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引用本文:黄夏樱,张雅雯,尹丽娜,王胜浩.积雪草酸脂质纳米粒的大鼠口服吸收研究[J].中国现代应用药学,2016,33(4):444-448.
HUANG Xiaying,ZHANG Yawen,YIN Lina,WANG Shenghao.Oral Absorption of Asiatic Acid Lipid Nanoparticles in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(4):444-448.
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积雪草酸脂质纳米粒的大鼠口服吸收研究
黄夏樱, 张雅雯, 尹丽娜, 王胜浩
浙江省医学科学院,杭州 310013
摘要:
目的 考察大鼠口服积雪草酸纳米结构脂质载体(asiatic acid loaded nanostructured lipid carriers,AA-NLC)的口服吸收情况。方法 建立清醒大鼠胆汁引流模型,按50 mg·kg-1的剂量灌胃给予AA-NLC和积雪草酸(asiatic acid,AA)原料(对照组),采用柱前衍生化HPLC检测胆汁药物浓度,考察AA纳米粒的吸收状况。结果 大鼠口服AA-NLC后,药物排泄峰值Cmax是对照组的1.7倍,达峰时间Tmax显著慢于对照组(P<0.05),AA-NLC的消除慢于对照,其消除半衰期T1/2是对照组的2.7倍,与纳米粒吸收有关的药时曲线下面积AUC0-24 h与对照组相比提高了150%。结论 新建立的口服吸收评价方法,初步评价AA-NLC大鼠灌胃后的吸收特性,AA制备成纳米结构脂质载体后可增加口服生物利用度。
关键词:  积雪草酸  纳米结构脂质载体  胆汁引流模型  口服吸收
DOI:
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基金项目:浙江省新世纪151人才工程(第二层次);浙江省医学重点学科群(XKQ-010-001)
Oral Absorption of Asiatic Acid Lipid Nanoparticles in Rats
HUANG Xiaying, ZHANG Yawen, YIN Lina, WANG Shenghao
Zhejiang Academy of Medical Sciences, Hangzhou 310013, China
Abstract:
OBJECTIVE To investigate oral absorption of asiatic acid loaded nanostructured lipid carriers (AA-NLC) in rats. METHODS Biliary drainage model was established in conscious rats and pre-column derivatization HPLC was used to determine the concentration of AA in bile after oral administration of AA-NLC and AA (the control group) to rats respectively at the dosage of 50 mg·kg-1. The absorption of AA nanoparticles was evaluated by comparing the concentrations of drugs. RESULTS In vivo study showed that the Cmax of AA-NLC group was 1.7 times of the control group. The Tmax of AA-NLC group prolonged significantly(P<0.05) in biliary excretion and the elimination half-life T1/2 was 2.7 times of the control group. And the AUC0→24 h increased to 150% compared to the control group. CONCLUSION The new assessment method can evaluate oral absorption of AA-NLC preliminarily. Nanostructured lipid carriers can increase the oral bioavailability of AA in rats.
Key words:  asiatic acid  nanostructured lipid carriers  biliary drainage model  oral absorption
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