Preparation and evaluation of orally disintegrating tablets containing taste-masked microcapsules of berberine hydrochloride.

Xuelian Hu, Yingbo Li, Engjuan Zhang, Xianzhu Wang, Mao Xing, Qian Wang, Jian Lei, Hua Huang

AAPS PharmSciTech 2013 Mar

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The purpose of this study was to prepare and evaluate a taste-masked berberine hydrochloride orally disintegrating tablet for enhanced patient compliance. Taste masking was performed by coating berberine hydrochloride with Eudragit E100 using a fluidized bed. It was found that microcapsules with a drug-polymer ratio of 1:0.8 masked the bitter taste obviously. The microcapsules were formulated to orally disintegrating tablets and the optimized tablets containing 6% (w/w) crospovidone XL and 15% (w/w) microcrystalline cellulose showed the fastest disintegration, within 25.5 s, and had a pleasant taste. The dissolution profiles revealed that the taste-masked orally disintegrating tablets released the drug faster than commercial tablets in the first 10 min. However, their dissolution profiles were very similar after 10 min. The prepared taste-masked tablets remained stable after 6 months of storage. The pharmacokinetics of the taste-masked and commercial tablets was evaluated in rabbits. The Cmax, Tmax, and AUC0-24 values were not significantly different from each other, suggesting that the taste-masked orally disintegrating tablets are bioequivalent to commercial tablets in rabbits. These tablets will enhance patient compliance by masking taste and improve patients' quality of life.

Citation

Xuelian Hu, Yingbo Li, Engjuan Zhang, Xianzhu Wang, Mao Xing, Qian Wang, Jian Lei, Hua Huang. Preparation and evaluation of orally disintegrating tablets containing taste-masked microcapsules of berberine hydrochloride. AAPS PharmSciTech. 2013 Mar;14(1):29-37