Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2022 Oct 15;11(1):97-115.
doi: 10.5599/admet.1474. eCollection 2023.

Pharmaceutical and pharmacokinetic evaluation of a newly formulated multiparticulate matrix of levodopa and carbidopa

Emelia Priscilla Imbeah  1 , Ofosua Adi-Dako  2 , Benoit Banga N'guessan  3 , Kennedy Kwami Edem Kukuia  1 , Benedicta Obenewaa Dankyi  1 , Ismaila Adams  1 , Ebenezer Ofori-Attah  4 , Regina Appiah-Opong  4 , Seth Kwabena Amponsah  1
Affiliations

Pharmaceutical and pharmacokinetic evaluation of a newly formulated multiparticulate matrix of levodopa and carbidopa

Emelia Priscilla Imbeah et al. ADMET DMPK. .

Abstract

Levodopa is routinely co-administered with carbidopa in the management of Parkinson's disease. Although the aforementioned combination therapy is effective, there may be fluctuating plasma levels of levodopa after oral administration. We formulated and evaluated the kinetic characteristics of the chitosan-pectin-based multiparticulate matrix of levodopa and carbidopa. Pectin was extracted from the cocoa husk, and the chitosan-pectin-based matrix was prepared by wet granulation. Formulations were evaluated for drug-excipient compatibility, drug content, precompression properties and in vitro release. For pharmacokinetic evaluation, rats were put into groups and administered either chitosan-pectin based matrix of levodopa/carbidopa, Sinemet® CR or levodopa/carbidopa immediate release powder. Rats were administered the different formulations of levodopa/carbidopa (20/5 mg/kg) per os every 12 hours. The pharmacokinetic parameters of levodopa were estimated for the various treatment groups. The percentage content of levodopa and carbidopa in the various formulations was within the acceptance criteria. The AUC0-24 for levodopa/carbidopa multiparticulate matrix (Formulation 3: 484.98 ± 18.70 μg.hr/mL); Formulation 4: 535.60 ± 33.04 μg.hr/mL), and Cmax (Formulation 3: 36.28 ± 1.52 μg/mL; Formulation 4: 34.80 ± 2.19 μg/mL) were higher than Sinemet® CR (AUC0-24 262.84 ± 16.73 μg.hr/mL and Cmax 30.62 ± 3.37 μg/mL). The t 1/2 of the new formulation was longer compared to Sinemet® CR.

Keywords: Chitosan; Formulation; Management; Parkinson’s disease; Pectin; Pharmacokinetics.

PubMed Disclaimer

Conflict of interest statement

Conflict of interest: The authors declare that they have no conflict of interest.

Figures

Figure 1.
Figure 1.
FTIR spectrum of CPH pectin
Figure 2.
Figure 2.
FTIR Spectra of levodopa, carbidopa, CPH pectin, chitosan and optimized formulations (F3 and F4)
Figure 3.
Figure 3.
In vitro release of levodopa (A) and carbidopa (B) from the various formulated multiparticulate matrices in phosphate buffered saline (pH = 6.8) at 37 °C (n=3). Error bars indicate SD.
Figure 4.
Figure 4.
In vitro release of levodopa (A) and carbidopa (B) from the optimized formulations F3 and F4 in phosphate buffered saline (pH = 4.5) at 37 °C (n=3). Error bars indicate SD.
Figure 5.
Figure 5.
Plasma concentration-time (A) and log concentration-time (B) curves of levodopa for the 4 treatment groups (n = 5) following administration of respective formulations administered at 20/5 mg/kg. Sinemet® CR = a controlled release formulation of levodopa/carbidopa. F3 = Formulation 3, F4 = Formulation 4, LC = levodopa plus carbidopa powder. Error bars indicate SD.
See this image and copyright information in PMC

Similar articles

See all similar articles

References

    1. Tysnes O.B., Storstein A. Epidemiology of Parkinson’s disease. Journal of Neural Transmission 124 (2017) 901–905. https://doi.org/10.1007/s00702-017-1686-y. 10.1007/s00702-017-1686-y - DOI - PubMed
    1. Kouli A., Torsney K.M., Kuan W.-L. Parkinson’s Disease: Etiology, Neuropathology, and Pathogenesis. in: Park. Dis. Pathog. Clin. Asp., 2018: pp. 3–26. https://doi.org/10.15586/codonpublications.parkinsonsdisease.2018.ch1. 10.15586/codonpublications.parkinsonsdisease.2018.ch1 - DOI - PubMed
    1. Ray Dorsey E., Elbaz A., Nichols E., Abd-Allah F., Abdelalim A., et al. . Global, regional, and national burden of Parkinson’s disease, 1990–2016: a systematic analysis for the Global Burden of Disease Study 2016. The Lancet Neurology 17 (2018) 939–953. https://doi.org/10.1016/S1474-4422(18)30295-3. 10.1016/S1474-4422(18)30295-3 - DOI - PMC - PubMed
    1. Williams U., Bandmann O., Walker R. Parkinson’s Disease in Sub-Saharan Africa: A Review of Epidemiology, Genetics and Access to Care. Journal of Movement Disorders 11 (2018) 53–64. https://doi.org/10.14802/jmd.17028. 10.14802/jmd.17028 - DOI - PMC - PubMed
    1. Arisoy S., Sayiner O., Comoglu T., Onal D., Atalay O., Pehlivanoglu B. In vitro and in vivo evaluation of levodopa-loaded nanoparticles for nose to brain delivery. Pharmaceutical Development and Technology 25 (2020) 735–747. https://doi.org/10.1080/10837450.2020.1740257. 10.1080/10837450.2020.1740257 - DOI - PubMed

LinkOut - more resources