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新型胃动力药MP3950在大鼠体内药动学的性别差异

Gender-related pharmacokinetics of newgastroprokinetic agent MP3950 in rats

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【作者】 江琦秦峰王绍杰何仲贵赵龙山郭兴杰

【Author】 JIANG Qi;QIN Feng;WANG Shao-jie;HE Zhong-gui;ZHAO Long-shan;GUO Xing-jie;School of Pharmaceutical Engineering,Shenyang Pharmaceutical University;School of Pharmacy,Shenyang Pharmaceutical University;

【机构】 沈阳药科大学药学院沈阳药科大学制药工程学院

【摘要】 目的考察新型胃动力药MP3950单剂量给药后,在大鼠体内的性别差异。方法取12只大鼠,雌雄各半,灌胃给予10 mg·kg-1MP3950,按设定的时间点采血,采用UPLC-MS/MS法测定血浆中MP3950的质量浓度;通过DAS软件计算其药动学参数,采用SPSS软件对不同性别的药动学参数进行显著性检验。结果雌、雄大鼠灌胃给予MP3950的主要药动学参数分别为达峰血药浓度(cmax):(1 171.0±174.4)、(874.5±200.1)μg·L-1;达峰时间(tmax):(0.53±0.21)、(0.44±0.10)h;消除半衰期(t1/2):(5.03±0.86)、(5.79±1.78)h;药时曲线下面积(AUC0-∞):(4 366.5±893.8)、(1 991.4±485.3)ng·L-1·h;表观分布容积(V/F):(0.017±0.004),(0.044±0.012)L·kg-1;药物清除率(CL/F):(2.356±0.486)、(5.457±1.346)L·h-1·kg-1。MP3950在大鼠血浆中ρmax,V/F,CL/F,AUC0-t,AUC0-∞等药动学参数的差异有统计学意义(P<0.05)。结论健康Wistar大鼠灌胃给予MP3950后其药动学过程存在性别差异。

【Abstract】 Objective To investigate gender-related pharmacokinetics of newgastroprokinetic agent MP3950 in rats after a single oral administration. Methods Plasma samples from 12 rats( both male and female) were collected after oral administration at a single dose of 10 mg·kg- 1MP3950. The concentrations of MP3950 in rat plasma were determined by a sensitive and well-validated UHPLC-MS / MS method. Main pharmacokinetic parameters were calculated by DAS 2. 0 software. Pharmacokinetic parameters between different genders were analyzed by using SPSS software. Results The main pharmacokinetic parameters of MP3950 between male and female rats were as follows: ρmax:(1 171. 0 ± 174. 4),(874. 5 ± 200. 1) μg·L- 1;tmax:(0. 53 ±0. 21),(0. 44 ± 0. 10) h;t1 /2:(5. 03 ± 0. 86),(5. 79 ± 1. 78) h;AUC0-∞:(4 366. 5 ± 893. 8),(1 991. 4 ±485. 3) ng·L- 1·h;V /F:(0. 017 ± 0. 004),(0. 044 ± 0. 012) L·kg- 1. The difference of pharmacokinetic parameters( ρmax,V /F,CL /F,AUC0-t,AUC0-∞)between male and female rats had statistical significance(P <0. 05). Conclusions There are gender differences in pharmacokinetic process of MP3950 in healthy Wistar rats after oral administration.

  • 【文献出处】 沈阳药科大学学报 ,Journal of Shenyang Pharmaceutical University , 编辑部邮箱 ,2017年02期
  • 【分类号】R965
  • 【下载频次】154
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