Physical Approaches to Masking Bitter Taste: Lessons from Food and Pharmaceuticals

Coupland, John N.; Hayes, John E.

doi:10.1007/s11095-014-1480-6

Cited by 101 publications

(65 citation statements)

References 143 publications

(156 reference statements)

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“…Differences in binding are useful for this study in order to provide a point of contrast between results. It is generally understood that in order for something to reach the taste receptor and be perceived, it must first dissolve in saliva (Matsuo ; Coupland and Hayes ). We hypothesized that by preventing the bitterant from accessing the saliva in the mouth, binding by WPI would cause a reduction of bitterness.…”

Section: Resultsmentioning

confidence: 99%

“…Because these pharmaceuticals or phytochemicals are essential to the function of the medication or food product, their removal is not possible and suppression of the bitter taste should therefore be a focus. One strategy to reduce bitterness is the prevention of interactions between bitterants and taste receptors via physical means, such as encapsulation or molecular binding (Coupland and Hayes ). Proteins can be useful in bitterness‐masking in foods because they have the ability to bind small molecules and have demonstrated capacity to alter taste and aroma perception (Bohin and others ).…”

Section: Introductionmentioning

confidence: 99%

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Binding of Caffeine and Quinine by Whey Protein and the Effect on Bitterness

Tenney

Hayes

Euston

et al. 2017

Journal of Food Science

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Many drugs and phytochemicals are bitter, leading to noncompliance with prescriptions and avoidance of healthy foods and a need to suppress their taste. The goal of this study was to investigate the binding of bitterants (quinine and caffeine) by whey protein isolate (WPI) and the effect on perceived bitterness. Caffeine interacted minimally with WPI, while the proportion of unbound quinine decreased exponentially with protein concentration. Molecular modeling was used to show the energy of the quinine-Β-lactoglubulin interaction was an order of magnitude greater than the caffeine-Β-lactoglobulin interaction. Untrained assessors were used to assess the bitterness of caffeine (1.8, 5.7, and 18 mM) and quinine (0.056, 0.10, and 0.18 mM) solutions with 0% or 1% WPI. There was no significant effect of protein on the bitterness of caffeine solutions, but WPI decreased the bitterness of quinine relative to the same concentration in water. This is generally consistent with our hypothesis that higher binding results in lower bitterness; however the magnitude of reduction was not large and the bitterness of the protein-quinine solutions was greater than would be expected for the unbound quinine present.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Binding of Caffeine and Quinine by Whey Protein and the Effect on Bitterness

Tenney

Hayes

Euston

et al. 2017

Journal of Food Science

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“…Prednisone and prednisolone, corticosteroid anti‐inflammatory agents approved for a variety of treatment indications in both children and adults, are both known to be inherently bitter. A variety of physical approaches have been used in an attempt to mask the taste of bitter‐tasting drugs administered as both oral solid and liquid dosage forms . In an attempt to overcome the limitations with current prednisone formulations (e.g.…”

Section: Discussionmentioning

confidence: 99%

Palatability of a novel oral formulation of prednisone in healthy young adults

Bai

Dormer

Shoults

et al. 2017

Journal of Pharmacy and Pharmacology

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Objectives Prednisone is a widely used anti-inflammatory for a variety of conditions. While oral liquid formulations of prednisone enable weight-based dosing, children frequently find them to be objectionable due to bitter taste. This limitation of prednisone can adversely impact patient acceptance and may result in non-compliance. Efforts to mask flavors often result in poorly controlled, heterogeneous particle distributions and can provide ineffective taste masking. The present work utilized a novel drug delivery technology developed by Orbis Biosciences, Inc., to create an oral taste-masked formulation of prednisone. Methods The study examined the palatability of Orbis’ microsphere prednisone formulation in healthy young adults (n=24). Four test articles were used in the study including a reference formulation (Roxane Laboratories), a control, and the test formulation (Orbis) prepared in two different ways. Study participants were randomized in a crossover design. Key Findings Results indicated that the test prednisone formulation was indistinguishable from the control, and both were preferable to the reference formulation in every category of palatability assessed using a validated 9-point Hedonic Scale. The data also suggested that preparing the microsphere suspension immediately prior to administration results in the most ideal palatability properties. Conclusions In conclusion, the novel microsphere formulation technology was effective in taste-masking prednisone.

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“…Paracetamol has a bitter taste and this taste is difficult to be masked in the liquid formulations like syrup and suspension. Encapsulation technologies are among several techniques to mask the bitter taste of drugs [14]. This study was conducted to encapsulate paracetamol in alginate beads so that I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s later the beads can be used for taste masking.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of the Immediate Release of Paracetamol From Alginate Beads

Hamed

Ayob

Alfatama³

et al. 2017

Int J App Pharm

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Objective: Alginate beads are not soluble in the acid leading to small portion released in the stomach. This may not be favourable for drugs administered for fast action like paracetamol. So, this study was aimed to increase the immediate release of paracetamol from alginate beads, i.e. the release in the acidic pH. Methods:The beads were prepared by dropwise paracetamol/alginate suspension in divalent cation solution. Two attempts were used to increase the dissolution of paracetamol in the acidic pH. First attempt was by only changing preparation variables: needle size, alginate viscosity and drug loading using 2 3 full factorial design. The second approach was by adding excipients like carbopol, tween and polyethylene glycol. The beads were characterized for their size, encapsulation efficiency and release profile.Results: First approach, changing preparation variables without excipient adding, helped to increase the drug release in the acid but to a maximum of 26% using a smaller needle, lower drug loading and higher alginate viscosity. However, optimising the formulation with suitable excipients increased the drug release in the acid to 77.3%. The optimised formulation included carbopol 940 (pH sensitive polymer) and tween 80 (facilitates water entry) in the beads, with using barium chloride instead of calcium chloride together with PEG 400 in the complexing solution.Conclusion: To achieve immediate release of paracetamol from alginate beads in the acidic pH, excipients need to be added. Rational selection of excipients is critical to achieve the desired drug release.

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Physical Approaches to Masking Bitter Taste: Lessons from Food and Pharmaceuticals

Cited by 101 publications

References 143 publications

Binding of Caffeine and Quinine by Whey Protein and the Effect on Bitterness

Binding of Caffeine and Quinine by Whey Protein and the Effect on Bitterness

Palatability of a novel oral formulation of prednisone in healthy young adults

Enhancement of the Immediate Release of Paracetamol From Alginate Beads

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