关键词: 伊马替尼, N-去甲基伊马替尼, 复方丹参片, 复方丹参滴丸

Abstract: OBJECTIVE： This study aimed to investigate effect of Danshen (Salvia miltiorrhiza) preparation on blood concentration of imatinib and N-desmethyl imatinib in rats. METHODS： Healthy male SD rats were randomly divided into three groups of 10 per group：control，Danshen tablet of 486 mg/kg and Danshen dripping pill of 72.9 mg/kg. All three groups were given imatinib at 30 mg/kg. Each group was given by intragastric administration for 14 consecutive days. Plasma samples were collected on day 1 and day 14. Blood concentrations of imatinib and N-desmethyl imatinib were determined by ultra-performance liquid chromatography-mass spectrometry (HPLC-MS/MS). Calculation of pharmacokinetic parameters of imatinib and N-desmethyl imatinib using DAS 2.0 software. RESULTS： On the 1st day after administration，the area under the concentration-time curve (AUC_0-∞) of imatinib in the compound Danshen tablet group was reduced by 19.00% (P<0.05) compared with the control group. On the 14th day after administration，the AUC_0-24 and peak concentration (Cmax) of imatinib in the compound Danshen tablet group were reduced by 19.45% and 17.84%， respectively (P<0.05). The AUC_0-24 and AUC_0-∞ of N-desmethylimatinib were reduced by 29.87% and 35.27%， respectively (P<0.05). On the 1st and 14th days after administration，there were no significant differences in the pharmacokinetic parameters of imatinib and N-desmethylimatinib between the compound Danshen dripping pill group and the control group (P>0.05). CONCLUSION： Compound Danshen tablets affected the plasma concentrations of imatinib in rats while compound Danshen dripping pills had no significant effect on the concentrations of imatinib and N-desmethylimatinib in rat plasma.

Key words: imatinib, N-desmethyl imatinib, compound Danshen tablet, compound Danshen drip pill