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目的 考察大鼠体内灯盏乙素对瑞舒伐他汀血浆浓度和组织分布的影响.方法 按照体重将大鼠随机分成4组,每组18只:对照组、实验Ⅰ组、实验Ⅱ组和实验Ⅲ组.实验Ⅰ组、实验Ⅱ组和实验Ⅲ组分别灌胃10,50,200 mg·kg-1灯盏乙素,同时均灌胃瑞舒伐他汀5 mg·kg-1;对照组灌胃等体积0.2％CMC-Na水溶液.分别于给药后1,2,6h摘眼球取血,取血后立即处死大鼠,取出心、肝、肺、肾、脑组织处理,HPLC-MS测定血浆及组织的瑞舒伐他汀含量.结果 所建立的瑞舒伐他汀血浆及组织样本HPLC-MS法符合要求.对照组、实验Ⅰ组、实验Ⅱ组和实验Ⅲ组大鼠的血浆瑞舒伐他汀浓度在1h分别为(170.38±40.77),(218.09±59.52),(278.64±76.26),(297.48±95.37)ng·mL-1;在2 h分别为(237.26±70.31),(293.76±89.04),(410.27±102.13),(461.49±121.73) ng·mL-1;在6 h分别为(131.58±40.52),(166.21±48.52),(236.78±73.40)和(251.33±82.94)ng·mL-1,各实验组大鼠瑞舒伐他汀血浆浓度高于对照组,差异均有统计学意义(均P ＜0.05).各组大鼠的瑞舒伐他汀均主要聚集于肝,对照组、实验Ⅰ组、实验Ⅱ组和实验Ⅲ组在大鼠肝的瑞舒伐他汀浓度在1 h分别为(2098.57±735.10),(1905.91 ± 703.16),(1406.39 ± 435.86),(1217.08±318.65)ng·mL-1;这4组在2h分别为(3204.19±893.53),(2863.87±836.12),(2114.28±598.31),(1973.15±512.64) ng· mL-1;这4组在6h分别为(1681.71±513.29),(1603.14±517.86),(1120.08±298.75),(1057.91±267.66) ng·mL-1,实验Ⅱ组和实验Ⅲ组在肝的瑞舒伐他汀浓度低于对照组;实验组Ⅲ组的瑞舒伐他汀在大鼠的心、肺、肾及脑组织的浓度高于对照组,以上差异均有统计学意义(均P ＜0.05).结论 剂量达到50 mg·kg-1的灯盏乙素对瑞舒伐他汀血浆浓度及肝组织分布均有显著影响,其分布机制可能与竞争蛋白转运体有关.“,”Objective To study the influence of scutellarin on the plasma concentration and tissue distributions of rosuvastatin in rats.Methods Male sprague-dawley rats were randomly divided into four groups:control group,experimental Ⅰ group,experimental Ⅱ group and experimental Ⅲ group.All rats were orally administrated with rosuvastatin (5 mg· kg-1).In low,medium,largethree doses (10,50,150 mg · kg-1 scutellarin) of experimental groups,scutellarin were added,respectively.Plasma samples were collected by picking eyeballs 1,2,6 h after administration.Then the rats were sacrificed and heart,liver,kidney,lung and brain were collected.The concentration of rosuvastatin in plasma and tissues were detected by HPLC-MS.Results The estabhshed HPLC-MS analyse method is in line with the requirements of this study.Concentrations of rosuvastatin in plasma at different time points were as follows:at 1 h it were (170.38 ± 40.77),(218.09 ± 59.52),(278.64 ± 76.26),(297.48 ± 95.37)ng.mL-1;at 2 h it were (237.26 ±70.31),(293.76 ±89.04),(410.27 ± 102.13),(461.49 ± 121.73)ng · mL-1;at 6 h it were (131.58 ±40.52),(166.21 ±48.52),(236.78 ±73.40),(251.33 ± 82.94) ng · mL-1.The concentration of rosuvastatin in experimental of rats plasma is higher than that of control group with significantly (all P ＜ 0.05).The rosuvastatin is mainly accumulated in the liver of the rats.Concentrations of rosuvastatin in liver at different time points were as follows:at 1 h it were (2098.57 ± 735.10),(1905.91 ± 703.16),(1406.39 ± 435.86),(1217.08 ± 318.65) ng · mL-1;at 2 h it were (3204.19 ± 893.53),(2863.87 ± 836.12),(2114.28 ± 598.31),(1973.15 ± 512.64) ng· mL-1;at 6 h it were (1681.71 ± 513.29),(1603.14 ± 517.86),(1120.08 ± 298.75),(1057.91 ± 267.66) ng · mL-1.In liver tissue,the concentration of rosuvastatin in experimental group H and Ⅲ were lower than that of the control group with significantly (all P ＜ 0.05).The concentration of rosuvastatin in heart,lung and kidney and brain tissue increased in experimental Ⅲ group;compared to that of the control group,the difference had significant difference (all P ＜ 0.05).Conclusion A specific concentration range of scutellarin can affect the plasma concentration and tissue distributions of rosuvastatin while rats were administrated with 5 mg · kg-1 of rosuvastatin.The concentration of rosuvastatin in liver under combined administration model was decreased,especially.This may be related to the competitive protein transporter.