Hagiwara A, Sakakura C, Tsujimoto H, Imanishi T, Ohgaki M, Yamasaki J, Sawai K, Takahashi T, Fujita T, Yamamoto A, Muranishi S, Ikada Y
First Department of Surgery, Kyoto Prefectural University of Medicine, Kamigyo-ku, Japan.
Anticancer Drugs. 1997 Feb;8(2):182-8. doi: 10.1097/00001813-199702000-00009.
A new formulation has been developed for the delivery of 5-fluorouracil (5-FU) in treating peritoneal carcinomatosis. The new formulation (5-FU-MS) involves the incorporation of 5-FU into microspheres composed of a poly(glycolide-co-lactide) matrix. The incorporated 5-FU is released slowly over a 3 week period. We investigated the drug distribution and pharmacokinetics of 5-FU in rats receiving an i.p. injection of 5-FU-MS or aqueous 5-FU solution. The concentration of 5-FU was higher in the i.p. tissues (omentum and mesentery) and lower in the extraperitoneal tissues (blood plasma, lung and heart) in rats given 5-FU-MS than in rats given the aqueous 5-FU solution. Pharmacokinetic analysis showed that the area under the curve (AUC) was significantly greater in the omentum and the mesentery than in other tissues of rats given 5-FU-MS. There was no significant difference in the AUC in the tissues of rats given the aqueous 5-FU solution.
已开发出一种用于递送5-氟尿嘧啶（5-FU）以治疗腹膜癌的新制剂。这种新制剂（5-FU-MS）涉及将5-FU掺入由聚（乙交酯-共-丙交酯）基质组成的微球中。掺入的5-FU在3周内缓慢释放。我们研究了接受腹腔注射5-FU-MS或5-FU水溶液的大鼠体内5-FU的药物分布和药代动力学。给予5-FU-MS的大鼠腹腔组织（大网膜和肠系膜）中5-FU的浓度高于给予5-FU水溶液的大鼠，而腹膜外组织（血浆、肺和心脏）中的浓度则较低。药代动力学分析表明，给予5-FU-MS的大鼠大网膜和肠系膜中的曲线下面积（AUC）显著大于其他组织。给予5-FU水溶液的大鼠各组织中的AUC没有显著差异。
