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目的:研究灌胃给予不同纯度吴茱萸提取物后大鼠体内吴茱萸次碱(Rut)和吴茱萸碱(Evo)的药动学特点。方法:以Rut、Evo分别为40、31mg·kg-1的剂量,灌胃给予雌性大鼠高、中、低不同纯度(Rut:45%、28%、9%,Evo:35%、21%、7%)的吴茱萸提取物混悬液(n=6),分别于灌胃后0·25、0·5、0·75、1·0、1·5、2·0、2·5、3·0、4·0h眼底静脉丛采血0·5mL,高效液相色谱法测定血样中Rut和Evo含量,并计算药动学参数cmax、tmax和AUC0～4h。结果:高、中、低纯度组中,cmax:Rut:(215·3±80·4)、(94·5±28·8)、(22·8±4·4)ng·mL-1,Evo:(164·8±65·1)、(78·8±23·5)、(43·4±17·2)ng·mL-1(两两比较P<0·01);tmax:Rut:(0·5±0·0)、(0·6±0·1)、(0·5±0·0)h,Evo:(0·5±0·2)、(0·7±0·2)、(0·5±0·0)h;AUC0～4h:Rut:(117·1±26·5)、(117·4±42·2)、(36·8±5·6)ng·h·mL-1,Evo:(148·9±39·1)、(122·2±23·3)、(80·4±14·3)ng·h·mL-1。3种纯度组中Rut和Evo的cmax具有统计学差异,AUC0～4h随纯度的升高而增加(P<0·01)。结论:吴茱萸提取物的纯度与Rut和Evo的吸收明显有关,在纯度为16%～80%(以二者总含量计)范围内,随着纯度的提高,二者生物利用度均明显增加。
Objective: To study pharmacokinetics of rut and evodiamine in rats after intragastric administration of Evodia rutaecarpa extract. Methods: Rut and Evo were administrated in different doses (Rut: 45%, 28%, 9%, Evo: 35%, 21% , 7%) of Evodia extract suspension (n = 6), respectively, after gavage 0.25, 0.5, The retinal venous plexus blood samples were collected for 0.5 and 4.0 mL at 3 and 0.4 h, respectively. The contents of Rut and Evo were determined by HPLC. The pharmacokinetic parameters (cmax, tmax and AUC0 ~ 4 h) were calculated. RESULTS: The cmax: Rut: (215.3 ± 80.4), (94.5 ± 28.8), (22.8 ± 4.4) ng · mL-1, Evo: (164.8 ± 65.1), (78.8 ± 23.5), (43.4 ± 17.2) ng · mL-1 (pairwise comparisons, P <0.01); tmax: Rut (0 · 5 ± 0 · 0), (0 · 6 ± 0 · 1), (0 · 5 ± 0 · 0) h, Evo: AUC0 ~ 4h: Rut: (117.1 ± 26.5), (117.4 ± 42.2), (36.8 ± 5.6) ng · h · mL-1, Evo: (148.9 ± 39.1), (122.2 ± 23.3), (80.4 ± 14.3) ng · h · mL-1.3 purity The cmax of Rut and Evo in the group was statistically different. The AUC0-4h increased with the increase of the purity (P <0.01). CONCLUSION: The purity of Evodia rutaecarpa extract is obviously related to the absorption of Rut and Evo. The purity of Evodia rutaecarpa extract increased significantly with the increase of purity in the range of 16% -80% (total content of both).