Citric Acid Suppresses the Bitter Taste of Olopatadine Hydrochloride Orally Disintegrating Tablets

Abstract

Orally disintegrating tablets (ODTs) are formulated to disintegrate upon contact with saliva, allowing administration without water. Olopatadine hydrochloride, a second-generation antihistamine, is widely used for treating allergic rhinitis. However, it has a bitter taste; therefore, the development of taste-masked olopatadine ODTs is essential. Some studies have suggested that citric acid could suppress the bitterness of drugs. However, these experiments were performed using solutions, and the taste-masking effect of citric acid on ODTs has not been evaluated using human gustatory sensation tests. Thus, this study evaluated citric acid's taste-masking effect on olopatadine ODTs. Six types of olopatadine ODTs containing 0-10% citric acid were prepared and subjected to gustatory sensation tests that were scored using the visual analog scale. The bitterness and overall palatability of olopatadine ODTs during disintegration in the mouth and after spitting out were evaluated in 11 healthy volunteers (age: 22.8 2.2 years). The hardness of the ODTs was >50 N. Disintegration time and dissolution did not differ among the different ODTs. The results of the gustatory sensation tests suggest that citric acid could suppress the bitterness of olopatadine ODTs in a dose-dependent manner. Olopatadine ODTs with a high content of citric acid (5-10%) showed poorer overall palatability than that of those without citric acid despite the bitterness suppression. ODTs containing 2.5% citric acid, yogurt flavoring, and aspartame were the most suitable formulations since they showed low bitterness and good overall palatability. Thus, citric acid is an effective bitterness-masking option for ODTs.

Structural and Thermal Analysis of Cannabidiol Orodispersible Formulations

“…Fourier transform-infrared (FTIR) spectroscopy FTIR results of the raw materials and the CBD-ODFs can be found in Figures 2 and 3 and Table III. The substances analysed were: CBD-a cannabinoid, Hypromellose-Vivapharm HPMC E3 , CA-used as a taste-masking agent [20], saliva stimulating agent [4] while other studies showed that it could be used as a plasticizer [18], SRB-a non-cariogenic sweetener [26], PFL-taste masking agent and flavouring agent. The other two spectra belonged to the ODFs.…”

Ease of Taking and Palatability of Fixed-Dose Orally Disintegrating Mitiglinide/Voglibose Tablets

“…It has been reported that the addition of flavor improves the sweetness of famotidine ODT and amlodipine ODT. 19,22) Generally, taste masking is adjusted to a certain target drug during ODT development. When two different ODTs are taken simultaneously, the respective flavoring agents might not be appropriate for drugs other than the target drug, which may greatly worsen palatability.…”

“…Subsequently, the bitterness, sweetness and overall palatability of the ODTs were evaluated using a VAS (first evaluation). [19][20][21][22][23] Bitterness VAS scores of 0 and 100 indicate "none" and "very bitter," sweetness scores of 0 and 100 indicate "none" and "very sweet," and overall palatability VAS scores of 0 and 100 indicate "bad" and "good," respectively. In parallel with the VAS evaluation, the clinical disintegration time was measured using a stopwatch.…”

Effects of MP-AzeFlu enhanced by activation of bitter taste receptor TAS2R

“…The result precludes a general anti histamine effect, instead strengthening the bitter taste theory. Olopatadine [9] and desloratadine [10], both known for their bitter taste, relaxed airway segments in a way that resembled the effects of MP-AzeFlu and azelastine ( Fig. 1c, d).…”