An in-vivo and in-vitro taste masking evaluation of bitter melt-extruded drugs

Maniruzzaman, Mohammed, Bonnefille, Marion, Aranyos, Attila, Snowden, Martin J and Douroumis, Dennis (2014) An in-vivo and in-vitro taste masking evaluation of bitter melt-extruded drugs. Journal of Pharmacy and Pharmacology, 66 (2). pp. 323-337. ISSN 0022-3573

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Abstract

Objectives
The purpose of this study was to investigate the potential of hot-melt extrusion (HME) for masking the taste of bitter active pharmaceutical ingredients (APIs) when incorporated into different polymer formulations.

Methods
Extrudates were produced by HME using two water soluble cationic model drugs (cetirizine HCl and verapamil HCl) processed with various grades of anionic polymers (Eudragit L100 and Eudragit L100-55 (Acryl EZE)). The process was optimised by using a single screw extruder to produce extruadates with the desirable characteristics.

Key findings
In-vivo results obtained from a panel of six healthy human volunteers demonstrated that the HME extruded formulations improved the taste significantly compared with that of the pure APIs. In addition, an in-vitro evaluation carried out by an Astree e-tongue equipped with seven specific sensors demonstrated significant taste improvement of the extrudates compared with placebo polymers and the pure APIs. Furthermore, the extrudates characterised by SEM, X-ray and differential scanning calorimetry studies showed the existence of molecularly dispersed APIs while in-vitro dissolution showed fast release for all drug substances.

Conclusions
HME can effectively be used to mask the taste of bitter APIs by enhancing drug–polymer interactions.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Depositing User: Mohammed Maniruzzaman
Date Deposited: 29 Jan 2016 11:09
Last Modified: 29 Jan 2016 11:09
URI: http://sro.sussex.ac.uk/id/eprint/59482
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