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研究

发布时间：2018-01-17 19:26

本文关键词：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研究　出处：《中国药房》2017年07期 　论文类型：期刊论文

【摘要】：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 m L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 m L,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c_(max)分别为(1.139±0.114)、(0.916±0.103)μg/m L,t_(max)分别为(2.167±0.606)、(3.083±0.801)h,t_(1/2α)分别为(5.500±3.610)、(5.593±1.795)h,AUC_(0-7 h)分别为(5.052±0.371)、(4.707±0.347)μg·h/m L,MRT_(0-7 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)m L/h。与正常组比较,模型组大鼠c_(max)显著减小,t_(max)和MRT_(0-7 h)显著延长(P0.05)。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。
[Abstract]:Objective: To study the activity of Tripterygium wilfordii multi glycoside tablet composition of triptolide in rats and normal rats adjuvant arthritis model pharmacokinetic characteristics, in order to provide reference for clinical rational drug use. Methods: 12 SD rats were randomly divided into normal group and model group, model group, 6 rats in each group. SC in complete Freund's adjuvant 0.1 M L replication model of adjuvant arthritis rats in the normal group, SC saline. 14 d after modeling, two rats in group Ig were Tripterygium wilfordii suspension 96 mg/kg, respectively, before and after administration of 10,30,45,60,90120150180240300420 min orbital blood 0.4 m L, determination of blood concentration of Tripterygium triptolide by HPLC; using DAS 2 pharmacokinetic software to calculate the pharmacokinetic parameters were compared. Results: triptolide in vivo in the normal group, the rats in the model group c_ (max) respectively (1.139 + 0.114), (0.916. 0.103) g/m L, t_ (max) respectively (2.167 + 0.606), (3.083 + 0.801) h, t_ (1/2 alpha) respectively (5.500 + 3.610), (5.593 + 1.795) h, AUC_ (0-7 h) respectively (5.052 + 0.371), (4.707 + 0.347) g - h/m L MRT_ (0-7, h) respectively (3.224 + 0.119), (3.429 + 0.139) h, CL respectively (11.616 + 2.986), (11.246 + 2.638) compared with the normal group, m L/h., c_ in the model group decreased significantly (max), t_ (max) and MRT_ (0-7 h) significantly extension (P0.05). Conclusion: adjuvant arthritis can affect the drug in vivo of triptolide in rat pharmacokinetic characteristics, which can promote the absorption and elimination of triptolide in rats.

【作者单位】：宜春学院化学与生物工程学院;
【分类号】：R285.5;R-332
【正文快照】： 类风湿关节炎(Rheumatoid arthritis,RA)属于慢性全身性自身免疫性疾病,主要临床表现为关节周围组织和滑膜非感染性炎症病变,临床治疗多采用口服给药。雷公藤多苷片(Tripterygium glycosides tablets,TGPT)为传统中成药,是从卫矛科植物雷公藤的根芯部分提取并精制而成的混合物

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