title: The In vitro/vivo Evaluation of Prepared Gastric Floating Tablets of Berberine Hydrochloride.
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.
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
authors.forename: Jun
authors.initials: J
authors.lastname: Ji
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210000, China.
authors.forename: Xin
authors.initials: X
authors.lastname: He
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210000, China.
authors.forename: Xiao-Lin
authors.initials: XL
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
authors.forename: Wen-Juan
authors.initials: WJ
authors.lastname: Du
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
authors.forename: Cheng-Long
authors.initials: CL
authors.lastname: Cui
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
authors.forename: Ling
authors.initials: L
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
authors.forename: Xue
authors.initials: X
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China. zhangchunfeng67@163.com.
authors.forename: Chun-Feng
authors.initials: CF
authors.lastname: Zhang
authors.affiliation: State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China. guochangrun@126.com.
authors.forename: Chang-Run
authors.initials: CR
authors.lastname: Guo
mesh_terms: D000180:Acrylic Resins / Q000494:pharmacology*; D000284:Administration, Oral; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D001599:Berberine / Q000008:administration & dosage / Q000493:pharmacokinetics; D001682:Biological Availability; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000493:pharmacokinetics; D004304:Dosage Forms; D004337:Drug Carriers / Q000494:pharmacology; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000494:pharmacology; D006801:Humans; D011480:Protease Inhibitors / Q000494:pharmacology; D013270:Stomach / Q000187:drug effects; D013607:Tablets
chemical_list: D000180:Acrylic Resins; D000897:Anti-Ulcer Agents; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D005079:Excipients; D011480:Protease Inhibitors; D013607:Tablets; C006912:carboxypolymethylene; D001599:Berberine
keywords: berberine hydrochloride; floating; gastrointestinal disease; gastroretensive drug delivery system; non-Fickian diffusion