Guan Zhi-Yu, Zhang Li-Hua, Chen Li-Hua, Zhu Wei-Feng, Liu Hong-Ning
Yao Xue Xue Bao. 2013 Dec;48(12):1836-43.
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 Papp values in the condition of pH 6.8 and pH 7.4 had significant difference (P<0.01), as drug concentration irlcreased, the absorption parameters of peimine and peiminine decreased, Ka and Papp 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 basically the 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 ofpeimine and peiminine.
为研究贝母碱和去氢贝母碱在大鼠体内的肠吸收动力学及配伍影响,采用原位单向灌流法考察贝母碱和去氢贝母碱在大鼠小肠(十二指肠、空肠和回肠)及结肠的吸收情况,并用高效液相色谱-蒸发光散射法测定药物含量。灌流速率、pH值、药物浓度、性别及胆管结扎均可显著影响贝母碱和去氢贝母碱的吸收,在pH 6.8和pH 7.4条件下的Ka和Papp值有显著差异(P<0.01),随着药物浓度增加,贝母碱和去氢贝母碱的吸收参数降低,低浓度与中浓度之间的Ka和Papp有显著差异(P<0.01)。维拉帕米不影响提取物中贝母碱和去氢贝母碱的Ka和Papp(P>0.05)。苦杏仁和甘草按常用剂量可显著降低贝母碱和去氢贝母碱的吸收(P<0.01),单独提取和一起提取对Ka和Papp无显著差异(P>0.05)。实验结果表明,贝母碱和去氢贝母碱的吸收特征基本相同,二者均可在大鼠肠道各段吸收,无特殊吸收窗,且雌雄个体间有显著差异。贝母碱和去氢贝母碱在肠道一般段的吸收符合主动转运和易化扩散。苦杏仁和甘草可降低贝母碱和去氢贝母碱的肠吸收速率。