Meka Lingam, Kesavan Bhaskar, Chinnala Krishna Mohan, Vobalaboina Venkateswarlu, Yamsani Madhusudan Rao
Novel Drug Delivery Systems Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, Andhra Pradesh, India.
AAPS PharmSciTech. 2008;9(2):612-9. doi: 10.1208/s12249-008-9090-4. Epub 2008 May 6.
A gastro retentive floating drug delivery system with multiple-unit minitab's based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter dissolution data after storage at 40 degrees C and 75% RH for 3 months showed, no significant change indicating the two dissolution profiles were considered to be similar (f2 value is more than 50).
为延长药物在胃内的滞留时间并提高药物的整体生物利用度,研发了一种基于气体形成技术的多单元微型片胃滞留漂浮给药系统。该系统由通过直接压片工艺制备的含药核心单元组成,这些核心单元依次涂覆有三层涂层,即内密封层、泡腾层(碳酸氢钠)和外气体包裹聚合物膜(聚甲基丙烯酸酯,如Eudragit RL30D、RS30D及其组合)。只有使用Eudragit RL30D及其组合作为气体包裹聚合物膜的系统能够漂浮。随着泡腾剂用量的增加和气体包裹聚合物膜包衣水平的降低,漂浮时间缩短。最佳系统在3分钟内完全漂浮,并在12小时内保持漂浮状态。药物释放得到控制,且与时间的平方根呈线性关系。增加气体包裹聚合物膜的包衣水平会降低药物释放。本研究开发的多单元漂浮给药系统实现了快速漂浮和控释特性。在40℃和75%相对湿度下储存3个月后对参数溶出数据的分析表明,无显著变化,表明两种溶出曲线被认为相似(f2值大于50)。