目的 探讨重组人粒细胞巨噬细胞集落刺激因子（rhGM-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、200 μg/kg rhGM-CSF栓剂，rhGM-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、200 μg/kg rhGM-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）。100 μg/kg栓剂给药后，与sc相同剂量的rhGM-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 rhGM-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。

Objective To investigate the pharmacokinetics behavior of recombinant human Granulocyte macrophage colony stimulating factor (rhGM-CSF) in tissues of vagina and cervix of female SD rats after vaginal and sc administration with suppositories and injections. Methods Female SD rats were given rhGM-CSF Suppositories at 50, 100, and 200 μg/kg by vaginal administration and rhGM-CSF injection at 100 μg/kg dose by subcutaneous administration. The contents of rhGM-CSF in vagina and cervix tissues were determined by ELISA method, as well as the 100 μg/kg dose rhGM-CSF concentration in plasma. Pharmacokinetic parameters were calculated by using DAS software. Results The pharmacokinetic parameters for 50, 100, and 200 μg/kg of rhGM-CSF Suppositories were as following:the elimination half-life (t_1/2ke) were 0.54, 0.70, and 1.19 h, respectively. The peak time (t_peak, measured value) was 0.5 h, and the peak concentrations (C_max, measured value) were 35.24, 61.45, and 125.5 ng/g, respectively. the area under the curve (AUC_{0~8 h}) calculated were 40.40, 75.89, and 334.9 h·ng/g, respectively. After vaginal administration at the 100 μg/kg dose, the drug concentration measured in plasma was only about 1/250 of of rhGM-CSF Injection. Conclusion rhGM-CSF Suppositories mainly act on local tissue after vaginal administration, and have limited impact or effect systematically.