Meka Lingam, Kesavan Bhaskar, Kalamata Venkatasimhadri Naidu, Eaga Chandra Mohan, Bandari Suresh, Vobalaboina Venkateswarlu, Yamsani Madhusudan Rao
Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009, Andhra Pradesh, India.
J Pharm Sci. 2009 Jun;98(6):2122-32. doi: 10.1002/jps.21562.
A gastro retentive floating drug delivery system with multiple-unit minitablets based on gas formation technique was developed for furosemide. The system consists of core units (solid dispersion of furosemide:povidone and other excipients), prepared by direct compression process, which are coated with two successive layers, one of which is an effervescent (sodium bicarbonate) layer and other one an outer polymeric layer of polymethacrylates. The formulations were evaluated for pharmacopoeial quality control tests and all the physical parameters evaluated were within the acceptable limits. Only the system using Eudragit RL30D and combination of them as polymeric layer could float within acceptable time. The time to float decreased as amount of the effervescent agent increased and, when the coating level of polymeric layer decreased. The drug release was controlled and linear with the square root of time. By increasing coating level of polymeric layer decreased the drug release. The rapid floating and the controlled release properties were achieved in this present study. The stability samples showed no significant change in dissolution profiles (f(2) = 81). The in vivo gastric residence time was examined by radiograms and it was observed that the units remained in the stomach for about 6 h.
基于气体形成技术，开发了一种用于呋塞米的具有多单元微型片的胃滞留漂浮药物递送系统。该系统由通过直接压片工艺制备的核心单元（呋塞米与聚维酮及其他辅料的固体分散体）组成，核心单元上依次包被两层，一层是泡腾层（碳酸氢钠），另一层是聚甲基丙烯酸酯类的外层聚合物层。对制剂进行了药典质量控制测试，所有评估的物理参数均在可接受范围内。只有使用欧巴代RL30D及其组合作为聚合物层的系统能够在可接受的时间内漂浮。随着泡腾剂用量的增加以及聚合物层包衣水平的降低，漂浮时间缩短。药物释放得到控制且与时间的平方根呈线性关系。通过增加聚合物层的包衣水平，药物释放减少。在本研究中实现了快速漂浮和控释特性。稳定性样品的溶出曲线无显著变化（f(2)=81）。通过射线照相法检查了体内胃滞留时间，观察到这些单元在胃中停留约6小时。
