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给药剂量对附子总生物碱在大鼠体内药代动力学特征的影响
引用本文:李燕,赵梦杰,袁岸,龚小红,彭成,李芸霞. 给药剂量对附子总生物碱在大鼠体内药代动力学特征的影响[J]. 中国实验方剂学杂志, 2016, 22(22): 82-85
作者姓名:李燕  赵梦杰  袁岸  龚小红  彭成  李芸霞
作者单位:成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137,成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137,成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137,成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137,成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137,成都中医药大学 四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地, 成都 611137
基金项目:国家自然科学基金项目(81373943,81573583);四川省杰出青年基金项目(2013JQ0018);四川省科技厅省青年科技创新研究团队专项计划项目(2014TD0007,2015TD0028)
摘    要:目的:考察不同剂量附子总生物碱在大鼠体内的药动学特征,并探讨剂量与药动学的关系。方法:将大鼠随机均分为低、中、高剂量组,分别按9.6,19.2,38.4 mg·kg-1灌胃附子总生物碱,在0,5,10,20,30,40,60,120,180,300,420,540,720,1 440 min共14个时间点眼眶内眦静脉取血,采用UHPLC-Q-TOF-MS测定不同时间点血浆中乌头碱、新乌头碱、次乌头碱、苯甲酰乌头原碱、苯甲酰新乌头原碱、苯甲酰次乌头原碱和乌头原碱的血药浓度,绘制药-时曲线,计算药动学参数。结果:与低剂量组比较,中、高剂量组上述7种生物碱类成分的药峰浓度(Cmax)和药时曲线下面积AUC0-∞升高,大部分差异有统计学意义;表观分布容积/生物利用度(Vz/F),清除率(CL)/F,半衰期(t1/2)和达峰时间(Tmax)则大部分无明显变化。结论:剂量对附子总生物碱在大鼠体内的药动学特征有显著影响,从低剂量到高剂量的范围内,附子总生物碱的体内过程基本符合线性动力学特征。

关 键 词:附子  总生物碱  药-时曲线  双酯型生物碱  单酯型生物碱  苯甲酰新乌头原碱
收稿时间:2015-12-09

Effect of Dosage on Pharmacokinetic Characteristics of Total Alkaloids from Aconiti Lateralis Radix Praeparata in Rats
LI Yan,ZHAO Meng-jie,YUAN An,GONG Xiao-hong,PENG Cheng and LI Yun-xia. Effect of Dosage on Pharmacokinetic Characteristics of Total Alkaloids from Aconiti Lateralis Radix Praeparata in Rats[J]. China Journal of Experimental Traditional Medical Formulae, 2016, 22(22): 82-85
Authors:LI Yan  ZHAO Meng-jie  YUAN An  GONG Xiao-hong  PENG Cheng  LI Yun-xia
Affiliation:Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China,Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China and Key Laboratory of Systematic Research, Development and Utilization of Chinese Medicine Resources in Sichuan Province, Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
Abstract:
Keywords:Aconiti Lateralis Radix Praeparata  total alkaloids  mean plasma concentration-time profiles  diester-type alkaloids  monoester-type alkaloids  benzoylmesaconine
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