Ji Jun, He Xin, Yang Xiao-Lin, Du Wen-Juan, Cui Cheng-Long, Wang Ling, Wang Xue, Zhang Chun-Feng, Guo Chang-Run
State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjia Lane, Nanjing, Jiangsu, 210009, China.
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210000, China.
AAPS PharmSciTech. 2017 Aug;18(6):2149-2156. doi: 10.1208/s12249-016-0696-7. Epub 2016 Dec 29.
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.
目前可用的抗溃疡药物存在严重的副作用，这限制了它们的使用，并促使人们需要一种安全有效的新型抗溃疡药物。本项目工作的目的是使药物在胃中保留，以获得更好的抗溃疡活性并减少副作用。因此，我们当前工作的目标是制备具有合适体外/体内性质的盐酸小檗碱（Ber）胃漂浮片。在本研究中，通过简单直接压片法，使用不同量的羟丙甲纤维素K15M和卡波姆971PNF并结合其他片剂辅料，制备了不同的Ber胃漂浮片。对片剂的性质进行了评估，包括硬度、漂浮性、溶胀能力、体外药物释放和体内药代动力学研究。所得结果表明，Ber片的硬度、漂浮性、溶胀性和体外药物释放主要取决于聚合物组合的比例。此外，在六种制剂中，F3表现出理想的漂浮性、溶胀性和延长的药物释放。另外，体内药代动力学研究表明，与市售片剂相比，制备的胃漂浮片具有显著的缓释效果。因此，所开发的Ber胃漂浮片可能是治疗胃肠道疾病的一种替代剂型。
