摘要
目的：通过体外法研究羧甲基魔芋胶的酶降解性能，评价其作为结肠定位给药系统载体材料使用的可行性。方法：分别用含大鼠胃、肠道内容物或商品酶的溶液模拟体内胃、肠道酶降解环境，采用黏度法考察羧甲基魔芋胶的酶降解性能，并对材料的酶降解动力学和醚化度与溶液pH对材料降解性能的影响进行研究。结果：羧甲基魔芋胶在模拟胃和小肠环境的溶液中不被降解，在模拟盲、结肠环境的溶液中可被降解；羧甲基魔芋胶和魔芋胶的酶降解动力学符合米氏方程，羧甲基魔芋胶的酶降解性能随其醚化度增加而降低，在pH6．0—6．8溶液中，羧甲基魔芋胶的酶降解性能高。结论：羧甲基魔芋胶具有结肠定位酶降解性能，可作为酶降解型结肠定位给药系统载体材料使用。
Objective： In vitro enzymatic degradation of carboxymethy konjac glucomannan （CMKGM） were studied to evaluate the feasibility of CMKGM used as carrier materials to prepare colon-specific drug delivery systems. Method： The solutions with rat gastrointestinal tract （GIT） contents or with commercial enzymes were chosen to stimulate in vivo GIT environment, respectively. Enzymatic degradation of CMKGM were studied by viscometic procedure. Degradation kinetics of CMKGM and konjac glucomannan （KGM） by enzymes, the effects of the degree of substitution （DS） of CMKGM and the pH of solution on its susceptibility to degradation were investigated. Result： CMKGM were degraded mainly in the simulated cecal and colonic media, but not in the simulated gastric and enteric media. Degradation of KGM and CMKGM by enzymes obeyed Michaelis-Menton kinetics. CMKGM with lower DS were more susceptible substrates. CMKGM were more susceptible substrates in solution with pH 6. 0-6. 8. Conclusion： CMKGM had colon-specific enzymatic degradation characteristics and could be used as carrier materials to prepare colon-specific drug delivery systems.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2007年第22期2360-2363,共4页
China Journal of Chinese Materia Medica
关键词
羧甲基魔芋胶
结肠定位
酶降解
大鼠盲
结肠内容物酶
Β-甘露聚糖酶
carboxymethyl konjac glucomannan
colon-specific
enzymatic degradation
rat cecal and colonic enzymes
β- mannase
