自微乳给药系统促进葛根素在大鼠淋巴及血液吸收的研究  

Study of Self-microemulsifying Drug Delivery System in Promoting Lymphatic and Hematological Transport of Puerarin in Rats After Oral Administration

作　　者：刘昌顺[1] 龙晓英[1] 陈莉[2] 陈月凤[1] 罗强[1] 梁浩明[1] 

机构地区：[1]广东药学院,广东广州510006 [2]遵义医学院,贵州遵义563003

出　　处：《中药新药与临床药理》2015年第6期809-813,共5页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：国家自然科学基金资助项目(30973953C1909)

摘　　要：目的探索葛根素自微乳给药系统(self-microemulsifying drug delivery systems of puerarin,PUE-SMEDDS)对PUE经肠淋巴转运及其口服生物利用度的影响。方法构建SD大鼠肠系膜淋巴转运模型,口服给药后同步收集淋巴液和血样,HPLC色谱法测定PUE在淋巴液和血浆中的含量,用梯形面积法计算AUC。结果葛根素混悬液(PUE-Suspension)的淋巴转运相对较低,Cmax仅为0.39μg·m L-1,而PUE-SMEDDS的Cmax为5.77μg·m L-1,显著提高PUE肠淋巴转运(P<0.001)。PUE-Suspension在淋巴液和血浆中的AUC0-12 h分别为158.1,438.1 min·μg·m L-1,淋巴转运量占体内吸收总量的36.09%;而PUE-SMEDDS在淋巴液和血浆中的AUC0-12 h分别为1953.3,1641.3 min·μg·m L-1,淋巴转运量占体内吸收总量的54.34%,PUE-SMEDDS的相对生物利用度(Fr)为603.0%。结论 SMEDDS能同时促进PUE经淋巴转运和血液吸收,显著提高PUE的口服生物利用度,而且PUE的淋巴转运量大于血液循环。Objective To investigate the effect of self-mieroemulsifying drug delivery system of puerarin （PUE- SMEDDS） on bioavailability improvement via enhancing the intestinal lymphatic transport after oral administration. Methods SD rat model of mesenteric lymphatic transport was established. After oral administration, lymph fluid and blood were sampled at the same time, PUE concentrations in the lymph liquid and plasma was determined by HPLC, and trapezoidal area method was used for the calculation of the area under the curve（AUC0-12h）. Results The lymphatic transport of puerarin suspension （PUE-Suspension） was low with Cmaxof 0.39 μg.mL-1, while the Cmax of PUE in PUE-SMEDDS was 5.77 μg.mL-1, indicating that the intestinal lymphatic transport of PUE was significantly improved （P 〈 0.001 ）. In PUE-suspension group, the AUC0-12h value of PUE was 158.1 min.μg.mL-1 in the lymph liquid and was 438.1 min .μg.mL-1 in the plasma, and the amount of lymphatic transport was accounted for 36.09 % of total absorption. In PUE-SMEDDS group, the AUC0-12h value of PUE was 1953.3 min.μg.mL-1 in lymph liquid and was 1641.3 min.μg.mL-1 in the plasma, the amount of lymphatic transport was accounted for 54.34 % of total absorption,and the relative bioavailability of PUE-SMEDDS was 603.0 %. Conclusion It was found that PUE-SMEDDS promotes the intestinal lymphatic transport and blood absorption of PUE, significantly improves the oral bioavailability of PUE, and the contribution of lymphatic transport is more than blood absorption.

关 键 词：葛根素 自微乳给药系统 淋巴转运 药物动力学 

分 类 号：R285.5[医药卫生—中药学]