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美洛昔康-β-环糊精包合物分散片的研制及其直接压片评价。

Development and evaluation of fast-dissolving tablets of meloxicam-β-cyclodextrin complex prepared by direct compression.

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, P.O. Box 3030, Irbid-Jordan.

出版信息

Acta Pharm. 2011 Mar;61(1):83-91. doi: 10.2478/v10007-011-0005-7.

Abstract

The aim of this study was to prepare fast-dissolving tablets of meloxicam after its complexation with β-cyclodextrin (β-CD) and to investigate the effect of using different superdisintegrants on the disintegration and release of meloxicam from the tablets. A complex of meloxicam with β-CD was prepared by spray drying and then compressed in the form of tablets utilizing the direct compression technique. Three superdisintegrants were employed at various levels - sodium starch glycolate, croscarmellose sodium, and crospovidone. Co-spray dried micro-crystalline cellulose and mannitol (Avicel HFE-102) were used as diluents in the tablets. Prior to compression, the pre-compression parameters showed satisfactory flow properties. Post-compression parameters showed that all tablet formulations had acceptable mechanical properties. Wetting and disintegration times were prolonged by increasing the level of sodium starch glycolate in the tablets. This was attributed to the formation of a viscous gel layer around the tablets by sodium starch glycolate whereas this effect was not observed with croscarmellose sodium and crospovidone. Dissolution studies showed fast release of meloxicam except in tablets containing a high level of sodium starch glycolate. Complexation of meloxicam with β-CD significantly improved the solubility of the drug and improved the mechanical properties of tablets produced by direct compression.

摘要

本研究的目的是制备美洛昔康与β-环糊精(β-CD)形成包合物后的速溶片,并考察使用不同超分散剂对美洛昔康从片剂中崩解和释放的影响。采用喷雾干燥法制备美洛昔康-β-CD 包合物,然后利用直接压片技术将其压制成片剂。采用三种不同水平的超分散剂——交联羧甲淀粉钠、羧甲基纤维素钠和交联聚维酮。共喷雾干燥的微晶纤维素和甘露醇(Avicel HFE-102)用作片剂中的稀释剂。在压缩之前,预压缩参数显示出令人满意的流动性能。压缩后的参数表明,所有片剂配方均具有可接受的机械性能。增加片剂中交联羧甲淀粉钠的水平会延长润湿和崩解时间。这归因于交联羧甲淀粉钠在片剂周围形成粘性凝胶层,而这种作用在羧甲基纤维素钠和交联聚维酮中没有观察到。溶出研究表明,除了含有高浓度交联羧甲淀粉钠的片剂外,美洛昔康都能快速释放。美洛昔康与β-CD 的络合显著提高了药物的溶解度,并改善了直接压片生产的片剂的机械性能。

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