大鼠口服灯盏花素的肠淋巴通道转运研究  

Intestinal lymphatic transport of breviscapine orally administered in rat

作　　者：弓艺涓[1,2] 王建新[1] 张赟[1] 沈敏[1] 傅超美[2] 沈腾[1] 

机构地区：[1]复旦大学药学院药剂学教研室智能化递药教育部和全军重点实验室,上海201203 [2]成都中医药大学药学院,四川成都611137

出　　处：《药学学报》2011年第10期1262-1267,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81072594);国家重大科技专项经费资助(2009ZX09310-006)

摘　　要：建立清醒大鼠肠系膜淋巴管和颈静脉的双插管模型,以探索灯盏花素口服经肠淋巴通道的转运规律。采用HPLC法测定血浆和淋巴液中灯盏乙素浓度。双插管大鼠模型分别进行静注和口服灯盏花素的药动学实验。灯盏乙素静脉注射后存在从血液循环向肠淋巴系统的分布,肠淋巴累积转运量为(2.78±0.25)μg,是静注剂量的0.079 2%。灯盏乙素口服经肠淋巴通道12 h累积转运量为(0.92±0.08)μg,是口服剂量的0.008 3%;口服主要经门静脉通道吸收,绝对生物利用度为4.91%。灯盏乙素与乳糜微粒表面载脂蛋白的结合可能是其肠淋巴转运的主要形式。本研究为通过促进灯盏乙素肠淋巴转运而获得高生物利用度的灯盏花素脂质给药系统的研制提供了生物药剂学基础。Double cannulation model of conscious rat allowing simultaneous collection of mesenteric lymph and jugular venous blood was established to investigate the intestinal lymphatic transport of breviscapine orally administered in rat.The concentrations of breviscapine in plasma and lymph were determined by HPLC.The pharmacokinetics of breviscapine after oral and intravenous administration was evaluated in the conscious rat model.It was observed that scutellarin distributed from blood circulation to lymphatic system after intravenous injection.The cumulative lymphatic transport amount within 12 h was（2.78 ± 0.25） μg,equivalent to 0.079 2% of intravenous dose.After oral administration of scutellarin to double-cannulation rats,the cumulative lymphatic transport amount within 12 h was（0.92 ± 0.08） μg,equal to 0.008 3% of oral dose.The absolute bioavailability of breviscapine orally administered to double-cannulation rats was 4.91%,indicating that scutellarin was mainly absorbed into the bloodstream through the portal vein.Lymphatic transport of scutellarin appears to reflect high affinity for the lymph lipoproteins to chylomicron.This study provided a biopharmaceutics basis for developing oral lipid delivery system for the promotion of intestinal lymphatic transport to improve oral bioavailability of breviscapine.

关 键 词：灯盏花素 淋巴转运 生物利用度 吸收 

分 类 号：R943[医药卫生—药剂学]