Abstract Purpose This study was to design and evaluate effervescent floating tablets with sustained release behaviour. Pentoxifylline is a water-soluble model drug with a short half-life, consequently developing sustained release preparations would be beneficial. Methods A binary (1:1) mixture of sodium alginate and hydroxyethyl cellulose containing pentoxifylline, with either 10% or 20% calcium carbonate or sodium carbonate, was used to prepare floating tablets. Results Tablets floated on the surface of the dissolution medium, showed an adequate floating lag time, and floated for more than 12 hours. Tablets manufactured from granules with 20%(w/w) calcium carbonate were promising with respect to their floating lag time (~ 7min), floating duration (> 24 hours), sustained drug release rate, and swelling ability. An in vivo study of these promising tablets and a reference solution of pentoxifylline were investigated following oral administration of 5.75 ± 0.15mg in rats. Compared with the reference solution, the pharmacokinetic parameters changed significantly ( p max of the tablets was decreased (945.32ng/ml versus 2552.30ng/ml for the solution), while the T max and t 1/2 were prolonged. Conclusion The study shows that a binary mixture of hydroxyethyl cellulose and sodium alginate, together with 20%(w/w) calcium carbonate, offers an exciting opportunity to develop sustained release pentoxifylline preparations.

中文翻译：

---

碳酸钙和碳酸钠充气剂对己酮可可碱漂浮片性质的影响

摘要 目的本研究旨在设计和评价具有缓释性能的泡腾漂浮片。己酮可可碱是一种半衰期短的水溶性模型药物，因此开发缓释制剂将是有益的。方法 使用含有己酮可可碱的海藻酸钠和羟乙基纤维素的二元 (1:1) 混合物与 10% 或 20% 碳酸钙或碳酸钠的混合物制备漂浮片。结果片剂漂浮在溶出介质表面，表现出足够的漂浮滞后时间，漂浮时间超过12小时。由含 20% (w/w) 碳酸钙的颗粒制成的片剂在漂浮滞后时间 (~ 7 分钟)、漂浮持续时间 (> 24 小时)、持续药物释放速率和溶胀能力方面很有前景。在大鼠中口服 5.75 ± 0.15mg 后，对这些有前景的片剂和己酮可可碱参考溶液进行了体内研究。与参比溶液相比，药代动力学参数发生显着变化（片剂p max 降低（945.32ng/ml vs 2552.30ng/ml），T max 和t 1/2 延长。结论 研究表明羟乙基纤维素和海藻酸钠的二元混合物以及 20% (w/w) 碳酸钙为开发缓释己酮可可碱制剂提供了令人兴奋的机会。