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目的:探讨芦丁与槲皮素不同配比对大鼠体内芦丁药动学的影响。方法:将30只大鼠随机分为芦丁组(芦丁-槲皮素物质的量之比为4 ∶ 0,下同)、槲皮素组(芦丁-槲皮素=0 ∶ 4)、BL1组(芦丁-槲皮素=3 ∶ 1)、BL2组(芦丁-槲皮素=2 ∶ 2)、BL3组(芦丁-槲皮素=1 ∶ 3),每组6只,各组大鼠ig给药10 mg/kg(以芦丁和槲皮素中槲皮素母核计)。分别于给药前及给药后0.25、0.5、0.75、1、1.5、2、3、4、6、8、10、12、16、20、24 h 后尾静脉取血0.3 mL,处理后采用高效液相色谱法测定血浆中槲皮素(芦丁代谢产物)的血药浓度,采用DAS 2.0药动学软件计算药动学参数。结果:芦丁、槲皮素、BL1、BL2、BL3组大鼠AUC0-24 h分别为(4.908±0.877)、(8.382±3.671)、(8.473±0.709)、(4.366±2.297)、(8.914±2.642) μg·h/L,MRT0-24 h分别为(9.675±1.359)、(3.142±0.489)、(3.517±1.128)、(3.376±1.046)、(4.494±1.653) h,tmax分别为(5.726±5.645)、(1.375±0.703)、(1.125±1.438)、(1.417±2.300)、(1.292±0.954) h,cmax分别为(0.609±0.202)、(2.341±0.539)、(2.425±1.217)、(1.464±0.677)、(3.325±2.425) μg/L。与芦丁组比较,槲皮素、BL1、BL3组大鼠AUC0-24 h、cmax显著升高(P<0.05),tmax、MRT0-24 h显著降低(P<0.05);BL2组大鼠cmax显著升高(P<0.05),tmax、MRT0-24 h显著降低(P<0.05)。与槲皮素组比较,除BL2组大鼠AUC0-24 h显著降低外(P<0.05),BL1、BL2、BL3组大鼠AUC0-24 h、MRT0-24 h、tmax、cmax差异均无统计学意义(P>0.05)。结论:槲皮素可提高芦丁在大鼠体内的相关指标。
OBJECTIVE: To explore the effects of the different compatibility ratios of rutin with quercetin on the pharmacokinetics of rutin in rats in vivo. METHODS: 30 rats were randomly divided into rutin group (rutin-quercetin molar ratio of 4 ∶ 0, the same below), quercetin group (rutin-quercetin ratio of 0 ∶ 4), BL1 group (rutin-quercetin ratio of 3 ∶ 1), BL2 group (rutin-quercetin ratio of 2 ∶ 2) and BL3 group (rutin-quercetin ratio of 1 ∶ 3), 6 rats in each group, all group was administrated 10 mg/kg (calculated by quercetin core of rutin and quercetin) intragastrically. The blood sample 0.3 mL was respectively taken from tail vein after 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 20, 24 h of administration, the plasma concentration of quercetin (rutin metabolite) was determined by HPLC. DAS 2.0 software was used to calculate the pharmacokinetic parameters. RESULTS: The AUC0-24 h in rutin group, quercetin group, BL1 group, BL2 group and BL3 group were (4.908±0.877), (8.382±3.671), (8.473±0.709), (4.366±2.297), (8.914±2.642) μg·h/L; MRT0-24 h were (9.675±1.359), (3.142±0.489), (3.517±1.128), (3.376±1.046), (4.494±1.653) h; tmax were (5.726±5.645), (1.375±0.703), (1.125±1.438), (1.417±2.300), (1.292±0.954) h; and cmax were (0.609±0.202), (2.341±0.539), (2.425±1.217), (1.464±0.677), (3.325±2.425) μg/L. Compared with rutin group, AUC0-24 h and cmax in quercetin group, BL1 group and BL3 group were significantly increased (P<0.05), tmax and MRT0-24 h were significantly decreased (P<0.05); cmax in BL2 group was significantly increased (P<0.05), tmax and MRT0-24 h were significantly decreased (P<0.05). Compared with quercetin group, except AUC0-24 h was significantly decreased in BL2 group (P<0.05), there were no significant differences in AUC0-24 h, MRT0-24 h, tmax or cmax in BL1 group, BL2 group and BL3 group (P>0.05). CONCLUSIONS: Quercetin can inhance the related indexes of rutin in rats in vivo.
芦丁槲皮素配比生物利用度大鼠药动学
RutinQuercetinCompatibility ratiobioavailabilityRatsPharmacokinetic
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