聚卡波非钙抑制环丙沙星吸收的体内及体外实验研究

Inhibition of ciprofloxacin absorption by calcium polycarbophil:in vivo and in vitro experimental studies

【目的】研究聚卡波非钙对广谱抗生素环丙沙星吸收的影响。【方法】采用体外溶出试验,观察金属阳离子存在对环丙沙星从纤维素膜中释放的影响;选用SD大鼠16只,分为对照组和实验组,每组8只,对照组经口服给予环丙沙星20 mg/kg,实验组经口服同时给予环丙沙星20 mg/kg和聚卡波非钙64 mg/kg,采用高效液相色谱法测定血浆和血清中环丙沙星的浓度。【结果】纤维素膜中存在铝、钙或铁离子时环丙沙星的释放速度会明显减慢(P<0.05);实验组环丙沙星的AUC0-4和Cmax均低于对照组,差异均有统计学意义(P<0.05);两组大鼠血药浓度达峰时间tmax差异无统计学意义,实验组大鼠AUC0-4比对照组低60%,且实验组Cmax明显低于对照组(P<0.05)。【结论】环丙沙星与聚卡波非钙同时使用时会降低环丙沙星的吸收,因此应避免两者同时使用。

【Objective】To study the effect of calcium polycarbophil on the absorption of broad-spectrum antibiotic ciprofloxacin.【Methods】The effects of metal cations on the release of ciprofloxacin from cellulose membranes were observed by in vitro dissolution test.A total of 16 SD rats were selected and divided into the control group and experimental group（n=8）.The rats in the control group were orally administered ciprofloxacin 20 mg/kg,and those in the experimental group were treated by oral administration of ciprofloxacin20 mg/kg and polycaprolte calcium 64 mg/kg.The plasma and serum concentrations of ciprofloxacin were determined by highperformance liquid chromatography.【Results】The release of ciprofloxacin was significantly decreased in the presence of aluminum,calcium or iron ions in the cellulose membrane（P〈0.05）.The AUC0-4 and Cmax of ciprofloxacin in the experimental group were lower than those in the control group,and the difference was statistically significant（P〈0.05）.There was no significant difference in the tmax of plasma concentration between the two groups.The area under the curve（AUC0-4） in the experimental group was 60% lower than that in the control group,and the Cmax in the experimental group was significantly lower than that in the control group（P〈0.05）.【Conclusion】The coadministration of ciprofloxacin and calcium polycarbophil can reduce the absorption of ciprofloxacin.Therefore,the coadministration should be avoided.