Fast-dissolving oral delivery systems are solid dosage forms which disintegrate or dissolve rapidly (< 1 min) when placed in the mouth, without drinking or chewing (tablets and films). As forming materials, maltodextrins (MDX) plasticized by glycerin were recently proposed to produce fast-dissolving films by solvent casting and hot-melt extrusion (Cilurzo F, Cupone IE, Minghetti P, Selmin F, Montanari L. (2008). Fast dissolving films made of maltodextrins. Eur. J Pharm Biopharm, 70(3), 895-900). In the development of orodispersible films, the main critical issues are represented by the tensile properties required for packaging and handling procedures, dissolution in the oral cavity, stability and taste. Generally speaking, organoleptic characteristics are important parameters which drive patients’ acceptance and compliance and, taste is one of the prime factors determining the market penetration and commercial success of oral pharmaceuticals. The development of more desirable and palatable formulations often represents a challenge for pharmaceutical companies, which are currently investing time and costs in the study of taste-masking techniques. The selection of a proper taste masking agent (TMA) is a critical issue in the development of fast-dissolving films containing bitter drugs since, compared to conventional liquid dosage forms, active ingredient is not diluted and the TMA amounts are limited with respect to orodispersible tablets due to the low weight of the film. This work aimed to evaluate the suppression of the bitter taste of a maltodextrin (MDX) fast dissolving film loaded with 13.4 mg sodium diclofenac (DS) by adding TMAs. Films were prepared by casting and drying aqueous mixtures of MDX (DE = 6), glycerin, sorbitan oleate and DS. Films were characterized in terms of thickness, tensile properties, film disintegration time and drug dissolution time. The bitterness intensity of DS and the masking effect of TMAs were evaluated by an electronic tongue (ET). The addition of mint flavour or liquorice flavour improved the taste of the DS-sucralose solutions and resulted appropriate to mask DS bitterness as confirmed by a panel of volunteers. By considering the sensory panel, sucralose-mint-liquorice solution appeared the most suitable combination to mask the DS taste. All films appeared homogeneous upon a visual inspection, flexible and not brittle. They were handled, cut and packed without occurring failure. The films weighted in the 95-110 mg range and the DS content complied the drug content assay according to the Ph. Eur. and was consistent with the theoretic drug loading, namely 13.4 mg. The addition of the selected TMAs did not significantly affect film disintegration time (15-20 s) and DS dissolution rate (about 5 min). The taste sensor system, i.e. electronic tongue, represents a useful tool to evaluate the feasibility to suppress the drug bitterness by TMAs during the development of fast-dissolving films. This system can allow discriminating the effect of the TMA also in presence of the other hydrosoluble constituents, namely polymers and surfactants. Since ET presents the advantages of simplicity and rapidity, this technique could assist, or even replace, the sensory evaluation in the development of new pharmaceutical formulations providing information about the taste without the need of humans to taste active compounds.
|Titolo:||Diclofenac fast dissolving film: suppression of bitterness by a taste-sensing system|
|Data di pubblicazione:||mag-2012|
|Settore Scientifico Disciplinare:||Settore CHIM/09 - Farmaceutico Tecnologico Applicativo|
|Enti collegati al convegno:||Associazione farmaceutici dell'industria|
|Citazione:||Diclofenac fast dissolving film: suppression of bitterness by a taste-sensing system / F. Cilurzo, P. Minghetti, S. Buratti, C.G.M. Gennari, L. Montanari. ((Intervento presentato al 52. convegno Simposio AFI tenutosi a Rimini nel 2012.|
|Appare nelle tipologie:||03 - Contributo in volume|