目的 考察原人参二醇纳米混悬剂的在体肠吸收特征。方法 采用溶剂蒸发法, 以白蛋白作为稳定剂制备原人参二醇纳米混悬剂。以酚红为标示物, 采用大鼠在体单向肠灌流法评价原人参二醇纳米混悬剂的大鼠在体肠吸收特性。结果 Zetasizer nano ZS仪测得原人参二醇纳米混悬剂平均粒径为(220±10)nm, Zeta电位为(-28±0.2)mV。肠吸收实验表明, 原人参二醇纳米混悬剂在整个肠段都有吸收, 且吸收速率常数(K_a)与渗透系数(P_eff)均大于原人参二醇原药(P<0.05), 原人参二醇纳米混悬剂在小肠段(十二指肠、空肠和回肠)的K_a与P_eff均大于结肠(P<0.05)。结论 原人参二醇纳米混悬剂能够有效促进原人参二醇的大鼠在体肠吸收, 其转运机制可能为主动转运或促进扩散。

Objective To investigate the rat intestinal absorption characters of protopanaxadiol (PPD) nanosuspensions (NPS). Methods PPD-NPS were made by using solvent evaporation method with bovinel serum albumin as carrier. The absorption of PPD-NPS were evaluated with phenol red as the marker by in situ single-pass perfusion model of rats. Results The mean diameter of the particle (220 ± 10) nm and the Zeta potential (-28 ± 0.2) mV were studied using Zetasizer nano ZS instrument. The result of rat intestinal absorption indicated that the absorption of PPD-NPS was observed in the whole intestinal tract. The absorption constant (K_a) and the effective absorption coefficient (P_eff) of PPD-NPS were higher than those of the bulk drug (P<0.05), the K_a and P_eff of PPD-NPS at small intestine (duodenum, jejunum, and ileum) were higher than those at colon (P<0.05). Conclusion PPD-NPS can improve the absorption of PPD in rat intestine. The transport mechanism may be active transport or facilitated diffusion.

国家自然科学基金(NO 81102813);黑龙江中医药大学重点实验室开放课题(2013kf05)