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目的研究氨溴索对大鼠肺组织利福平浓度的影响。方法大鼠分为A、B两组,每组10只:A组单次静注利福平30 mg/kg;B组先静注氨溴索15 mg/kg,20 min后再静注利福平30 mg/kg。于利福平给药后于30 min、1、2、4 h四个时间点采集肺组织。利福平给药后11个不同时间点采集血样,用反相高效液相色谱(HPLC)法测定利福平浓度。比较两组间的血液及肺组织利福平浓度、主要药动学参数。结果利福平给药后1、2、4 h,B组肺组织利福平浓度均明显高于A组[(35.51±5.33)μg/ml v.s(31.82±4.77)μg/ml、(25.61±4.10)μg/ml vs.(15.21±2.58)μg/ml、(13.62±2.45)μg/ml vs.(6.24±1.18)μg/ml](P<0.01)。两组血药浓度及主要药代动力学参数无明显差异。结论氨溴索与利福平联合使用能显著增加肺组织利福平浓度;其作用机制不是通过对利福平血药浓度及其代谢的影响。
Objective To study the effect of ambroxol on the concentration of rifampicin in rat lung tissue. Methods The rats were divided into two groups A and B, 10 rats in each group: group A received a single intravenous injection of rifampin 30 mg / kg; Group B received intravenous ambroxol 15 mg / kg for 20 min followed by intravenous injection Fuping 30 mg / kg. After rifampicin administration, lung tissues were collected at four time points of 30 min, 1, 2 and 4 h. Blood samples were taken at 11 different time points after rifampicin administration, and rifampicin concentration was determined by reversed-phase high performance liquid chromatography (HPLC). The levels of rifampicin in blood and lung tissue were compared between the two groups and the main pharmacokinetic parameters were compared. Results The concentrations of rifampicin in group B were significantly higher than those in group A at 1, 2 and 4 h after rifampicin administration [(35.51 ± 5.33) μg / ml vs (31.82 ± 4.77) μg / ml, (25.61 ± 4.10 μg / ml vs. 15.21 ± 2.58 μg / ml, 13.62 ± 2.45 μg / ml vs. 6.24 ± 1.18 μg / ml] (P <0.01). There was no significant difference between the two groups in plasma concentration and the main pharmacokinetic parameters. Conclusions Combination of ambroxol and rifampicin can significantly increase the concentration of rifampicin in lung tissue. Its mechanism of action is not through the influence of rifampicin plasma concentration and metabolism.