石杉碱甲注射用缓释微粒在大鼠体内的药动学

来源 :中国医药工业杂志 | 被引量 : 0次 | 上传用户:digitalmachineu
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以石杉碱甲(1)为模型药物,聚左旋丙交酯为载体,制备了注射用生物降解缓释微粒.所得微粒粒径小于120μm,1含量为6.27%,在pH 7.4磷酸盐缓冲液(含0.02% Tween-80)中72 h累积释放率约为5%,30 d累积释放可达93%.用LC-MS/MS法测定大鼠血浆中的药物浓度.结果表明,本品注射首日内血药浓度快速下降,24 h后又缓慢上升,至11d达极值(1.94±-0.01)ng/ml.结果提示所得1缓释微粒体内外均有良好的缓释效果.
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