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目的评价中药成分大黄素对大鼠灌服环孢素A(CsA)的药代动力学。方法 60只雄性SD大鼠按体重进行随机分为5组,分别灌服CsA+60 mg.kg-1高剂量蒸馏水;CsA+30 mg.kg-1低剂量酮康唑;CsA+大黄素(60 mg.kg-1);CsA+大黄素(30 mg.kg-1);1～3 d大黄素,第4 d灌服CsA+大黄素。用HPLC-MS法测定全血中CsA的浓度,kinetica软件计算主要药代动力学参数,用SPSS17.00进行统计学分析。结果阳性对照组与空白对照组药代动力学参数除吸收速率外均有显著性差异;高剂量大黄素组使其较快达到峰浓度(P<0.05);低剂量大黄素组药代动力学参数与空白对照组比较无显著性差异;服用3 d大黄素后,最后1 d灌服CsA+大黄素组的吸收速率和峰浓度与空白对照组比较有显著性差异(P<0.05)。结论大黄素对CsA的生物利用度和代谢无明显影响。
Objective To evaluate the pharmacokinetics of Chinese traditional medicine Emodin on rats by cyclosporin A (CsA). Methods Sixty male Sprague-Dawley rats were randomly divided into 5 groups according to their body weights. The rats were given CsA + 60 mg.kg-1 high-dose distilled water, CsA + 30 mg.kg-1 low dose ketoconazole, CsA + emodin mg.kg-1), CsA + emodin (30 mg.kg-1), emodin for 1-3 days and CsA + emodin on the 4th day. The concentration of CsA in whole blood was determined by HPLC-MS. The main pharmacokinetic parameters were calculated by kinetica software and analyzed by SPSS 17.00. Results The pharmacokinetic parameters of the positive control group and the blank control group were significantly different except the absorption rate; the high-dose emodin group reached the peak concentration (P <0.05); the pharmacokinetics of the low-dose emodin group There was no significant difference between the control group and the blank control group. After 3 days of emodin treatment, the absorption rate and peak concentration of CsA + emodin group were significantly different from those of the blank control group (P <0.05). Conclusion Emodin has no obvious effect on the bioavailability and metabolism of CsA.