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重组人粒细胞巨噬细胞集落刺激因子栓在雌性大鼠体内药动学研究
引用本文:张星艳,于飞,伊秀林,高晶,刘昌孝,李亚卓,曾勇.重组人粒细胞巨噬细胞集落刺激因子栓在雌性大鼠体内药动学研究[J].现代药物与临床,2018,33(10):2477-2481.
作者姓名:张星艳  于飞  伊秀林  高晶  刘昌孝  李亚卓  曾勇
作者单位:天津中医药大学;天津药物研究院新药评价有限公司释药技术与药代动力学国家重点实验室;天津医科大学药学院
摘    要:目的探讨重组人粒细胞巨噬细胞集落刺激因子(rh GM-CSF)的栓剂经阴道给药和注射剂皮下给药后雌性SD大鼠阴道和宫颈组织的药动学行为。方法雌性SD大鼠分别阴道给以50、100、200μg/kg rh GM-CSF栓剂,rh GM-CSF注射剂sc 100μg/kg,用酶联免疫测定法(ELISA)检测动物组织和血清中的药物浓度,数据经DAS药动学程序处理并计算药动学参数。结果大鼠阴道给予50、100、200μg/kg rh GM-CSF栓剂后,阴道和宫颈组织药物消除半衰期(t_(1/2ke))分别为0.54、0.70、1.19 h;达峰时间(t_(peak),实测值)均为0.5 h;达峰浓度(C_(max),实测值)分别为35.24、61.45、125.55 ng/g,药-时曲线下面积(AUC_(0~8 h))分别为40.40、75.89、334.90 h·ng/g(统计矩法计算)。100μg/kg栓剂给药后,与sc相同剂量的rh GM-CSF注射剂比较,测得的最大血药浓度仅有后者的约1/250。结论rh GM-CSF栓剂阴道给药后主要作用于局部,对全身作用的影响极小。

关 键 词:重组人粒细胞巨噬细胞集落刺激因子栓  重组人粒细胞巨噬细胞集落刺激因子  雌性SD大鼠  阴道给药  药动学
收稿时间:2018/3/29 0:00:00

Pharmacokinetic study of Recombinant Human Granulocyte Macrophage Colony Stimulating Factor Suppositories in female rats
ZHANG Xing-yan,YU Fei,YI Xiu-lin,GAO Jing,LIU Chang-xiao,LI Ya-zhuo and ZENG Yong.Pharmacokinetic study of Recombinant Human Granulocyte Macrophage Colony Stimulating Factor Suppositories in female rats[J].Drugs & Clinic,2018,33(10):2477-2481.
Authors:ZHANG Xing-yan  YU Fei  YI Xiu-lin  GAO Jing  LIU Chang-xiao  LI Ya-zhuo and ZENG Yong
Institution:Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China;State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China,School of Pharmacy, Tianjin Medical University, Tianjin 300071, China,State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China,State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China,State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China,State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China and State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research New Drug Evaluation Co. Ltd, Tianjin 300301, China
Abstract:
Keywords:Recombinant Human Granulocyte Macrophage Colony Stimulating Factor Suppositories  rhGM-CSF  female SD rat  vaginal administration  pharmacokinetics
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