Validation of a rat behavioral avoidance model from a drug delivery perspective

Conventional taste-masking strategies are used to overcome the bitter taste perception of pharmaceuticals by coating the drug particles and/or adding flavoring agents. However, for certain product categories such as rapid dissolve sublingual tablets, taste-masking is challenging. Programs exploring...

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Bibliographic Details
Published in:International journal of pharmaceutics 2005-10, Vol.303 (1), p.31-36
Main Authors: Bhat, Meenakshi G., Jordt, Raymond M., Khan, M. Amin, Foley, Christine E., Gilbertson, Timothy A.
Format: Article
Language:English
Subjects:
Animals
Avoidance Learning - drug effects
Behavior, Animal - drug effects
Biological and medical sciences
Bitter taste
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical - methods
Ergotamine
Ergotamine - pharmacology
Fluoxetine
Fluoxetine - pharmacology
General pharmacology
Inhibitory Concentration 50
Male
Medical sciences
Migraine therapy
Models, Animal
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rat model
Rats
Reproducibility of Results
Sumatriptan
Sumatriptan - pharmacology
Taste Threshold - drug effects
Water Deprivation
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Summary:Conventional taste-masking strategies are used to overcome the bitter taste perception of pharmaceuticals by coating the drug particles and/or adding flavoring agents. However, for certain product categories such as rapid dissolve sublingual tablets, taste-masking is challenging. Programs exploring such formulation strategies in the LO–CS phase or post CS phase possess very little toxicological information available in order to conduct human taste panel studies. The potential of a bitter taste perception can present a significant business risk. The objective of the study was to validate a rat behavioral avoidance model that identifies bitter-tasting compounds. Most classic bitter substances elicit a response in the micromolar concentration range while most drugs elicit a response in the millimolar range, hence a validation exercise was conducted to examine if the existing biological model was sensitive enough to identify known bitter tasting drugs as such. Five compounds: ergotamine tartrate, fluoxetine, sucrose, sumatriptan and povidone were chosen to represent a spectrum of compounds. The bitter tasting compounds were identified as such in the model. Based on these results, the assay may serve as a useful surrogate test to identify compounds that may have bitter taste issues.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2005.06.015