Samoemulgující systém (SEDDS) pro podání léčiva ibuprofen: hodnocení vzorků v podmínkách in vitro a in vivo

English version

Autoři: Subhash Chandra Bose Penjuri; Saritha Damineni; Nagaraju Ravouru; Srikanth Reddy Poreddy
Vyšlo v časopise: Čes. slov. Farm., 2017; 66, 23-34
Kategorie: Původní práce

Souhrn

Cílem této studie bylo vyvinout samoemulgující systém (SEDDS) pro perorální podání těžce rozpustného léčiva ibuprofenu a zhodnotit jeho biologickou dostupnost. K určení fázového chování mikroemulzí a srovnání účinnosti různých směsí povrchově aktivní látky a oleje byly sestaveny fázové diagramy. Samoemulgující systémy ibuprofenu byly připraveny ze směsi Labrafilu M2125, Cremophoru RH40 a Plurol oleique. U připravených emulzí bylo hodnoceno jejich chování v podmínkách in vitro a in vivo. FTIR hodnocení nepotvrdilo žádnou interakci mezi léčivem a pomocnými látkami. DSC studie prokázaly, že léčivo je v systému solubilizováno. Vzorky byly dále hodnoceny na termodynamickou stabilitu, dispersibilitu, index lomu, viskozitu a bod zákalu. Připravené vzorky ukázaly negativní náboj částic vnitřní fáze, což ukazuje na jejich stabilitu. Systém optimalizovaného složení představoval mikroemulzi s velikostí vnitřní fáze 177,5 nm. Množství uvolněného léčiva v podmínkách in vitro bylo významně vyšší než u přípravku dostupného na trhu a čistého léčiva. Farmakodynamické studie optimalizované složení ukázala vyšší protizánětlivý účinek ve srovnání s přípravkem dostupným na trhu a čistým léčivem. Hodnoty AUC a C_max po perorálním podání byly vyšší pro SEDDS s obsahem ibuprofenu ve srovnání s přípravkem dostupným na trhu. Dosažené výsledky naznačují, že SEDDS by mohl být užitečnou alternativou pro zvýšení biologické dostupnosti špatně rozpustných léčiv.

Klíčová slova:
ibuprofen • samoemulgující systém • fázový diagram • zeta potenciál • protizánětlivá aktivita

Zdroje

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