Oslobađanje celekoksiba iz mukoadhezivnih diskova s polimerima poliaspartamidnog tipa

Abstract

A series of mucoadhesive disks with celecoxib as a model drug of very low aqueous solubility were prepared and characterized. Two polymers of polyaspartamide type, poly,-(N-2-hydroxyethyl-DL-aspartamide) (PHEA, 1) and its thiolated analogue poly[α,β-(N-2-hydroxyethyl-DL-aspartamide)]-poly[α,β-(N-2-thioethyl-DL-aspartamide)] copolymer (PHTA, 2a,b), and two commercially available polymers Carbopol 934P and hydroxypropylmethyl cellulose 4000 were used as excipients. Disks containing a mixture of equivalent amounts of thiomer 2b and Carbopol 934P as an excipient exhibited the highest dissolution rate.Pripravljeni su i karakterizirani mukoadhezivni diskovi s celekoksibom kao lipofilnom modelnom supstancijom. Kao ekscipiensi uporabljena su dva polimera poliaspartamidnog tipa, poli[α,β-(N-2-hidroksietil-DL-aspartamid) (PHEA, 1) i njegov tiolirani analog poli[α,β-(N-2-hidroksietil-DL-aspartamid)]-poli[α,β-(N-2-tioetil-DL-aspartamid)] kopolimer (PHTA, 2a,b), te dva komercijalno dostupna polimera Carbopol 934P i hidroksipropilmetilceluloza 4000. Najbolji profil oslobađanja celekoksiba postignut je iz diskova sastavljenih od tiomera 2b i Carbopola 934P u masenom omjeru 1:1