果胶酮洛芬前药的合成及体外评价
药物前体,,酮洛芬;果胶类;药物前体,0引言,1材料和方法,2结果,3讨论,【参考文献】
Synthesis and in vitro evaluation of pectinketoprofen prodrugXI MiaoMiao, ZHANG SanQi, GU Yi, ZHOU Min, FANG KunQuan
Department of Pharmacy, Xijing Hospital, Fourth Military Medical University, Xian 710033, China
【Abstract】 AIM: To investigate the synthesis and colontargeted characteristics of pectinketoprofen prodrug. METHODS: Pectinketoprofen prodrug was synthesized by the reaction of pectin and ketoprofen in the presence of N, N,Dicyclohexy l carbodiimide. The amount of ketoprofen released from the prodrug was examined after incubating in different simulated gastrointestinal fluids and pectinolytic enzymes fluid at 37℃. RESULTS: The analysis of HPLC results showed that the amount of ketoprofen carried by prodrug was 10.6%. During the incubation, 96.2% ketoprofen released from prodrug in 8h in simulated pectinolytic enzymes fluid. However, there was almost no ketoprofen released in simulated stomach fluid and small intestinal fluid as well as in simulated colon fluid. CONCLUSION: The experiment suggests that pectinketoprofen may be potentially useful in the colonspecific delivery of ketoprofen. ......
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