李校, 许华, 赵文, 郑青, 黄亚东, 吴晓萍, 刘长征. 重组人酸性成纤维细胞生长因子皮肤用药的药代动力学J. 药学学报, 2002, 37(6): 424-427.
引用本文: 李校, 许华, 赵文, 郑青, 黄亚东, 吴晓萍, 刘长征. 重组人酸性成纤维细胞生长因子皮肤用药的药代动力学J. 药学学报, 2002, 37(6): 424-427.
LI Xiao-kun, XU Hua, ZHAO Wen, ZHENG Qing, HUANG Ya-dong, WU Xiao-ping, LIU Chang-zheng. PHARMACOKINETIC STUDY OF RECOMBINANT HUMAN ACIDIC FIBROBLAST GROWTH FACTOR IN RABBITS BY SKIN EXTERNAL USEJ. Acta Pharmaceutica Sinica, 2002, 37(6): 424-427.
Citation: LI Xiao-kun, XU Hua, ZHAO Wen, ZHENG Qing, HUANG Ya-dong, WU Xiao-ping, LIU Chang-zheng. PHARMACOKINETIC STUDY OF RECOMBINANT HUMAN ACIDIC FIBROBLAST GROWTH FACTOR IN RABBITS BY SKIN EXTERNAL USEJ. Acta Pharmaceutica Sinica, 2002, 37(6): 424-427.

重组人酸性成纤维细胞生长因子皮肤用药的药代动力学

PHARMACOKINETIC STUDY OF RECOMBINANT HUMAN ACIDIC FIBROBLAST GROWTH FACTOR IN RABBITS BY SKIN EXTERNAL USE

  • 摘要: 目的研究rhaFGF在健康及破损皮肤用药的药代动力学特征。方法在兔健康及破损皮肤上均匀涂抹125I-rhaFGF 180 U·cm-2后,在不同的时间测血浆及组织中的放射性计数,结合纸层析的方法测定组织和血浆中的125I-rhaFGF的含量。结果破损皮肤用药后,血中rhaFGF原型物浓度呈快速上升状态,0.5 h达最大值(73.03 pg·mL-1),其后迅速下降,3 h后接近0。125I-rhaFGF给药后96 h,放射性主要浓集于皮肤,其次是肾,大脑最少。结论rhaFGF不能通过健康皮肤进入体内,可通过破损皮肤进入血循环,但吸收量少,原形物半衰期短,无蓄积作用;吸收后的rhaFGF对皮肤有较大亲和力,可分布于远处皮肤,且含量较高。

     

    Abstract: AIMTo investigate the pharmacokinetic characteristics of recombinant human acidic fibroblast growth factor (rhaFGF) after external use in rabbits. METHODS125I-rhaFGF 180 U·cm-2 was daubed to normal skin and scathed skin in rabbits. The radioactivity and paper chromatography were used to determine the 125I-concentrations and distribution in plasma and organs at different times. RESULTSThe plasma concentration of 125I-rhaFGF increased rapidily, and reach peak plasma level (73.03 pg·mL-1) thirty minutes after administration. Then the concentration of 125I-rhaFGF decreased quickly after thirty minutes, and approached to zero after three hours. Highest radioactivity accumulated in the skin, followed by kidney, lowest in the brain 96 h after administration. CONCLUSIONrhaFGF can not be absorbed from the normal skin, whereas a small amount of rhaFGF can be absorbed through scathed skin. The t1/2 of rhaFGF in plasma was very short. Cumulative effect of rhaFGF was not observed. Absorbed rhaFGF showed high affinity to skin, and can be distributed to skin far from the site of administration.

     

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