Yamaoka T, Tabata Y, Ikada Y
Research Center for Biomedical Engineering, Kyoto University, Japan.
J Pharm Sci. 1995 Mar;84(3):349-54. doi: 10.1002/jps.2600840316.
The biological fate of synthetic water-soluble polymers administered to mice by injection at different sites is described. After intraperitoneal (ip), subcutaneous (sc), and intramuscular (im) injections of 125I-labeled poly(vinyl alcohol) (PVA) and poly(ethylene glycol) (PEG) with various molecular weights, the time-course of polymer concentration in the blood was measured and analyzed pharmacokinetically. The location of PVA in the body was similar to that of PEG; that is, the elimination from the injection sites and the translocation from the injection sites into the blood circulation were similar for both polymers. The elimination rate of both polymers from the injection sites increased in the order ip > sc > im. After sc and im injections of polymers, the elimination rate decreased with an increase in the molecular weight, whereas the elimination rate of polymers injected showed no molecular weight dependence over the range studied, regardless of the type of polymers used. The time-course of polymer concentration in the blood depended largely on the injection route of the polymers, and the polymer elimination from the blood circulation was enhanced with the decreasing molecular weight of polymers injected. It was concluded that the molecular weight and the injection site are the important factors that affect the concentration profile of polymers in the blood circulation.
描述了通过在不同部位注射给予小鼠的合成水溶性聚合物的生物学命运。在腹腔内（ip）、皮下（sc）和肌肉内（im）注射不同分子量的125I标记的聚乙烯醇（PVA）和聚乙二醇（PEG）后，测量了血液中聚合物浓度的时间进程并进行了药代动力学分析。PVA在体内的分布与PEG相似；也就是说，两种聚合物从注射部位的消除以及从注射部位向血液循环的转运是相似的。两种聚合物从注射部位的消除速率按ip > sc > im的顺序增加。在sc和im注射聚合物后，消除速率随分子量的增加而降低，而在所研究的范围内，无论使用何种类型的聚合物，注射聚合物的消除速率均与分子量无关。血液中聚合物浓度的时间进程在很大程度上取决于聚合物的注射途径，并且随着注射聚合物分子量的降低，聚合物从血液循环中的消除增强。得出结论，分子量和注射部位是影响血液循环中聚合物浓度分布的重要因素。
