论文部分内容阅读
高效液相色谱法测定小檗碱(BBR)和8-十六烷基小檗碱(8-BBR-C16)在大鼠血浆及组织中的浓度,比较二者的药代动力学规律和组织分布差异,为8-BBR-C16的机制研究及药物开发提供实验数据。大鼠灌胃80mg·kg-1药物后,在药动学实验结果中,与BBR相比,8-BBR-C16的Cmax、AUC0-t分别是BBR的2.8倍和12.9倍,tl/2由3.61 h延长到11.90 h。在组织分布实验结果中,与BBR相比,8-BBR-C16在各种组织的分布浓度均有显著提高,停滞时间明显延长。其在肺中的药物浓度最高,最高浓度达到3 731.82 ng·g-1。8-BBR-C16经衍生化后,在血浆中Cmax及生物利用度显著提高,体内循环时间延长,组织中的药物分布浓度显著提高,分布比例改变,具有较强的肺靶向性。
The concentrations of berberine (BBR) and 8-cetylbermazine (8-BBR-C16) in rat plasma and tissues were determined by HPLC. The pharmacokinetics and tissue Distribution differences, provide experimental data for 8-BBR-C16 mechanism research and drug development. Compared with BBR, the Cmax and AUC0-t of 8-BBR-C16 were 2.8 times and 12.9 times that of BBR respectively after rats were orally administered with 80 mg · kg -1 of drug, and the ratio of t / 3.61 h extended to 11.90 h. Compared with BBR, the distribution of 8-BBR-C16 in all tissues showed a significant increase in tissue distribution test results, and the stagnation time was significantly prolonged. The highest concentration of the drug in the lung, the highest concentration of 3 731.82 ng · g-1.8-BBR-C16 after derivatization, in the plasma Cmax and bioavailability was significantly increased in vivo circulation time, the drug in the tissue Distribution of concentration increased significantly, the proportion of distribution changes, with strong lung targeting.