Comparative in vitro and in vivo taste assessment of liquid praziquantel formulations

Abstract

The taste of pharmaceuticals strongly affects the compliance of patients. This study investigated the applicability of the electronic tongue and rodent brief-access taste aversion (BATA) model for the bitter compound praziquantel (PZQ) and taste masked liquid formulations for PZQ. In a comparative study maltodextrin (MD) Kleptose linecaps 17 was selected as an alternative taste masking agent to two cyclodextrins; hydroxypropyl-beta-cyclodextrin (HP-β-CD) and sulfobutyl ether-beta-cyclodextrin (SBE-β-CD). A phase solubility study showed the highest affinity and solubilization capabilities for SBE-β-CD over HP-β-CD and MD, suggesting the highest taste masking ability for SBE-β-CD. No reliable results were achieved for PZQ with the Insent electronic tongue. Thus this system was not used for further evaluation of solutions with MD and CDs to confirm the results of the solubility study. In contrast the BATA model demonstrated conclusive responses for the aversiveness of PZQ. The concentration of PZQ inhibiting 50% of water lick numbers (called IC value) was 0.06mg/ml. In contrast to the phase solubility study, the MD enabled an equal taste masking effect in vivo in comparison to both CDs. Moreover HP-β-CD showed superior taste masking capabilities for PZQ compared to SBE-β-CD as the SBE-β-CD itself was less acceptable for the rodents than HP-β-CD. In conclusion, the BATA model was identified as a more efficient taste assessment tool for the pure PZQ and liquid formulations in contrast to the electronic tongue and the phase solubility study.

Evaluation of the taste-masking effects of (2-hydroxypropyl)-β-cyclodextrin on ranitidine hydrochloride; a combined biosensor, spectroscopic and molecular modelling assessment

“…In particular, a previous investigation has compared the ability of the e tongue approach with an animal model to assess cyclodextrin as a means of taste masking praziquantel. 20 The rationale for using an electronic taste sensing system to determine taste-masking effects is that it enables one to measure the activity of molecules within a formulation based on its non-specic multi-sensor approach. In addition, the sensors are able to interact with different chemical structures, which allows one to assume an overall impression rather than to determine the concentration of the drug substance.…”

Multi-Methodological Quantitative Taste Assessment of Anti-Tuberculosis Drugs to Support the Development of Palatable Paediatric Dosage Forms

“…The BATA model is showing great promise as a tool to assess the aversiveness of APIs and is gaining interest within the pharmaceutical industry [49]. It is possible that, in the future, its use could be expanded to assess the taste of formulations [50,51], in which case the BATA data obtained in this study would be extremely useful to facilitate the formulation development of these drugs.…”

Taste Masking of Nizatidine Using Ion-Exchange Resins

“…As explained in previous studies, the electronic tongue system detects the difference in taste by using potentiometric sensors, voltammetric sensors, impedimetric sensors, etc. [29,30]. This implies that the charged objects are more easily detected than the non-charged object.…”