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(K_a)和表观渗透系数(P_app)。结果 MGC在十二指肠与结肠的K_a和P_app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K_a数据排序:十二指肠 > 空肠 > 回肠 > 结肠;P_app数据排序:十二指肠 > 空肠 > 结肠 > 回肠, MGC的全肠段K_a为(9.966±0.030)×10^-3 min^-1, P_app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 (K_a), and apparent permeability coefficients (P_app). Results The K_a and P_app 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 P_app was: duodenum > jejunum > colon > ileum. The K_a and P_app 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.

浙江省自然科学基金资助项目(LY15H290005, LY14H290007)