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目的考察雷公藤甲素在大鼠肠道的吸收情况,为其安全合理应用提供生物药剂学依据。方法采用大鼠在体肠灌流实验,利用超高效液相色谱(UPLC)法测定雷公藤甲素的量,分别研究吸收部位和药物浓度对雷公藤甲素吸收的影响。结果4、8.3、20μmol/L雷公藤甲素灌流液在各肠段的有效渗透系数(Peff*)和10 cm肠段吸收百分比(10 cm%ABS)依次为十二指肠>结肠>空肠>回肠,各肠段之间无显著性差异(P>0.05)。不同质量浓度(4~20μmol/L)的雷公藤甲素在肠道内的吸收无显著性差异(P>0.05)。结论雷公藤甲素在大鼠肠道内有较好的肠吸收,对肠段无明显的吸收部位选择性,一定范围内的药物浓度对雷公藤甲素的Peff*和10 cm%ABS无影响,初步判断其吸收机制为被动扩散。
Objective To investigate the absorption of triptolide in the intestine of rats and to provide a biopharmaceutical basis for its safe and rational application. Methods Rat intestine perfusion experiments were performed. The content of triptolide was determined by UPLC. The effects of absorption site and drug concentration on the absorption of triptolide were studied. Results The effective permeation coefficient (Peff *) and 10 cm% absorption (10 cm% ABS) of 4, 8.3 and 20 μmol / L triptolide perfusate in each intestine were duodenum> colon> jejunum> Ileum, intestinal segments between no significant difference (P> 0.05). There was no significant difference in intestinal absorption of triptolide with different concentrations (4 ~ 20μmol / L) (P> 0.05). Conclusion Triptolide has good intestinal absorption in the intestine of rats and no obvious absorption site selectivity in the intestine. A certain range of drug concentration has no effect on Peff * and 10 cm% ABS of triptolide, Initially determine the absorption mechanism for passive diffusion.