title: 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.
authors.affiliation: Department of Pharmacy Practice and Science, School of Pharmaceutical Sciences University of Shizuoka.
authors.forename: Mai
authors.initials: M
authors.lastname: Sotoyama
authors.forename: Shinya
authors.initials: S
authors.lastname: Uchida
authors.forename: Shimako
authors.initials: S
authors.lastname: Tanaka
authors.forename: Akio
authors.initials: A
authors.lastname: Hakamata
authors.forename: Keiichi
authors.initials: K
authors.lastname: Odagiri
authors.forename: Naoki
authors.initials: N
authors.lastname: Inui
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Watanabe
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Namiki
mesh_terms: D000284:Administration, Oral; D019343:Citric Acid / Q000008:administration & dosage*; D004339:Drug Compounding; D005260:Female; D005421:Flavoring Agents / Q000008:administration & dosage*; D039563:Histamine H1 Antagonists, Non-Sedating / Q000008:administration & dosage* / Q000378:metabolism; D006801:Humans; D008297:Male; D000069605:Olopatadine Hydrochloride / Q000008:administration & dosage* / Q000378:metabolism; D012995:Solubility; D013649:Taste / Q000187:drug effects* / Q000502:physiology; D055815:Young Adult
chemical_list: D005421:Flavoring Agents; D039563:Histamine H1 Antagonists, Non-Sedating; D019343:Citric Acid; D000069605:Olopatadine Hydrochloride