Cyclodextrin multicomponent complexation and controlled release delivery strategies to optimize the oral bioavailability of vinpocetine

• Type: Article in International Scientific Journal
• Date: 2007

Authors

Laura S S Ribeiro (Author) Other; Amilcar C Falcao (Author) Other; Joao A B Patricio (Author) Other; Domingos C Ferreira (Author) FFUP; Francisco J B Veiga (Author) Other

Journal

Title: Journal of Pharmaceutical Sciences

Vol. 96

Pages: 2018-2028

ISSN: 0022-3549

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 20 Citations

Scopus - 25 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-004-8JG

DOI: 10.1002/jps.20294

Abstract (EN): In the present work, to maintain a suitable blood level of vinpocetine (VP) for a long period of time, VP-cyclodextrin-tartaric acid multicomponent complexes were prepared and formulated in hydroxypropylmethylcellulose matrix tablets. In vitro and in vivo performances of these formulations were investigated over a VP immediate release dosage form. Solubility studies were performed to evaluate the drug pH solubilization profile and to assess the effect of multicomponent complexation on VP solubility. The drug release process was investigated using United States Pharmacopeia apparatus 3 and a comparative oral pharmacokinetic study was subsequently undertaken in rabbits. Solubility studies denoted the pH-solubility dependence of VP and solubility improvement attained by complexation. Dissolution results showed controlled and almost complete release behavior of VP over a 12-h period from complex hydroxypropylmethylcellulose-based formulations. A clear difference between the pharmacokinetic patterns of VP immediate release and VP complex-based formulations was revealed. The area under the plasma concentration-time curve after oral administration of complex-based formulations was 2.1-2.9 times higher than that for VP immediate release formulation. Furthermore, significant differences found for mean residence time, elimination half-life, and elimination rate constant values corroborated prolonged release of VP from complex-based formulations. These results suggest that the oral bioavailability of VP was significantly improved by both multicomponent complexation and controlled release delivery strategies. (c) 2007 Wiley-Liss, Inc.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11