Azuma I, Ogawa Y, Igari Y, Ukei S, Yamamura Y
Methods Find Exp Clin Pharmacol. 1986 Jan;8(1):15-8.
The pharmaceutical properties of quinonyl-MDP-66 were discussed with special reference to the stability of oil-in-water emulsion, distribution capacity into regional lymph nodes and tumor regressive activity. The oil-in-water emulsion of quinonyl-MDP-66, which was prepared by treatment of quinonyl-MDP-66 with squalane (25 x) and emulsified with aqueous solution of 5% HCO-60 and 5.6% d-mannitol, was kept in lyophylized state and used after reconstitution by the addition of water before use. The reconstituted suspension of quinonyl-MDP-66 in oil-in-water emulsion was stable for more than 24 hrs. The oil-in-water emulsion of quinonyl-MDP-66 as prepared above was effective for the distribution of quinonyl-MDP-66 into regional lymph node in rats and for the regression of line 10 hepatoma in strain 2 guinea pigs by intralesional injection.
对喹啉基-MDP-66的药学性质进行了讨论，特别提及了水包油乳液的稳定性、向局部淋巴结的分布能力以及肿瘤消退活性。喹啉基-MDP-66的水包油乳液是通过将喹啉基-MDP-66与角鲨烷（25倍）处理并与5% HCO-60和5.6% d-甘露醇的水溶液乳化而制备的，以冻干状态保存，使用前加水复溶后使用。复溶后的喹啉基-MDP-66水包油乳液悬浮液在24小时以上保持稳定。上述制备的喹啉基-MDP-66水包油乳液通过瘤内注射对喹啉基-MDP-66在大鼠局部淋巴结中的分布以及对2系豚鼠10号线肝癌的消退有效。
