Hanaue H, Kurosawa T, Miyakawa S, Horie F, Nemoto A, Nishimura S, Yamoto H, Yasuda H, Asagoe T, Miura S
Jpn J Cancer Res. 1985 Dec;76(12):1230-5.
In 8 postoperative patients with gastric cancer the effectiveness of fat emulsification of tegafur as a means of improving the drug distribution in the lymphatic tissue was studied. A water-in-oil type of emulsion of tegafur (FT-w/o) and an oil-in-water type of emulsion of tegafur (FT-o/w) were orally administered. A fistula in the thoracic duct, prepared in advance, was used to collect lymph. The concentrations of tegafur and 5-FU were compared in simultaneously obtained specimens of lymph and peripheral blood. In the case of FT-w/o, the tegafur concentration at 30-60 min after administration was significantly higher in both the lymph and plasma than that found using FT-o/w. In the case of FT-w/o, the 5-FU concentration at 30-120 min after the administration was significantly higher than that found with FT-o/w in both the lymph and the plasma. Thus, FT-w/o shows excellent distribution in both lymph and blood, and is considered useful as an adjuvant chemotherapeutic agent in the postoperative treatment of gastric cancer patients.
对8例胃癌术后患者研究了替加氟脂肪乳化剂作为改善药物在淋巴组织中分布的手段的有效性。口服了替加氟的油包水型乳剂(FT-w/o)和替加氟的水包油型乳剂(FT-o/w)。预先制备的胸导管瘘用于收集淋巴液。对同时采集的淋巴液和外周血标本中的替加氟和5-氟尿嘧啶浓度进行了比较。对于FT-w/o,给药后30 - 60分钟时,淋巴液和血浆中的替加氟浓度均显著高于使用FT-o/w时的浓度。对于FT-w/o,给药后30 - 120分钟时,淋巴液和血浆中的5-氟尿嘧啶浓度均显著高于使用FT-o/w时的浓度。因此,FT-w/o在淋巴液和血液中均显示出良好的分布,被认为是胃癌患者术后辅助化疗的有效药物。