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The In vitro/vivo Evaluation of Prepared Gastric Floating Tablets of Berberine Hydrochloride

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Abstract

Currently available antiulcer drugs suffered from serious side effects which limited their uses and prompted the need for a safe and efficient new antiulcer agent. The objective of this project work was to retain the drug in the stomach for better antiulcer activity and less side effects. Hence, the aim of our present work was to prepare a gastric floating tablet of Berberine hydrochloride (Ber) with suitable in vitro/vivo properties. In this study, different Ber gastric floating tablets were prepared by simple direct compression using various amounts of HPMCK15M and Carbopol 971PNF combined with other tablet excipients. The properties of the tablets including hardness, buoyancy, swelling ability, in vitro drug release, and in vivo pharmacokinetic study were evaluated. The obtained results disclosed that hardness, floating, swelling, and in vitro drug release of the Ber tablets depended mainly on the ratio of polymer combinations. Moreover, among six formulations, F3 exhibited desirable floating, swelling, and extended drug release. In addition, in vivo pharmacokinetic study suggested that prepared gastric floating tablets had significantly sustained-releasing effects compared with market tablets. Therefore, the developed gastric floating tablets of Ber could be an alternative dosage form for treatment of gastrointestinal disease.

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Acknowledgments

This research was supported in part by a grant (BK 20131309) from The Natural Science Foundation of Jiangsu Province (CHN) and a grant (81573565) from The Natural Science Foundation of China (NSFC).

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    Authors and Affiliations

    1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China

      Jun Ji, Wen-Juan Du, Cheng-Long Cui, Ling Wang, Xue Wang, Chun-Feng Zhang & Chang-Run Guo

    2. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210000, China

      Xin He & Xiao-Lin Yang

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    1. Jun Ji
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    2. Xin He
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    Correspondence to Chun-Feng Zhang or Chang-Run Guo.

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    All the animal experiments were approved and supervised conducted by the China Pharmaceutical University Ethics Committee of Care and Use of laboratory animals. All the animals were house and handled according to the University Unit for Laboratory Animal Medicine guidelines.

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    The authors declare that they have no conflicts of interest.

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    Jun Ji and Xin He contributed equally to this work.

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    Ji, J., He, X., Yang, XL. et al. The In vitro/vivo Evaluation of Prepared Gastric Floating Tablets of Berberine Hydrochloride. AAPS PharmSciTech 18, 2149–2156 (2017). https://doi.org/10.1208/s12249-016-0696-7

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    • DOI: https://doi.org/10.1208/s12249-016-0696-7

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