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

• Published in: AAPS PharmSciTech 2017-08, Vol.18 (6), p.2149-2156
• Main Authors: Ji, Jun, He, Xin, Yang, Xiao-Lin, Du, Wen-Juan, Cui, Cheng-Long, Wang, Ling, Wang, Xue, Zhang, Chun-Feng, Guo, Chang-Run
• Format: Article
• Language: English
• Subjects: Acrylic Resins - pharmacology; Administration, Oral; Anti-Ulcer Agents - administration & dosage; Anti-Ulcer Agents - pharmacokinetics; Berberine - administration & dosage; Berberine - pharmacokinetics; Biochemistry; Biological Availability; Biomedical and Life Sciences; Biomedicine; Biotechnology; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - pharmacokinetics; Dosage Forms; Drug Carriers - pharmacology; Drug Compounding; Drug Delivery Systems - methods; Excipients - pharmacology; Humans; Pharmacology/Toxicology; Pharmacy; Protease Inhibitors - pharmacology; Research Article; Stomach - drug effects; Tablets
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-016-0696-7

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.