Abstract

A variety of pharmacologically active substances, including chemotherapeutic drugs and the substances from traditional Chinese medicine (TCM), always exhibit potent bioactivities after oral administration. However, their unpleasant taste (such as bitterness) and/or odor always decrease patient compliance and thus compromise their curative efficacies in clinical application. Therefore, the developments of taste-masking techniques are of great significance in improving their organoleptic properties. However, though a variety of taste-masking techniques have been successfully used to mask the unpalatable taste of chemotherapeutic drugs, their suitability for TCM substances is relatively limited. This is mainly due to the fact that the bitter ingredients existing in multicomponent TCM systems (i.e., effective fractions, single Chinese herbs, and compound preparations) are always unclear, and thus, there is lack of tailor-made taste-masking techniques to be utilized to conceal their unpleasant taste. The relevant studies are also relatively limited. As a whole, three types of taste-masking techniques are generally applied to TCM, including (i) functional masking via sweeteners, bitter blockers, and taste modifiers; (ii) physical masking via polymer film-coating or lipid barrier systems; and (iii) biochemical masking via intermolecular interaction, β-cyclodextrin inclusion, or ion-exchange resins. This review fully summarizes the results reported in this field with the purpose of providing an informative reference for relevant readers.

Highlights

  • A variety of pharmacologically active substances orally administrated are proved to be quite effective in treating diseases

  • Biochemical masking is mainly used for bioactive traditional Chinese medicine (TCM)-derived ingredients, while the others are suitable for both single TCM ingredients and multicomponent TCM systems

  • It has been clearly proven that adding sweeteners, bitter blockers, and/or taste modifiers into TCM formulations could significantly weaken their bitterness sensation

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Summary

Introduction

A variety of pharmacologically active substances orally administrated are proved to be quite effective in treating diseases. The higher taste-masking efficiency could be achieved by the combination of sweeteners and flavors (for example, the mixture of sodium saccharin and some flavors was used to conceal the bitterness of ibuprofen formulated as syrup with pyridoxine HCl) [1]. Three types of taste-masking techniques were applied to TCM, including: (i) functional masking via sweeteners, bitter blockers, and taste modifiers; (ii) physical masking via polymer film-coating and lipid barrier systems; and (iii) biochemical masking via intermolecular interaction, cyclodextrin inclusion, and ion-exchange resins (Figure 1) [16,17].

Bitter Blockers
Taste Modifiers
Others
Physical Masking
Preparation Method
Polymer Film-Coating
Acrylate Copolymers
Biopolymers
Lipid Barrier Systems
Biochemical Masking
Intermolecular Interaction
Cyclodextrin Inclusion
Complexation with Ion-Exchange Resins
Findings
Conclusions
Full Text
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