Hagiwara A, Takahashi T, Shimotsuma M, Shirasu M, Tsujimoto H, Ohyama T, Ohgaki M, Imanishi T, Yamazaki J, Fujita T
First Dept. of Surgery, Kyoto Prefectural University of Medicine.
Gan To Kagaku Ryoho. 1995 Sep;22(11):1638-40.
A new dosage formulation (5-FU-MS), composed of 5-fluorouracil (5-FU) incorporated in polyglactin microspheres, was studied by animal experiments, which revealed the following results. Intraperitoneal 5-FU-MS delivered greater concentrations of 5-FU for longer periods selectively to the intraperitoneal tissues, whereas it delivered a lower concentration to the blood plasma, than 5-FU solution did in rats. In mice, the 50% lethal dose value of intraperitoneal 5-FU-MS was 535 mg/kg. The toxicity of 5-FU-MS was less than 1/2 that of intraperitoneal 5-FU solution, of which the 50% lethal dose value was 242 mg/kg. Intraperitoneal 5-FU-MS at 200 mg of 5-FU/kg improved the survival curve of mice with peritoneal carcinomatosis better than the identical dose of 5-FU solution.
一种新的剂型（5-氟尿嘧啶微球，5-FU-MS），由包裹在聚丙交酯乙交酯微球中的5-氟尿嘧啶（5-FU）组成，通过动物实验进行了研究，结果如下。在大鼠中，腹腔注射5-FU-MS比5-FU溶液能更长时间地选择性向腹腔组织输送更高浓度的5-FU，而向血浆输送的浓度较低。在小鼠中，腹腔注射5-FU-MS的半数致死剂量值为535mg/kg。5-FU-MS的毒性小于腹腔注射5-FU溶液的毒性的1/2，腹腔注射5-FU溶液的半数致死剂量值为242mg/kg。腹腔注射200mg 5-FU/kg的5-FU-MS比相同剂量的5-FU溶液能更好地改善腹膜癌小鼠的生存曲线。
