中文摘要：

为了研究冰片对磷酸川芎嗪的肠吸收以及考察冰片对大鼠灌胃磷酸川芎嗪后药代动力学的影响，初步探讨冰片促吸收的机制，本文采用在体肠循环实验研究不同浓度的冰片对磷酸川芎嗪在十二指肠、空肠、回肠及结肠等4个肠段吸收的影响。通过大鼠分别灌胃磷酸川芎嗪、磷酸川芎嗪与冰片的混合物及磷酸川芎嗪与维拉帕米的混合物，采用高效液相色谱法测定不同时间血浆中磷酸川芎嗪的浓度，比较3组整体动物实验的药代动力学参数。结果表明磷酸川芎嗪在4个肠段的单位面积吸收量顺序为：结肠〉十二指肠〉空肠〉回肠，且随药物浓度的增大各个肠段的单位面积吸收量均没有吸收饱和现象，推断磷酸川芎嗪在大鼠肠道以被动扩散方式吸收。加入冰片后，磷酸川芎嗪在4个肠道的单位面积吸收量均增加。冰片质量浓度为10μg·mL^-1时，与对照组相比，无显著性差异（P〉0．05）；而冰片质量浓度为25和50μg·mL^-1时，与对照组相比，均具有显著性差异（P〈0．05），可见冰片对磷酸川芎嗪的促吸收无明显的靶部位，但其发挥促吸收作用需要一定的浓度。整体动物实验结果表明，冰片和维拉帕米均提高了磷酸川芎嗪的生物利用度，冰片促进磷酸川芎嗪生物利用度增加的机制之一可能是由于抑制了肠上皮细胞CYP3A代谢和P—gP的外排作用。

英文摘要：

To explore the mechanism of the absorption enhancement of borneol, the effect of borneol on the intestinal absorption and the pharmacokinetics of tetramethylpyrazine phosphate after oral administration were investigated. In situ intestinal recirculation was performed to study the effect of various concentrations of borneol on the absorption of tetramethylpyrazine phosphate at duodenum, jejunum, ileum and colon. After oral administration of tetramethylpyrazine phosphate, the mixture of tetramethylpyrazine phosphate and borneol and the mixture of tetramethylpyrazine phosphate and verapamil in rats, the concentrations of tetramethylpyrazine phosphate in plasma were determined by RP-HPLC at predesigned time. The pharmacokinetic parameters were compared based on the results of the three animal experiments, and analyzed with software program 3p97. The result showed that tetramethylpyrazine phosphate could be absorbed at all of the four intestinal segments with increasing absorption amount per unit as follows： colon 〉 duodenum 〉 jejunum 〉 ileum, but without saturation, which demonstrated that tetramethylpyrazine phosphate was absorbed via simple diffusion. Borneol could enhance the intestinal absorption of tetramethylpyrazine phosphate, however, not in proportion. There was no obvious difference between the test group and the control group when 10 μg·mL^-1 borneol was added （P 〉 0.05）,while when the concentration comes to 25 μg·mL^-1 and 50 μg·mL^-1, significant differences were observed （P 〈 0.05）. Borneol and verapamil did enhance the bioavailability of tetramethylpyrazine phosphate after oral administration in rats. The enhancing effect of borneol showed only when the concentration came to a certain level but with no specific sites existed in the intestine. One of the mechanisms of borneol on the enhancing effect on absorption of tetramethylpyrazine phosphate might be the inhibition of the metabolism of CYP 3A and exocytosis of P-gp.