氯化钙对吲哚美辛果胶骨架片体外释放的影响

Effect of Calcium Choloride on Indomethacin Release from Pectin-Based Matrix Tablets

目的制备含吲哚美辛的果胶氯化钙骨架片,考察影响其体外释放的因素。方法湿法制粒压片法制备吲哚美辛果胶氯化钙骨架片。分别考察氯化钙质量、果胶-氯化钙质量比以及释放介质对释放度的影响。通过溶蚀及吸水性试验,考察氯化钙的作用机制。结果骨架中果胶-氯化钙的质量比、药物-骨架质量比以及骨架的组成均可显著影响药物的释放。果胶氯化钙骨架片在不同的释放介质中表现出不同的释放行为。药物的释放与骨架的溶蚀及吸水速率呈正相关。在果胶酶(PectinexUltraSP-L)存在的条件下,骨架中药物的释放加快且释放完全。结论果胶氯化钙骨架片可通过果胶与钙离子的交联钙化形成强度较高的凝胶,降低了果胶的溶解度,具有缓控释效果,可通过进一步的设计达到结肠靶向的目的。

OBJECTIVE To prepare pectin-calcium chloride matrix tablets and evaluate indomethacin release profiles in vitro, METHODS wet granulation technique was employed to prepare pectin-calcium chloride matrix tablets, The amount of calcium chloride, the mass ratio of calcium chloride/pectin and release media on drug release profiles were investigated. Matrix erosion and water uptake were performed to elucidate the mechanisms of calcium chloride on drug release. RESULTS The ratio of pectin/calcium chloride and mass ratio of drug/matrix were important factors on the drug release. The pectin-calcium chloride matrix tablets had different release profile in various media. The drug release rate was positively correlated to matrix erosion rate and the relative water uptake rate. The drug released quickly and completely with the Pectinex Ultra SP-L. CONCLUSION The pectin-calcium chloride-based matrix tablets can form relative rigid gel by crosslinking between pectin and calcium ions in situ. This kind of system has potential to be used to target drugs to the colon.