基于Ussing Chamber技术评价阿苯达唑纳米晶体在大鼠不同肠段的吸收特性

Absorption study of albendazole nanocrystals in different intestinal segments in rats by Ussing Chamber system

目的:研究阿苯达唑纳米晶体(ABZ-NCs)在大鼠不同肠段的吸收动力学特征。方法:采用尤斯室技术进行肠吸收试验,利用高效液相色谱法测定ABZ-NCS在大鼠十二指肠、空肠、回肠、结肠4个肠段的吸收状况,并考察不同浓度药物对肠吸收的影响,同时与ABZ片剂(T-ABZ)进行比较。结果:ABZ-NCS不同浓度在不同肠段均有吸收,且各肠段的吸收速率常数Ka随着药物浓度的增加而增加,具有明显的浓度依赖性,提示其可能为被动吸收;ABZ-NCS组各肠段的累积吸收量Q、吸收速率常数Ka和表观渗透系数P_(app)均高于相同质量浓度的T-ABZ组(P<0.01)。结论:该研究结果表明,ABZ-NCS与T-ABZ在整个大鼠小肠均有吸收,吸收机制可能为被动吸收,尤其是ABZ-NCS能显著改善药物的肠吸收。

OBJECTIVE To explore the absorption characteristics of albendazole nanocrystals(ABZ-NCs)in different intestinal segments of rats.METHODS Ussing Chamber system model was adopted for intestinal absorption test and ABZ content determined by high performance liquid chromatograph(HPLC)for examining the absorption characteristics of ABZ-NCs in rat duodenum,jejunum,ileum and colon,understanding the effects of different drug concentrations on intestinal absorption and comparing them with Albendazole tablets(T-ABZ).RESULTS ABZ-NCs were absorbed at different intestinal segments and different concentrations.The absorption constant Ka increased with a rising drug concentration,indicating a probable passive absorption.The accumulative absorption volume Q,absorption constant Ka and apparent permeability coefficients(P_(app))of ABZ-NCs were higher than those of T-ABZ at each intestinal segment(P<0.01).CONCLUSION ABZ-NCs and T-ABZ are absorbed in whole intestinal segments and its mechanism may be through a passive absorption.In particular,ABZ-NCs can significantly improve the intestinal absorption of drugs.