Effect of drug-ion exchange resin complex in betahistine hydrochloride orodispersible film on sustained release, taste masking and hygroscopicity reduction

Abstract

Orodispersible film (ODF) is a widely used oral solid dosage form. However, it's not suitable for drugs with short half-life, bitterness and strong hygroscopicity. The present study aims to develop a sustained release and stable betahistine hydrochloride ODF without bitterness. Drug-resin complex (IRDC) was prepared using batch method. In vitro dissolution experiment, e-Tongue and hygroscopicity experiment were conducted to compare the differences between ODF containing IRDC and ODF containing betahistine hydrochloride. Drug release kinetics showed that the diffusion of drug in IRDC was the rate-limiting step of drug release. DSC and FT-IR were conducted to explore the molecular mechanism of taste masking and hygroscopicity reduction. It turned out that taste masking was attributed to the ionic interaction between drug and resin and the slow dissolution of drug from IRDC. The site where drug form hydrogen bonds with water molecular was occupied by drug-resin interaction leading to hygroscopicity reduction. In summary, in this study we not only developed a betahistine hydrochloride ODF with good properties but also explored the effect of drug-resin interaction on sustained release, taste masking and hygroscopicity reduction.

Keywords: Betahistine hydrochloride; Ion exchange resin; Orodispersible film; Sustained release; Taste masking.