Bitter taste? Masked!

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Although there are several commercial examples for the uses of cyclodextrins as taste-masking agents (Nicorette, Ulgut, Zyrtec, etc), their use is not that well-spread. This has little to do with their performance, since their taste-masking capabilities are outperforming other alternatives in most cases. It’s rather the mass balance, as frequently to efficiently mask the taste, you need CD in a molar ratio comparable to the active which makes a solid oral formulation simply too big. For liquids, this is not that big of a problem.

Nevertheless, cyclodextrins are definitely excipients to consider for this purpose and their advantages are not to be neglected. A patent application from CTC BIO has recently become public disclosing an invention related to a pharmaceutical preparation for oral administration, comprising an inclusion complex formed by varenicline (Champix/Chantix – Pfizer, quite popular in this area) or a pharmaceutically acceptable salt thereof in cyclodextrin. This formulation is claimed to improve the convenience of administration by effectively blocking the bitter taste of the drug and the irritation in swallowing it. Also, the cyclodextrin is expected to have a stabilizing effect in view of oxidation of varenicline, and can improve the solubility of a drug. So pretty much everything a cyclodextrin can do.

So would you consider using CDs for taste masking or not?

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