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洛索洛芬的新型缓释速崩多单位压缩片剂,包含 Eudragit RS 包衣壳聚糖-海藻酸钠珠。

Novel sustained-release fast-disintegrating multi-unit compressed tablets of lornoxicam containing Eudragit RS coated chitosan-alginate beads.

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Pharm Dev Technol. 2011 Aug;16(4):316-30. doi: 10.3109/10837451003692595. Epub 2010 Mar 23.

DOI:10.3109/10837451003692595
PMID:20307250
Abstract

Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of sustained-release lornoxicam beads directly compressed with fast-disintegrating component, containing amorphous solid dispersion of lornoxicam, anticipating rapid drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain extended analgesic effect. Initially, calcium-alginate and chitosan-alginate beads containing lornoxicam were prepared. Then, the erosion of selected beads formulation was suppressed by treatment with Eudragit RS either through polymer-reinforcement or beads coating. The beads, which elicited appropriate sustainment of lornoxicam release, were directly compressed with fast-disintegrating components to form FDMUTs. The release characteristics of the original beads were maintained after compression which indicates that the adopted compression process did not induce mechanical damage to the beads or coating. All of the prepared FDMUTs demonstrated acceptable physical properties that complied with compendial requirements. Release studies, performed in simulated gastric and intestinal fluids used in sequence to mimic the gastrointestinal transit, illustrate that the FDMUTs containing 8?mg lornoxicam equally distributed between the sustained-release beads and the fast-release component, showed the desired release profile.

摘要

新型速崩多单元片剂(FDMUT)被制备用于控制洛索洛芬(一种半衰期短的强效非甾体抗炎药)的释放,同时将多单元系统的优势与片剂的成本效益相结合。所提出的 FDMUT 由与速崩成分直接压缩的控释洛索洛芬丸组成,其中包含洛索洛芬的无定形固体分散体,预计药物在胃中快速释放以迅速缓解疼痛症状,并在肠道中持续释放以维持延长的镇痛效果。最初,制备了含有洛索洛芬的海藻酸钙和壳聚糖-海藻酸钙珠。然后,通过用 Eudragit RS 处理来抑制选定的珠粒制剂的侵蚀,通过聚合物增强或珠粒包衣来实现。引发洛索洛芬释放适当维持的珠粒直接与速崩成分压缩形成 FDMUT。压缩后保持了原始珠粒的释放特性,这表明采用的压缩工艺不会对珠粒或涂层造成机械损伤。所有制备的 FDMUT 均表现出可接受的物理性质,符合典则要求。在模拟胃和肠道液中进行的释放研究,按胃肠道转运的顺序进行,表明含有 8?mg 洛索洛芬的 FDMUT 均匀分布在控释珠和速释成分之间,显示出所需的释放特征。

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