFUP; Jose S Lobo (Author) Other; Maria J Bonifacio (Author) Other; Rita Machado (Author) Other; Amilcar Falcao (Author) Other; Patrcio Soares da Silva (Author) FMUP

Journal

Title: Journal of Pharmacy and Pharmacology

Vol. 63

Pages: 780-785

ISSN: 0022-3573

Publisher: Oxford University Press

Indexing

ISI Web of Knowledge - 5 Citations

ISI Web of Science

Scopus - 5 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-002-R2C

DOI: 10.1111/j.2042-7158.2011.01278.x

Abstract (EN): Objectives Patients with Parkinson's disease can benefit from controlled released levodopa dosage forms since there is a clear clinical advantage in obtaining sustained plasma concentrations. The purpose of this study was to obtain a tablet that prolonged the release of levodopa. Methods A novel bilayer tablet, consisting of an immediate release layer containing nebicapone (100 mg) and an erosion-matrix type prolonged release layer containing levodopa (100 mg) and carbidopa (25 mg) was developed (LCN PR). A pharmacokinetic study in Gottingen minipigs was performed to evaluate this formulation. Key findings LCN PR tablets prolonged the in-vitro release of levodopa in HCl 0.1 m for more than 3 h. In-vivo plasma levodopa levels peaked at a later time point with LCN PR tablets as compared with that obtained with Sinemet 100/25 (2.7 vs 0.5 h). Nebicapone increased the maximum plasma concentration and area under the plasma concentration-time curve values for levodopa. Conclusions The results obtained suggested that LCN PR tablets may have decreased the number of tablets and daily intake in the treatment of patients with Parkinson's disease.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 6