Li Yiqun, Cao Huiting, Liu Mengzhu, Zhang Benyong, Zhang Xinlong, Shi Donglei, Guo Liwei, Duan Jinao, Zhou Xueping, Zhu Huaxu, Zhang Qichun
Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, Nanjing, 210023 China.
Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing, 210023 China.
Chin Med. 2018 Jan 8;13:1. doi: 10.1186/s13020-017-0157-6. eCollection 2018.
Compatibility with (PN) reduced the plasma concentration of triptolide and delayed the T of (TW), the sovereign medicine of Qing-Luo Tong-Bi decoction, which hinted the absorption process of triptolide might be involved in decreasing the toxicity in liver and kidney.
The absorption of triptolide, triptonide, wilforlide and tripterine from monomer, TW, TW-PN, TW- (TW-CS) and Qing-Luo Tong-Bi were analyzed in duodenum, jejunum, ileum and colon of rat via single-pass intestinal perfusion model. An UPLC-MS/MS analysis method was developed to determine the concentration of triptolide, triptonide, wilforlide and tripterine in the inlet and outlet. Then P, 10 cm%ABS and K were calculated based on the perfusate flux, perfusate volume and candidate chemicals concentration.
The absorption of triptolide, triptonide, wilforlide and tripterine in duodenum, jejunum, ileum and colon was independent of concentration within range of 3-9 μg/mL. The target compounds, triptolide, triptonide, wilforlide and tripterine from the TW extract, showed higher absorption extent and rate than those administrated alone, and compared with the absorption situation of the chemicals of TW extract, the absorption of triptolide, triptonide and wilforlide of the extract of TW-PN, TW-CS and Qing-Luo Tong-Bi were decreased in these intestinal segments. However, PN-promoted tripterine absorption was observed in the intestine.
Modulation of absorption of chemicals in TW by subsidiary herbs may be responsible for reinforcing the actions and neutralizing the adverse effects through compatibility in the formula of Qing-Luo Tong-Bi. PN inhibits the absorption of triptolide of TW and promote the absorption of tripterine.
与(PN)配伍可降低雷公藤甲素的血浆浓度,并延迟清络通痹汤君药雷公藤(TW)的T,这提示雷公藤甲素的吸收过程可能参与降低肝肾毒性。
采用单通道肠灌注模型,分析雷公藤甲素、雷公藤酮、卫矛醇和雷公藤碱在大鼠十二指肠、空肠、回肠和结肠中从单体、TW、TW-PN、TW-(TW-CS)和清络通痹汤中的吸收情况。建立了超高效液相色谱-串联质谱(UPLC-MS/MS)分析方法,以测定进样口和出口处雷公藤甲素、雷公藤酮、卫矛醇和雷公藤碱的浓度。然后根据灌注液通量、灌注液体积和候选化学物质浓度计算P、10 cm%ABS和K。
在3-9μg/mL范围内,雷公藤甲素、雷公藤酮、卫矛醇和雷公藤碱在十二指肠、空肠、回肠和结肠中的吸收与浓度无关。TW提取物中的目标化合物雷公藤甲素、雷公藤酮、卫矛醇和雷公藤碱的吸收程度和速率高于单独给药时,并且与TW提取物中化学物质的吸收情况相比,TW-PN、TW-CS和清络通痹汤提取物中雷公藤甲素、雷公藤酮和卫矛醇在这些肠段的吸收降低。然而,在肠道中观察到PN促进了雷公藤碱的吸收。
佐药对TW中化学物质吸收的调节可能是清络通痹汤配方中通过配伍增强药效和中和不良反应的原因。PN抑制TW中雷公藤甲素的吸收并促进雷公藤碱的吸收。