【摘 要】
：
采用放射性标记的方法：研究生物大分子多糖MP-1关节腔内药动学.以14C标记葡萄糖与普通葡萄糖作为混合碳源,通过发酵对MP-1进行放射性标记.给予大鼠关节腔注射0.25、0.5、1 mg/只3个剂量的14C标记MP-1,测定给药后不同时间关节腔内放射性残留.结果：显示通过发酵可成功制备比活度为7.27 μ Ci/mg,放化纯度为99.5％的放射性标记MP-1样品.关节腔注射MP-1 1 mg/只,
【机 构】
：
山东省药学科学院新药评价中心,山东济南250101 天津药物研究院释药技术与药代动力学国家重点实验
【出 处】
：
2015第11届全国药物和化学异物代谢学术会议
论文部分内容阅读
采用放射性标记的方法：研究生物大分子多糖MP-1关节腔内药动学.以14C标记葡萄糖与普通葡萄糖作为混合碳源,通过发酵对MP-1进行放射性标记.给予大鼠关节腔注射0.25、0.5、1 mg/只3个剂量的14C标记MP-1,测定给药后不同时间关节腔内放射性残留.结果：显示通过发酵可成功制备比活度为7.27 μ Ci/mg,放化纯度为99.5％的放射性标记MP-1样品.关节腔注射MP-1 1 mg/只,在大鼠膝关节内的平均滞留时间(mean residence time,MRT)约为333 h,给药后30 d仍有约27％的残留,180 d后仍有9.85％的残留.AUC与给药剂量成正相关,相关系数为0.9999,且同一时间点、不同给药剂量MP-1在关节腔内的残留比例差异并不明显,表明在0.25～1 mg/只剂量范围内,MP-1在关节腔内随时间消除的比例并无明显剂量依赖性.
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