贝母提取物中贝母甲素和贝母乙素的大鼠肠吸收特性  

Rat intestinal absorption trait of peimine and peiminine in Thunberg Fritillary Bulb extract

作　　者：关志宇[1] 张丽华[1] 陈丽华[1] 朱卫丰[1] 刘红宁[1] 

机构地区：[1]江西中医药大学,江西南昌330004

出　　处：《药学学报》2013年第12期1836-1843,共8页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81060346)

摘　　要：本文考察了浙贝母醇提浸膏中贝母甲素和贝母乙素的肠吸收特征以及配伍影响。建立了HPLC-ELSD测定肠灌流液中贝母甲素和贝母乙素含量测定的方法,并进行了方法学研究。采用大鼠在体单向灌流法,重量法校正实验结果,分别考察灌流速度、灌流液pH、性别差异、胆总管结扎、药物浓度、不同肠段、维拉帕米和配伍苦杏仁、甘草对贝母甲素、乙素肠吸收的影响。结果表明:灌流速度、灌流液pH和浓度可影响贝母甲素和贝母乙素吸收,pH 6.8和pH 7.4时吸收有显著差异(P<0.01);灌流液中药物浓度升高,贝母甲素和贝母乙素的肠吸收参数呈下降趋势,低浓度和中、高浓度间吸收速度常数(Ka)和表观渗透系数(Papp)有显著性差异(P<0.01);贝母甲素和贝母乙素在雌鼠肠道中的吸收显著低于雄鼠(P<0.01);胆管结扎可显著影响贝母甲素和贝母乙素的吸收(P<0.05),贝母甲素和贝母乙素在各个肠段均有一定吸收,且无显著性差异(P>0.05);加入维拉帕米对浸膏中贝母甲素和贝母乙素的吸收无显著性影响(P>0.05);苦杏仁和甘草与贝母在常用配伍剂量下皆能显著降低贝母甲素和贝母乙素的肠吸收(P<0.01),药材单煎后组合与合煎两组间二者吸收无显著性差异(P>0.05)。实验结果说明,贝母甲素和贝母乙素的体内吸收特征基本一致,二者在整个肠道均有一定吸收,并具有显著的性别差异,吸收机制可能有主动吸收或易化扩散参与;配伍苦杏仁、甘草可降低其肠吸收速度。To study the in situ intestinal absorption kinetics and compatibility influence of peimine and peiminine in rats, the absorption of peimine and peiminine in small intestine （duodenum, jejunum and ileum） and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC-ELSD. Perfusion rate, pH, concentration of drug, gender and bile duct ligation can significantly affect the absorption of peimine and peiminine, the Ka and Papv values in the condition of pH 6.8 and pH 7.4 had significant difference （P〈 0.01）, as drug concentration increased, the absorption parameters of peimine and peiminine decreased, between low concentrations and middle concentrations was significant difference （P〈0.01）. Verapamil can not affect Ka and Papp of peimine and peiminine which are in the extract （P〉 0.05）. Bitter almonds and licorice can significantly reduce the absorption of peimine and peiminine with the usual dose （P〈0.01）, extracted separately and together had no significant difference on Ka and Papp （P〉 0.05）. Experimental results show that the absorption features of peimine and peiminine are basicallythe same, both of them could be absorbed at all segments of the intestine in rats and had no special absorption window, and with significant differences between male and female individuals. The absorption of peimine and peiminine complies with the active transport and facilitated diffusion in the general intestinal segments. Bitter almond and licorice can reduce the intestinal absorption rate of peimine and peiminine.

关 键 词：贝母甲素 贝母乙素 小肠吸收 单向灌流法 重量法 

分 类 号：R943[医药卫生—药剂学]