Jiangsu Province Academy of Traditional Chinese Medicine, No. 100 shizhijie, Nanjing 210028, China.
Molecules. 2011 Dec 14;16(12):10347-56. doi: 10.3390/molecules161210347.
The purpose of this research was to prepare floating calcium alginate beads of berberine for targeting the gastric mucosa and prolonging their gastric residence time. The floating beads were prepared by suspending octodecanol and berberine in sodium alginate (SA) solution. The suspension was then dripped into a solution of calcium chloride. The hydrophobic and low-density octodecanol enhanced the sustained-release properties and floating ability of the beads. The bead formulation was optimized for different weight ratios of octodecanol and SA and evaluated in terms of diameter, floating ability and drug loading, entrapment and release. In vitro release studies showed that the floating and sustained release time were effectively increased in gastric media by addition of octodecanol. In vivo studies with rats showed that a significant increase in gastric residence time of beads had been achieved.
本研究旨在制备靶向胃黏膜并延长其胃滞留时间的漂浮型海藻酸钠包载小檗碱微丸。通过将十八醇和小檗碱混悬于海藻酸钠（SA）溶液中，制备漂浮微丸。然后将混悬液滴入氯化钙溶液中。疏水性低密度的十八醇增强了微丸的持续释放性能和漂浮能力。通过优化不同十八醇与 SA 的重量比，对微丸的粒径、漂浮能力和载药量、包封率和释放度进行了评价。体外释放研究表明，加入十八醇可有效增加胃介质中的漂浮和持续释放时间。大鼠体内研究表明，包载小檗碱的微丸在胃中的滞留时间显著延长。
