The aim of the study was to assess the possibility of using hydroxypropylomethylocellulose acetate succinate (AQOAT®) as a carrier for antifungal drugs, hardly or practically insoluble in the water. Itraconazole and terbinafine hydrochloride were used in the study as model drugs. In the studies the properties of 22 binary and ternary solid dispersions with itraconazole, 5 binary solid dispersions with terbinafine and 26 nail varnishes, were assessed. The solid dispersions were prepared by the spray drying of itraconazole with AQOAT® AS-LF, ASHF as carriers and with addition of Gelucire® 44/14, 50/13, PVP or PEG 6000. For preparation of binary solid dispersions and nail varnishes with terbinafine, AQOAT® AS-LF and AS-HF were used as excipients. In case of nail varnishes plasticizers were also used. All solid dispersions with AQOAT® contained drugs in the amorphous state. In case of itraconazole binary solid dispersions the best results were obtained for formulation with AQOAT® AS-HF (1:4). The solubility of itraconazole was 44-fold greater than the solubility of drug alone. During the dissolution studies quantity of the drug dissolved after 2 h was 14-fold larger than for pure drug. The further improvement of the itraconazole dissolution was achieved by preparation of ternary solid dispersions with Gelucire® or PVP. In case of solid dispersions with terbinafine the amounts of dissolved and permeated drug were decreased. Application of terbinafine hydrochloride in form of the nail polish to membrane or nail plate was effective and inhibited the growth of Trichophyton mentagrophytes (ATTC 18784) colony during 14 days of incubation.
farmacja ; dermatologia ; mikrobiologia
Biblioteka Medyczna Uniwersytetu Jagiellońskiego - Collegium Medicum
Nov 19, 2019
Nov 21, 2012
|ZB-110912||Nov 19, 2019|