姜黄素葡甲胺共晶的大鼠肠吸收特征研究  

Research on intestinal absorption characteristics of meglucumin cocrystal in rats

作　　者：邢潇琳 范春雷[3] 丛晓东[1,2] 杨培培[1,2] 蔡宝昌[1] 

机构地区：[1]浙江中医药大学中药炮制技术研究中心,浙江杭州310053 [2]浙江省省级药学类工程实践教学基地,浙江杭州310053 [3]浙江中医药大学生命科学院,浙江杭州310053

出　　处：《中草药》2015年第11期1645-1648,共4页Chinese Traditional and Herbal Drugs

基　　金：浙江省自然科学基金资助项目(LY15H290005;LY14H290007)

摘　　要：目的比较姜黄素葡甲胺共晶(MGC,姜黄素与葡甲胺通过氢键连接的新共晶化合物)与姜黄素的肠吸收参数变化。方法采用大鼠在体肠段单向灌流模型,用紫外分光光度法(UV)对药物的质量浓度进行检测,分别计算在大鼠各肠段的吸收速率常数(Ka)和表观渗透系数(Papp)。结果 MGC在十二指肠与结肠的Ka和Papp比较有明显差异(P<0.05),其他各肠段间吸收特征相近(P>0.05)。各肠段Ka数据排序:十二指肠>空肠>回肠>结肠;Papp数据排序:十二指肠>空肠>结肠>回肠,MGC的全肠段Ka为(9.966±0.030)×10-3 min-1,Papp为(6.871±0.013)×10-3 cm/min,较姜黄素分别提高了1.53和2.21倍。结论 MGC较姜黄素有更好的肠吸收特征,提示MGC生物利用度可能提高。Objective Meglucumin cocrystal（MGC） is a new cocrystal compound which consists of curcumin with meglumine by hydrogen bond. The intestinal absorption parameter changes of MGC would be observed and be compared with curcumin. Methods The intestine in rats was cannulated for in situ perfusion to study the absorption mechanism of MGC; UV was used to determine the concentration of MGC, to calculate the order of the absorption rate constants（Ka）, and apparent permeability coefficients（Papp）. Results The Ka and Papp of MGC in the duodenum has significantly increased compared with the colon（P〈0.05）, there has been no significant difference（P〉0.05） in other isolated regions of the intestine. The order was： duodenum 〉jejunum 〉ileum 〉colon; And that of Papp was： duodenum〉 jejunum colon 〉ileum. The Ka and Papp in the whole intestine were（9.966 ± 0.030） × 10-3 min-1and（6.871 ± 0.013） × 10^-3 cm/min respectively for the MGC which were 1.53 times and 2.21 times higher than these of curcumin. Conclusion MGC is a better intestinal absorption characteristic than these of curcumin, suggesting that the bioavailability of MGC may be increased.

关 键 词：姜黄素葡甲胺共晶 姜黄素 肠吸收 吸收速率常数 表观渗透系数 

分 类 号：R285.5[医药卫生—中药学]