Zhang M, Hou S X, Gong T, Cheng Y H, Liao G T
School of Pharmacy, West China University of Medical Sciences, Chendu.
Yao Xue Xue Bao. 1994;29(5):380-6.
An optimum procedure was established by orthogonal test for preparing cisplatinum albumin microspheres (CDDP-BSA-MS) with emulsion-chemical cross-linking. The quality, stability, distribution in vivo, kinetic characteristics and safety of the albumin microspheres were studied. The results showed that the surface was regular, the mean size was 13.13 +/- 3.55 microns, embedding ratio was 21.62% and the release characteristics in vitro were in accord with "biphase kinetics equation". The stability of the albumin microspheres was good after three months storage. The microspheres accumulated almost entirely in the lung 15 minutes after intravenous injection to mice. The total amount in the lung was about 97% of the injected dose at the peak concentration. Two-compartmental model can be used to describe the regulation of the pharmacokinetics of albumin microspheres in lung. Observation of the lung slice of mice showed no pathological damage.
通过正交试验建立了一种用乳液化学交联法制备顺铂白蛋白微球（CDDP-BSA-MS）的优化方法。对白蛋白微球的质量、稳定性、体内分布、动力学特征及安全性进行了研究。结果表明，微球表面规整，平均粒径为13.13±3.55微米，包封率为21.62%，体外释放特性符合“双相动力学方程”。白蛋白微球在储存三个月后稳定性良好。小鼠静脉注射后15分钟，微球几乎全部聚集在肺部。肺部总量在峰值浓度时约为注射剂量的97%。二室模型可用于描述白蛋白微球在肺部的药代动力学规律。对小鼠肺切片的观察未发现病理损伤。
