RESUMEN
This study was aimed at preparing and evaluating oral disintegrating tablets (ODTs) using a strongly cationic resin, Amberlite(®) IRP-69, to mask the bitter taste of a delivered drug, i..e. dextromethorphan hydrobromide. The drug was loaded into the resin (referred to as resinate) or physically mixed with the resin (referred to as physical mixture), and was then incorporated into ODTs by direct compression. A variety of formulae was developed to acquire the optimal formulations of taste-masked ODTs that had acceptable hardness and mouth feel (grittiness). The optimized ODTs were further evaluated for thickness, diameter, weight, friability, disintegration time, wetting time, wetting rate, drug content, drug release and degree of bitter taste, respectively. The thickness, diameter, weight and friability of the tablet with resinate were slightly higher than those with physical mixture. The tablet with resinate had a longer disintegration time, corresponding with its slower wetting time and rate. Both tablets with resinate and physical mixture provided a sustained pattern of drug release. However, only tablets with resinate successfully masked the bitter taste of the drug. In conclusion, the combination of drug and ion exchange resin as resinate could increase the palatability and acceptability of ODTs containing bitter drugs.
Asunto(s)
Antitusígenos/administración & dosificación , Dextrometorfano/administración & dosificación , Resinas Sintéticas/química , Gusto , Administración Oral , Antitusígenos/química , Dextrometorfano/química , Dureza , Humanos , ComprimidosRESUMEN
This study focused on investigating and comparing between the effect of the strongly cationic exchange resin, Dowex 88 (Dow88), and the weakly cationic exchange resin, Amberlite IRP64 (Am64), on the physical properties of matrices and their drug release profiles. The matrices were prepared by direct compression of Methocel K4M (HPMC) or Ethocel 7FP (EC) polymeric matrix formers and contained diphenhydramine hydrochloride as a model drug. The addition of Dow88 to the matrices decreased matrix hardness and increased thickness, diameter, and friability. In contrast, the addition of Am64 increased matrix hardness and maintained the original thickness, diameter, and friability. In deionized water, both resins lowered drug release from HPMC-based matrices by virtue of the gelation property of matrix former and the drug exchange property of embedded resin, in other words in situ resinate formation. Dow88 strongly dissociated and lowered the drug release to a greater extent than Am64, which was weakly dissociated. However, Am64 could retard drug release under simulated gastrointestinal conditions. EC-based matrices containing either resin displayed a propensity for disintegration caused by swelling and wicking (water adsorption) actions by the resin. The results of this study provided useful information on the utilization of ion exchange resins as release modifiers in matrix systems.