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5-氟尿嘧啶在pH敏感型分子筛控释载体中的缓释行为

     

摘要

以肠溶性的羟丙基甲基纤维素邻苯二甲酸酯(HPMCP)作为包覆材料,制备了HPMCP包覆的SBA-15介孔分子筛药物控释载体(HPMCP/SBA-15),并考察了抗癌药物5-氟尿嘧啶(5-Fu)负载于控释载体后,在不同pH释放环境中的释放行为.结果表明,在模拟胃液中(pH=1.2),HPMCP能明显地延缓5-Fu的释放速度;药物释放4h后,其释放率仅为15%.而在模拟肠液中(pH=7.5) HPMCP迅速溶解,对5-Fu释放速度的影响甚微;药物释放4h后,释放率可达到80%.与此同时,包覆膜的干燥温度影响5-Fu的释放行为,干燥温度越高,药物在模拟胃液中的释放速度越慢.%A pH-sensitive mesoporous molecular sieve as drug release carrier was synthesized by coating SBA-15 tablet with hydroxypropyl methylcellulose phthalate (HMPCP) so as to improve the cancer targeting ability and selectivity of antineoplastic agent 5-fluorouracil (5-Fu). Into the drug release carrier (HPMCP/SBA-15) was loaded 5-Fu by adsorption in the mixed solution of water and methanol (volume ratio 1:1). The releasing behavior of loaded 5-Fu in two kinds of release fluids with different pH environment, simulated intestinal fluid (SIF, pH = 7. 4) and simulated gastric fluid (SGF, pH = 1.2), was examined. Results indicate that in SGF the coating carrier can effectively delay the release rate of 5-Fu, with release rate being only 15% after 4 h of drug release. However, in SIF it has no obvious effect on the drug delivery rate, possibly due to the dissolution of HPMCP in SIF; and in this case the release rate reaches 80% after 4 h of drug release. Moreover, the release behavior of 5-Fu is also dependent on the temperature for drying HPMCP, and higher drying temperature corresponds to better drug release performance of loaded 5-Fu in SGF.

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