钟延强, 蒋雪涛, 孙其荣, 张国庆, 王义. 肝动脉栓塞用顺铂白蛋白微球的研究J. 药学学报, 1995, 30(7): 543-548.
引用本文: 钟延强, 蒋雪涛, 孙其荣, 张国庆, 王义. 肝动脉栓塞用顺铂白蛋白微球的研究J. 药学学报, 1995, 30(7): 543-548.
YQ Zhang, XT Jiang, QR Sun, GQ Zhang , Y Wang, . STUDIES ON CDDP-ALBUMIN MICROSPHERES FOR HEPATIC APTERIAL CHEMOEMBOLIZATIONJ. Acta Pharmaceutica Sinica, 1995, 30(7): 543-548.
Citation: YQ Zhang, XT Jiang, QR Sun, GQ Zhang , Y Wang, . STUDIES ON CDDP-ALBUMIN MICROSPHERES FOR HEPATIC APTERIAL CHEMOEMBOLIZATIONJ. Acta Pharmaceutica Sinica, 1995, 30(7): 543-548.

肝动脉栓塞用顺铂白蛋白微球的研究

STUDIES ON CDDP-ALBUMIN MICROSPHERES FOR HEPATIC APTERIAL CHEMOEMBOLIZATION

  • 摘要: 按正交设计筛选乳化热固化法制备顺铂白蛋白微球的最佳工艺,并对影响微球粒径大小和体外释药速率的诸多因素进行了研究。该微球粒径范围为50.8~256μm。平均粒径为148.46μm,药物含量为51.16%(W/W)。兔肝动脉栓塞后,与对照组相比铂的分布半衰期延长336%,消除半衰期延长123%,体内最高血浓仅为对照组的30%。肝组织顺铂量显著增加(P<0.01),肾组织药物量明显降低(P<0.05),体内外相关性研究表明顺铂白蛋白微球体外累积溶出百分率与兔体内药物吸收分数呈显著相关(P<0.01)。

     

    Abstract: An optimum procedure was established by orthogonal test for preparing cis -platin albumin microspheres(CDDP- AMS ) with emulsion-heating stabilization method. The factors which affect particle size and release rate in vitro were studied. The particle size focusing on 58.8~256μm,the mean size was 148.46 μm, drug content was 51.16%(w/w).The dissolution profiles of the CDDP-AMS followed Higuchi kinetics. In rabbits the distribution and elimination half times of platinum were prulonged 3. 36 times and 1.23 times vs injection group, respectively , after hepatic arterial chemoembolization with CDDP-AMS. The highest serum concentration of platinum is 30 percent of that of the injection grou The platinum concentration was increased in liver(P<0.01)and decreased in kidney(P<0.05) vs that of injection group.

     

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