preparation In vitro and In vivo studies
Dritan Hasa (Avtor), Simon Žakelj (Avtor), Iztok Grabnar (Avtor), Francesco Cilurzo (Avtor), Stefano Dall'Acqua (Avtor), Antonella Riva (Avtor), Beatrice Perissutti (Avtor), Dario Voinovich (Avtor)

Povzetek

Dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) is the main component of Echinacea angustifolia DC. lipophilic extract, the bioavailability and immunomodulatory effect after oral administration in soft gel capsules in healthy volunteers of which we have already demonstrated. In the present work, we assessed the transdermal administration as an alternative route of administration of such an alkamide. The first step, therefore, encompassed the preparation of a drug-in-adhesive patch with an area of 868 mm2 and containing a dose of 0.64 mg of tetraene. In vitro skin permeation studies in Franz-type diffusion chambers resulted in a tetraene flux of (103 - 10) ng +- cm-2 - h-1 with a very good linearity (r = 0.99). The relatively low lag time of just 13 min indicates low binding and the accumulation of tetraene in the skin. Finally, the patch was administered to six healthy volunteers, and the pharmacokinetic analysis was performed by nonlinear mixed effects modelling with soft gel oral capsules serving as the reference formulation. The in vivo results correlated well with the in vitro permeation and indicated an initial burst tetraene absorption from the patch that was in parallel with the zero-order kinetics of absorption. The rate of the latter process was in good agreement with the one estimated in vitro. The tetraene absorption rate was therefore slow and prolonged with time, resulting in a bioavailability of 39% relative to the soft gel capsules and a very flat plasma concentration profile.

Ključne besede

Echinacea angustifolia lipophilic extract;tetraene;drug-in-adhesive patch;in vitro skin permeation;pharmacokinetic;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 615.015
COBISS: 37568515 Povezava se bo odprla v novem oknu
ISSN: 1999-4923
Št. ogledov: 151
Št. prenosov: 46
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Sekundarne ključne besede: lipofilni ekstrakt Echinacea angustifolia;tetraen;zdravilna učinkovina v adhezivnem obližu;prehod skozi kožo in vitro;Farmakokinetika;
Vrsta dela (COBISS): Članek v reviji
Strani: str. 1-11
Letnik: ǂVol. ǂ12
Zvezek: ǂiss. ǂ11
Čas izdaje: 2020
DOI: 10.3390/pharmaceutics12111096
ID: 14344612