Návrh a vývoj systému pro transmukózní přívod diltiazem hydrochloridu

English version

Autoři: Subhash Chandra Bose Penjuri; Saritha Damineni; Nagaraju Ravouru
Vyšlo v časopise: Čes. slov. Farm., 2013; 62, 19-27
Kategorie: Původní práce

Souhrn

Diltiazem hydrochlorid je antihypertenzní látka, která vykazuje značný first pass metabolismus, a to ji činí vhodným kandidátem pro bukální podání. Mukoadhezivní bukální náplasti byly připraveny s HPMC, chitosanem, PVP, PVA a carbopolem. Fyzikálně-chemické interakce mezi léčivem a polymery byly sledovány pomocí FTIR a DSC: stanovení neprokázala žádné interakce mezi diltiazem hydrochloridem a polymery. U bukálních náplastí se stanovily různé fyzikálně-chemické parametry, uvolňování léčiva in vitro a permeace ex vivo přes bukální sliznici prasete. Zbytkové obsahy rozpouštědel v náplastech se určily plynovou chromatografií a byly pod tolerovanými limity. Při ex vivo studii se léčivo z náplastí uvolňovalo rovnoměrně po dobu 12 hodin kinetickým modelem podle Korsmeyer-Peppase. Stabilita optimalizované formulace se zkoumala podle pokynů ICH a z hlediska obsahu léčiva a jeho permeace ex vivo vykazovala výborné výsledky.

Klíčová slova:
diltiazem hydrochlorid • bukální náplasti • bytková rozpouštědla • mukoadheze, uvolňování léčiva in vitro • permeace ex vivo

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