title: In vitro controlled release of vinpocetine-cyclodextrin-tartaric acid multicomponent complexes from HPMC swellable tablets.
abstract: The objective of this study was to investigate the effect of multicomponent complexation (MCC) of vinpocetine (VP), a poorly soluble base-type drug, with beta-cyclodextrin (betaCD), sulfobutylether beta-cyclodextrin (SBEbetaCD), tartaric acid (TA), polyvinylpyrrolidone (PVP) and hydroxypropylmethylcellulose (HPMC), on the design of controlled release hydrophilic HPMC tablets and to evaluate their in vitro release profiles by a pH gradient method. Multicomponent complexation led to enhanced dissolution properties of VP both in simulated gastric and intestinal fluids, and became possible the development of HPMC tablet formulations with more independent pH dissolution profiles. Drug release process was investigated experimentally using USP apparatus 3 and by means of model-independent parameters. Responses studied included similarity of dissolution profiles, time for 60% of the drug to dissolve (T(60%)), percent of VP released after 7 h (PD(7 h)) and the dissolution efficiency parameter at 12 h (DE(12 h)). Influence of multicomponent complexation was proved to increase the release of VP from HPMC tablets and superior PD(7 h) and DE(12 h) values were obtained in formulations containing VP-CD-TA complexes. Results supported the use of HPMC matrices to provide a useful tool in retarding the release of VP and that dissolution characteristics of the drug may be modulated by multicomponent complexation in these delivery systems, suggesting an improvement on VP bioavailability.
authors.affiliation: Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, 3000-004 Coimbra, Portugal. laura_ribeiro@lycos.com
authors.forename: Laura
authors.initials: L
authors.lastname: Ribeiro
authors.forename: Domingos C
authors.initials: DC
authors.lastname: Ferreira
authors.forename: Francisco J B
authors.initials: FJ
authors.lastname: Veiga
mesh_terms: D001826:Body Fluids; D004339:Drug Compounding; D005753:Gastric Mucosa / Q000378:metabolism; D006801:Humans; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D007413:Intestinal Mucosa / Q000378:metabolism; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008954:Models, Biological; D012995:Solubility; D013608:Tablets, Enteric-Coated; D013644:Tartrates / Q000737:chemistry*; D014748:Vinca Alkaloids / Q000737:chemistry*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D013608:Tablets, Enteric-Coated; D013644:Tartrates; D014748:Vinca Alkaloids; D047392:beta-Cyclodextrins; D065347:Hypromellose Derivatives; C013983:vinpocetine; D008747:Methylcellulose; C031215:betadex; C029768:tartaric acid