Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent
Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent
复制标题
羟丙基纤维素与泡腾剂复合压制包衣氧氟沙星控释漂浮片
DOI：
10.1016/j.ijpharm.2015.05.007
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发表时间：
2015-07-15
影响因子：
5.8
通讯作者：
Wu, Zhenghong
中科院分区：
文献类型：
--
作者：
Qi, Xiaole;Chen, Haiyan;Wu, Zhenghong
如何延长药物在胃肠道内的滞留时间，使药物以预期的速率释放，是口服控释给药系统面临的真实的挑战之一。本文以亲水性高分子羟丙基纤维素为包衣材料，结合碳酸氢钠为缓释剂，研制了一种同时控制氧氟沙星释放速率和定位的漂浮片。在包衣层中还加入海藻酸钠以调节药物释放速率。考察了药物质量比、羟丙基纤维素粘度对释药行为的影响。优化的制剂被发现立即浮动在30秒内，并保持持久的浮力超过12小时的时间内在模拟胃液（SGF，pH 1.2）没有胃蛋白酶，表明一个令人满意的浮动和零级药物释放曲线。此外，新西兰兔口服生物利用度实验表明，与市售普通释放片泰利必妥（R）相比，口服漂浮片后氧氟沙星的相对生物利用度为172.19%。这些结果表明，这种控释漂浮片是一种很有前途的胃内滞留给药系统。(C)2015 Elsevier B.V.版权所有。
To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system. Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin. Sodium alginate was also added in the coating layer to regulate the drug release rate. The effects of the weight ratio of drug and the viscosity of HPC on the release profile were investigated. The optimized formulations were found to immediately float within 30 s and remain lastingly buoyant over a period of 12 h in simulated gastric fluid (SGF, pH 1.2) without pepsin, indicating a satisfactory floating and zero-order drug release profile. In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172.19%, compared to marketed common release tablets TaiLiBiTuo (R). These results demonstrated that those controlled-released floating tables would be a promising gastro-retentive delivery system for drugs acting in stomach. (C) 2015 Elsevier B.V. All rights reserved.