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出 处:《环球中医药》2015年第10期1158-1163,共6页Global Traditional Chinese Medicine
基 金:国家自然科学基金(30801549);北京中医药大学创新团队发展计划(2011-CXTD-13);北京中医药大学自主选题(2014-JYBZZ-XS-087)
摘 要:目的考察姜黄素—胡椒碱复方自微乳给药系统对姜黄素在结肠部位稳定性的改善作用,为其治疗结肠炎或结肠癌等结肠局部疾病提供科学依据。方法通过HPLC测定姜黄素的含量,37℃体外考察并比较姜黄素溶液、姜黄素—胡椒碱混合溶液及姜黄素—胡椒碱复方自微乳在人工结肠液及小鼠结肠组织匀浆液中的稳定性。结果 37℃人工结肠液中孵育24小时后,姜黄素溶液、姜黄素—胡椒碱混合溶液和姜黄素—胡椒碱复方自微乳中姜黄素的降解百分率分别为19.93%、12.67%和10.50%,降解过程符合一级动力学方程,半衰期分别为19.67小时、57.87小时和75.23小时;37℃小鼠结肠组织匀浆液中孵育8小时后,姜黄素溶液、姜黄素—胡椒碱混合溶液和姜黄素-胡椒碱复方自微乳中姜黄素的降解百分率分别为19.96%、14.49%和4.63%。结论姜黄素-胡椒碱复方自微乳给药系统可以显著改善姜黄素在结肠部位的的稳定性(P<0.05),有望增强对结肠局部疾病的治疗效果。Objective To investigate whether the curcumin-piperine dual drug loaded self-microe-mulsifying drug delivery system ( Cur-PIP-SMEDDS ) could enhance the curcumin’s stability in the colon site. This study could provide scientific basis for the treatment of colonic disease, such as colitis and colon cancer. Methods HPLC method was established for the determination of the content of curcumin. To determine whether Cur-PIP-SMEDDS is more stable in the colonic site, free curcumin, curcumin-piperine mixture and Cur-PIP-SMEDDS were incubated in the artificial colon fluid and the mice colonic tissue homogenized mixture at 37℃, and sampled periodically to determine the concentration of curcumin by HPLC. Results The degradation percentage of curcumin in free curcumin solution, curcumin-piperine mixture, and Cur-PIP-SMEDDS were 19. 93%, 12. 67% and 10. 50% respectively after incubation for 24 hours in the artificial colon fluid at 37℃. The degradation process of curcumin followed apparent first-order kinetics equation, and the half-life were 19. 67 h, 57. 87 h and 75. 23 h respectively. The degradation percentage of curcumin in free curcumin solution, curcumin-piperine mixture, and Cur-PIP-SMEDDS were 19. 96%, 14. 49% and 4. 63% respectively. After incubation for 8 hours in the mice colonic tissue homogenized mixture at 37℃. Conclusion The results showed that Cur-PIP-SMEDDS could significantly enhance the stability of curcumin ( P〈0. 05 ) in the colonic site, and may enhance the efficacy for the treatment of colonic disease.
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