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  • Characterization of ternary...
    El-Maradny, Hoda; Mortada, Sana; Kamel, Ola; Hikal, Ahmed

    Acta pharmaceutica (Zagreb, Croatia), 12/2008, Letnik: 58, Številka: 4
    Journal Article

    Ternary complexes of meloxicam (ME) (a poorly water soluble anti-inflammatory drug) with hydroxypropyl-β-cyclodextrin (HPβCD) and either a hydrophilic polymer, namely, polyvinyl pyrrolidone (PVP) or a basic amino acid such as L-arginine, were prepared by the spray-drying technique. The solubilizing efficiency, physical properties and dissolution behaviour of each ternary system of ME-HPβCD with either PVP or L-arginine were compared with those of the corresponding binary system of ME-HPβCD. Tablets compressed from the ternary system of ME-HPβCD-L-arginine were compared with plain and commercial tablets. Phase solubility experiments suggested the formation of an inclusion complex of AL type. Ternary system of ME-HPβCD-L-arginine exhibited a stability constant 30.3 times higher than the binary system of ME-HPβCD, while the ternary system of ME-HPβCD-PVP increased the stability constant 2.2 times only. The prepared complexes were characterized by scanning electron microscopy, differential scanning calorimetry and infra red spectroscopy. Ternary solid complexes indicated the presence of strong interactions between the components. The dissolution behaviour of ME from different ternary complexes was higher than its dissolution from the binary system. Tablets compressed from ternary complexes of ME-HPβCD-L-arginine highly improved drug release compared to plain and commercial tablets. Ternarni kompleksi meloksikama (ME) (slabo vodotopljivi protuupalni lijek) s hidroksipropil-β-ciklodekstrinom (HPβCD) i/ili hidrofilnim polimerom polivinil pirolidonom (PVP) ili bazičnom aminokiselinom poput L-arginina, pripravljeni su metodom sušenja sprejom. Uspoređivan je utjecaj topljivosti, fizikalna svojstva i oslobađanje svakog ternarnog sustava ME-HPβCD s PVP ili L-argininom s odgovarajućim binarnim sustavom ME-HPβCD. Tablete priređene iz ternarnog sustava ME-HPβCD-L-arginin uspoređene su s jednostavnim i komercijalno dostupnim tabletama. Pokusi topljivosti ukazuju na to da se stvara inkluzijski kompleks AL tipa. Ternarni sustav ME-HPβCD-L-arginin imao je konstantu stabilnosti 30,3 puta veću nego binarni sustav ME-HPβCD, dok je ternarni sustav ME-HPβCD-PVP imao tu konstantu uvećanu za samo 2,2 puta. Pripravljeni kompleksi karakterizirani su pomoću pretražne elektronske mikroskopije, diferencijalne pretražne kalorimetrije i infracrvene spektroskopije. Ternarni čvrsti kompleksi ukazali su na prisutnost snažnih interakcija između komponenata. Oslobađanje ME iz različitih ternarnih kompleksa bilo je veće značajno iz binarnih sustava. Tablete komprimirane iz ternarnog kompleksa ME-HPβCD-L-arginin imaju vrlo poboljšano oslobađanje ljekovite tvari u usporedbi s jednostavnim i komercijalno dostupnim tabletama.