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

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 (2013) 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 (Print), 2042-7158 (Online) (doi:10.1111/jphp.12169)

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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
Additional Information: [1] Published in Journal of Pharmacy and Pharmacology, Volume 66, Issue 2, February 2014. Special Issue: Engineering and solid state drugs. Guest Editors: Gavin P. Andrews and David S. Jones.
Uncontrolled Keywords: e-tongue, hot-melt extrusion, molecular dispersions, taste masking
Subjects: R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Related URLs:
Last Modified: 17 Oct 2016 09:12
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/12185

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