5-氟脲嘧啶在欧巴代包覆介孔SBA-15的药物系统中的缓释行为研究.docVIP

5-氟脲嘧啶在欧巴代包覆介孔(SBA-15的药物系统中的缓释行为研究 吴都督1，陈稚2*，陈戊生1，麦维琴1，刘小柳3，周晓莹3，黎永坚3 （1广东医学院 药学院，广东 东莞 523808；2广东医学院 分析中心，广东 东莞 523808；3 广东医学院 医学检验学院，广东 东莞 523808） 摘要：将肠溶包衣欧巴代（OPD）包覆于负载了抗癌药物5-氟脲嘧啶（5-Fu）的SBA-15介孔分子筛表面，制备了pH敏感的药物控释系统OPD/SBA-15，并考察了该药物系统在不同pH释放环境中的释放行为。实验结果表明，在模拟胃液中（pH=1.2），OPD能明显地延缓5-Fu的释放速度。药物释放6 h后，其释放率仅为20.2 %。而在模拟肠液中（pH=7.5），OPD能够迅速溶于肠液，对5-Fu释放速度的影响甚微。药物释放6 h后，释放率可达到88.6 %。同时，膜的干燥温度影响5-Fu的释放行为，干燥温度越高，药物系统在模拟胃液中的缓释效果越强。 关键词：5-氟脲嘧啶；介孔分子筛；pH敏感；药物缓释; 欧巴代 SBA-15 tablet coated with opadry as a drug release carrier for 5-fluorouracil Wu Dudu1, Chen Zhi2*, Chen Wusheng 1, Mai Weiqin1, Liu Xiaoliu3, Zhou Xiaoying3, Li Yongjian3 (1 School of Pharmacy, Guangdong Medical College, Dongguan, 523808, Guangdong , China; 2 Center of Analysis, Guangdong Medical College, Dongguan, 523808, Guangdong , China; 3 School of Laboratory Medicine, Guangdong Medical College, Dongguan, 523808, Guangdong , China) Abstract: In order to improve the cancer targeting and selectivity of antineoplastic agent 5-fluorouracil (5-Fu), a pH-sensitive drug release system was synthesized by coating opadry (OPD) on a SBA-15 tablet. 5-Fu was loaded into the carriers by an adsorption method in methanol and water mixed solution (volume ratio 1:2). Two kinds of release fluids, including simulated intestinal fluid (SIF, pH=7.4) and simulated gastric fluid (SGF, pH=1.2), were used to investigate the drug release behavior of the OPD/SBA-15 system. In SGF, compared with without OPD coating materials, the coating carriers could effectually delay the release rate of 5-Fu. However, in SIF, no distinct influence of the coating materials on the drug delivery rate was found, which was possible that OPD could quickly dissolve into the SIF. Moreover, it was found that the higher drying temperature of OPD, the better performance of the drug release OPD/SBA-15 system. Keywords: 5-fluorouracil; Mesoporous molecular sieves; pH-sensitive; Drug release; Opadry 药物是目前治疗癌症的常用手段，5-氟脲嘧啶（5-Fu）是常用的治疗肠癌的药物[1]。但在传统口服给药方式中，5-Fu在到达肠道以前大部