Development of oral acetaminophen chewable tablets with inhibited bitter taste.
Various formulations with some matrix bases and corrigents were examined for development of oral chewable tablets which suppressed the bitter taste of acetaminophen, often used as an antipyretic for infants. Corn starch/lactose, cacao butter and hard fat (Witepsol H-15) were used for matrix bases, and sucrose, cocoa powder and commercial bitter-masking powder mixture made from lecithin (Benecoat BMI-40) were used for corrigents against bitter taste. The bitter taste intensity was evaluated using volunteers by comparison of test samples with standard solutions containing quinine at various concentrations. For the tablets made of matrix base and drug, Witepsol H-15 best inhibited the bitter taste of the drug, and the bitter strength tended to be suppressed with increase in the Witepsol H-15 amount. When the inhibitory effect on the bitter taste of acetaminophen solution was compared among the corrigents, each tended to suppress the bitter taste; especially, Benecoat BMI-40 exhibited a more inhibitory effect. Further, chewable tablets were made of one matrix base and one corrigent, and of one matrix base and two kinds of corrigents, their bitter taste intensities after chewing were compared. As a result, the tablets made of Witepsol H-15/Benecoat BMI-40/sucrose, of Witepsol H-15/cocoa powder/sucrose and of Witepsol H-15/sucrose best masked the bitter taste so that they were tolerable enough to chew and swallow. The dosage forms best masking bitter taste showed good release of the drug, indicating little change in bioavailability by masking.
Suzuki
Hiroyuki
H
Department of Drug Delivery Research, Hoshi University, 2-4-41, Ebara, Shinagawa-ku, Tokyo 142-8501, Japan.
Onishi
Hiraku
H
Takahashi
Yuri
Y
Iwata
Masanori
M
Machida
Yoshiharu
Y
D000082:Acetaminophen / Q000008:administration & dosage* / Q000737:chemistry*; D000284:Administration, Oral; D006801:Humans; D008409:Mastication; D009055:Mouth / Q000187:drug effects / Q000378:metabolism; D013607:Tablets; D013649:Taste / Q000187:drug effects* / Q000502:physiology; D013678:Technology, Pharmaceutical / Q000379:methods*
D013607:Tablets; D000082:Acetaminophen