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目的:研究雷公藤多苷片中活性成分雷公藤甲素在正常大鼠和佐剂性关节炎模型大鼠体内的药动学特征,为其临床合理用药提供参考。方法:将12只SD大鼠随机分为正常组和模型组,每组6只。模型组大鼠sc完全弗氏佐剂0.1 mL复制佐剂性关节炎模型,正常组大鼠sc等体积生理盐水。造模14 d后,两组大鼠均ig雷公藤多苷片混悬液96 mg/kg,分别于给药前及给药后10、30、45、60、90、120、150、180、240、300、420 min眼眶取血0.4 mL,采用高效液相色谱法测定雷公藤甲素的血药浓度;采用DAS 2.0药动学软件计算药动学参数,并进行比较。结果:雷公藤甲素在正常组、模型组大鼠体内的cmax分别为(1.139±0.114)、(0.916±0.103) μg/mL, tmax分别为(2.167±0.606)、(3.083±0.801) h, t1/2α分别为(5.500±3.610)、(5.593±1.795) h,AUC0-7 h分别为(5.052±0.371)、(4.707±0.347) μg·h/mL, MRT0-7 h分别为(3.224±0.119)、(3.429 ±0.139) h,CL分别为(11.616±2.986)、(11.246±2.638) mL/h。与正常组比较,模型组大鼠cmax显著减小,tmax和MRT0-7 h显著延长(P<0.05)。结论:佐剂性关节炎会影响大鼠体内雷公藤甲素的药动学特征,其可促进大鼠体内雷公藤甲素的吸收与消除。
OBJECTIVE: To study the pharmacokinetics of triptolide in Tripterygium glycosides tablet in normal rats and adjuvant arthritis model rats in vivo, and provide reference for clinical rational drug use. METHODS: 12 SD rats were randomly divided into normal group and model group, 6 in each group. Model group was subcutaneously injected complete Freund’s adjuvant 0.1 mL to induce adjuvant arthritis model, normal group was subcutaneously injected the same volume of saline. After 14 d modeling, 2 groups were given Tripterygium glycosides tablet suspension 96 mg/kg intragastrically, the blood sample of eyes 0.4 mL were respectively taken before and 10, 30, 45, 60, 90, 120, 150, 180, 240, 300, 420 min after administration. The plasma concentration of triptolide was determined by HPLC, the pharmacokinetic parameters were calculated by DAS 2.0 software, and the parameters were compared. RESULTS: The pharmacokinetic parameters of triptolide in normal group were cmax of (1.139±0.114) μg/mL, tmax of (2.167±0.606) h, t1/2α of (5.500±3.610) h, AUC0-7 h of (5.052±0.371) μg·h/mL, MRT0-7 h of (3.224±0.119) h, and CL of (11.616±2.986) mL/h; and those in model group were cmax of (0.916±0.103) μg/mL, tmax of (3.083±0.801) h, t1/2α of (5.593±1.795) h, AUC0-7 h of (4.707±0.347) μg·h/mL, MRT0-7 h of (3.429±0.139) h, and CL of (11.246±2.638) mL/h. Compared with normal group, cmax in model group was significantly decreased, tmax and MRT0-7 h were significantly prolonged (P<0.05). CONCLUSIONS: Adjuvant arthritis can affect the pharmacokinetics of triptolide in rats in vivo, and promote its absorption and removal.
雷公藤多苷片佐剂性关节炎雷公藤甲素药动学大鼠
Tripterygium glycosides tabletAdjuvant arthritisTriptolidePharmacokineticsRats
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