中国中药杂志

2018, v.43(22) 4528-4533

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体内外实验探究五倍子中鞣质类成分对利福平药代动力学的影响
Effects of tannins in Galla Chinensis on pharmacokinetics of rifampicin in vivo and in vitro

王强;董姊怡;叶嘉超;程婧;唐涵;王铭爽;刘彦玲;金锐;黄建梅;
WANG Qiang;DONG Zi-yi;YE Jia-chao;CHEN Jing;TANG Han;WANG Ming-shuang;LIU Yan-ling;JIN Rui;HUANG Jian-mei;School of Chinese Materia Medica,Beijing University of Chinese Medicine;Department of Pharmacy,Beijing Shijitan Hospital,Capital Medical University;

摘要(Abstract):

该实验探究五倍子中鞣质类成分对利福平体内过程的影响。体外实验分别采用紫外分光光度法和HPLC,考察利福平在p H 1. 3,6. 8,人工胃液环境和人工肠液环境中的溶解性以及在上述环境加入五倍子鞣质对利福平溶解性的影响。体内实验研究大鼠分别灌胃利福平以及利福平和五倍子鞣质后利福平在大鼠体内过程并计算药代动力学参数。结果显示,利福平在人工胃液环境中随时间不断析出,6 h后近85%利福平已析出。在人工肠液环境中溶解性良好。加入五倍子鞣质后,利福平在2种环境中的浓度均有较显著下降,且在人工肠液中,利福平的浓度保持在相对平稳的水平;在人工胃液中则保持原来的下降趋势。药代动力学参数显示,与单用利福平组相比,利福平与五倍子鞣质合用组的AUC0-t和Cmax显著降低,MRT0-t显著变慢,Tmax增加1倍,生物利用度为31. 65%。实验提示,利福平在酸性环境溶解性差;利福平与鞣质合用后生物利用度下降的重要原因是利福平与鞣质的络合减小利福平在肠道的溶解度,从而影响其在肠道的吸收。所以,利福平与含鞣质丰富的中药汤剂或中成药,不宜同时服用。
This study was aimed to explore the effects of tannins in Galla Chinensis on rifampicin in vivo. In the experiment in vitro,UV spectrophotometry and high performance liquid chromatography(HPLC) were used to investigate the solubility of rifampin in p H 1. 3,6. 8,artificial gastric juice environment and artificial intestinal fluid environment as well as the effects of tannins on solubility of rifampin in the above conditions. In the experiment in vivo,the process of rifampicin was studied after intragastric administration of rifampicin and rifampicin + tannins in Galla Chinensis,and then the pharmacokinetic parameters were calculated. The results showed that rifampicin was constantly precipitated in the artificial gastric juice environment over time,and nearly 85% of the rifampicin was precipitated after 6 hours; it showed a good solubility in the artificial intestinal juice environment. After adding the said tannins,the concentration of rifampicin was decreased significantly in both environments,and the concentration of rifampicin in artificial intestinal juice remained relatively stable,while that in artificial gastric juice remained the original downward trend. The pharmacokinetic parameters displayed that as compared with rifampicin alone,AUC0-tand Cmaxwere decreased significantly,MRT0-tslowed down significantly,Tmaxdoubled to 7. 0 h and the bioavailability was only 31. 65% in rifampicin + tannins in Galla Chinensis group. The experiment indicated rifampicin had a poor solubility in acidic environment and the decrease of bioavailability of rifampicin when in combination with tannin was mainly due to the reduction of rifampicin solubility in intestinal tract by complexation of rifampicin with tannin,thus affecting its absorption in intestinal tract. Therefore,rifampicin and the Chinese herbal medicines or Chinese patent medicines rich in tannin should not be taken simultaneously.

关键词(KeyWords): 利福平;鞣质;溶解性;药代动力学;中西药相互作用
rifampicin;tannin;solubility rate of gastrointestinal tract;pharmacokinetics;herb-drug interaction

Abstract:

Keywords:

基金项目(Foundation): 北京中医药科技发展资金项目(QN2016-04)

作者(Authors): 王强;董姊怡;叶嘉超;程婧;唐涵;王铭爽;刘彦玲;金锐;黄建梅;
WANG Qiang;DONG Zi-yi;YE Jia-chao;CHEN Jing;TANG Han;WANG Ming-shuang;LIU Yan-ling;JIN Rui;HUANG Jian-mei;School of Chinese Materia Medica,Beijing University of Chinese Medicine;Department of Pharmacy,Beijing Shijitan Hospital,Capital Medical University;

DOI: 10.19540/j.cnki.cjcmm.20180815.003

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