The bitterness masking effect of β-cyclodextrin in the formulation of ODTs using Granfiller D

CycloLab Cyclodextrin R&D Laboratory, Ltd., Hungary and Daicel Corporation have jointly published a white paper on the bitterness masking effect of β-cyclodextrin (β-CD) in the formulation of orally disintegrating tablets (ODTs) using GRANFILLER-D.

ODTs disintegrate in the oral cavity within 30 seconds without water so that patients with dysphagia can also swallow tablets easily. However, ODTs remain in the mouth while they are disintegrating, palatability is more important compared to when regular tablets taken with water. Therefore, taste masking is one of the most important issues in manufacturing ODTs. In this paper, we report the preparation of ODT including a β-CD-masked active pharmaceutical ingredient (API).

Introduction: Improving medication adherence is an important aspect of patient-centric pharmaceutical development. Patients and healthcare providers are looking for routes of administration or dosage forms that are easy to take. Orally disintegrating tablets (ODTs) are one of the most popular dosage forms for improving medication adherence. ODTs disintegrate in the oral cavity within 30 seconds without water so that patients with dysphagia can also swallow tablets easily.

To produce ODTs, rapid disintegration is required under sufficient tablet hardness. Additionally, as ODTs taken without water remain in the mouth while they are disintegrating, palatability is more important compared to when regular tablets taken with water. Active pharmaceutical ingredients (APIs)which have an unpleasant or bitter taste decrease medication adherence. Therefore, taste masking is one of the most important issues in manufacturing ODTs.

There are three types of bitterness masking methods: physical, organoleptic and chemical masking. While physical and organoleptic masking methods are the mainstream in marketed formulations, chemical masking has different advantages. It is the simplest method with fewer steps and at lower cost than the others. The main technique used in chemical masking is conducted with cyclodextrins (CDs) due to their complex-forming ability1).

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