Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran.
Pharm Dev Technol. 2011 Aug;16(4):400-7. doi: 10.3109/10837451003774393. Epub 2010 Apr 30.
In the present study, metronidazole was used for preparing floating dosage forms that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. For this means, various formulations were designed using multi-factorial design. HPMC, psyllium and carbopol in different concentrations were used as floating agents, and sodium bicarbonate was added as a gas-forming agent. Hardness, friability, drug loading, floating ability and release profiles as well as kinetics of release were assessed. Formulations containing HPMC as filler showed prolonged lag times for buoyancy. Adding psyllium to these formulations had reduced relative lag times. Overall, selected formulations were able to float immediately and showed buoyancy for at least 8?h. Meanwhile, sustained profiles of drug release were also obtained. Kinetically, among the 10 assessed models, the release pattern of metronidazole from the tablets fitted best to Power law, Weibull and Higuchi models in respect overall to mean percentage error values of 3.8, 4.73 and 5.77, respectively, for calcium carbonate-based tablets and, 2.95, 6.39 and 3.9, respectively, for calcium silicate-based tablets. In general, these systems can float in the gastric condition and control the drug release from the tablets.
在本研究中，使用甲硝唑制备了漂浮剂型，旨在在胃中长时间保留，并开发为治疗消化性溃疡疾病中幽门螺杆菌的药物传递系统。为此，使用多因素设计设计了各种配方。以不同浓度的 HPMC、车前子和卡波姆作为漂浮剂，并添加碳酸氢钠作为产气剂。评估了硬度、脆碎度、载药量、漂浮能力和释放曲线以及释放动力学。含有 HPMC 作为填充剂的制剂显示出延长的浮力滞后时间。向这些制剂中添加车前子可以减少相对滞后时间。总的来说，所选制剂能够立即漂浮并保持至少 8 小时的浮力。同时，还获得了药物持续释放的曲线。动力学方面，在所评估的 10 种模型中，甲硝唑从片剂中的释放模式最符合幂律、Weibull 和 Higuchi 模型，对于基于碳酸钙的片剂，整体平均百分比误差值分别为 3.8、4.73 和 5.77，对于基于硅酸钙的片剂，分别为 2.95、6.39 和 3.9。总的来说，这些系统可以在胃环境中漂浮，并控制片剂的药物释放。
