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人参皂苷Rd口服吸收及其体内药代动力学的研究

Study on absorption and pharmacokinetic behavior of ginsenoside Rd

中文摘要英文摘要

目的 建立检测小鼠血浆样品中人参皂苷Rd的分析方法,考察人参皂苷Rd的口服生物利用度及小鼠灌胃给药后Rd在各肠段内的滞留时间,探讨其治疗溃疡性结肠炎的药动学特征。方法 正常小鼠静脉及灌胃给药后测定血药浓度;灌胃给药后在不同时间分别取十二指肠、空肠、回肠及结肠内容物,采用HPLC法测定各肠段内容物中的药物浓度。结果 实验表明小鼠灌胃给药后,血浆中检测不到药物;给药1h后Rd在小肠的药物含量为给药量的24.0±2.3%,2h后,空肠中的药物大部分转移到回肠,空肠中的药物含量下降到仅为给药量的5.0±1.0%,回肠的药量增加为给药量的23.0±6.0%。灌胃给药5h后,结肠内的药物含量占给药量的8.0±4.4%,6h后,小肠的药物浓度已接近检测限,相反,结肠中检测到药物含量占给药量的19.8±13.7%,10h结肠内检测不到药物。结论 本方法操作简单、专属性强、灵敏度高、准确性好,可用于人参皂苷Rd的体内药物测定。小鼠口服人参皂苷Rd后药物不吸收,大量聚集在结肠部位,这是人参皂苷Rd治疗溃疡性结肠炎的药动学基础。

im To develop a HPLC method for the determination of ginsenoside Rd in mice plasma ,and to study the oral bioavailability of ginsenoside Rd and the time course of Rd contents in the digestive tract after oral administration, and to investigate the characteristics of pharmacokinetic behavior of ginsenoside Rd in the treatment of ulcerative colitis. Methods After intravenous administration and oral administration, the concentrations of drug in mice blood were recorded; such samples as duodenum ,jejunum, ileum and colon included their contents at different time points after oral administration were taken out and analyzed by HPLC. Results It showed that Rd in plasma were not detected after oral administration. The amount of Rd in the small intestine 1 hour after administration were 24.0±2.3% of the dose. Two hours later ,when most of the Rd in the jejunum transferred into the ileum ,the amount of Rd in the jejunum decreased to only 5.0±1.0% of the dose and that in the ileum increased largely to 23.0±6.0% of the dose. Then, that in the colon 5 hours later was as high as 8.0±4.4% of the dose, 6 hours later ,that in the small intestine was near the limit of detection and , on the contrary , 19.8±13.7% of the dose was found in the colon. Ten hours later ,ginsenoside Rd was not detected in the colon. Conclusion The method was sensitive, accurate, rapid and can be applied to determine the ginsenoside Rd in plasma. Most of the Rd was found in the colon after oral administration, it is the pharmcokinetic basis of ginsenoside Rd in the treatment of ulcerative colitis.

刘霞、闫帅、吴勇杰、程军军、高明堂

药学基础医学中医学

人参皂苷Rd血药浓度结肠药物浓度

ginsenoside Rdplasma concentrationintestinalconcentrations of drug in the colon

刘霞,闫帅,吴勇杰,程军军,高明堂.人参皂苷Rd口服吸收及其体内药代动力学的研究[EB/OL].(2011-02-18)[2025-08-02].http://www.paper.edu.cn/releasepaper/content/201102-249.点此复制

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