Zhang Y Q, Jiang X T, Sun Q R, Zhang G Q, Wang Y
School of Pharmacy, Second Military Medical University, Shanghai.
Yao Xue Xue Bao. 1995;30(7):543-8.
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 58.8-256 microns, the mean size was 148.46 microns, 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 prolonged 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 group. The platinum concentration was increased in liver (P < 0.01) and decreased in kidney (P < 0.05) vs that of injection group.
采用乳液加热固化法，通过正交试验建立了制备顺铂白蛋白微球（CDDP-AMS）的优化工艺。研究了影响体外粒径和释放速率的因素。粒径集中在58.8 - 256微米，平均粒径为148.46微米，药物含量为51.16%（w/w）。CDDP-AMS的溶出曲线符合Higuchi动力学。用CDDP-AMS进行肝动脉化疗栓塞后，兔体内铂的分布半衰期和消除半衰期分别比注射组延长3.36倍和1.23倍。铂的最高血清浓度为注射组的30%。与注射组相比，肝脏中铂浓度升高（P < 0.01），肾脏中铂浓度降低（P < 0.05）。
