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    • 92. 发明申请
    • FAT EMULSION
    • FAT乳液
    • WO1991007973A1
    • 1991-06-13
    • PCT/JP1990001531
    • 1990-11-26
    • NIPPON SHINYAKU CO., LTD.
    • NIPPON SHINYAKU CO., LTD.SEKI, JunzoUSHIMARU, KouichiSUGIYAMA, Makoto
    • A61K31/71
    • A61K9/1075A61K31/7048
    • A fat emulsion developed to solve the problems of polyene antifungal antibiotics that they have such a severe toxicity as to limit the administration range thereof by suitably designing the administration form, thereby reducing the hemolytic toxicity and nephrotoxicity and facilitating the migration of a drug toward infected parts without adversely affecting the pharmacological action (antifungal action) on a molecular level. The emulsion comprises 0.005 to 5 % of a polyene antifungal antibiotic, 0.5 to 30 % of a simple lipid, and a phospholipid in an amount 0.15 to 2 times as large as that of the simple lipid, wherein the relative proportion of each ingredient is controlled to give a fine microemulsion of a mean particle diameter of at least 10 nm up to 100 nm. This emulsion can remarkably enhance the efficacy of polyene antifungal antibiotics such as Amphotericin B and is very useful for the development of medicines.
    • 为了解决多烯抗真菌抗生素的问题,开发了一种脂肪乳剂,它们具有如此严重的毒性,通过适当地设计给药形式来限制其给药范围,从而降低溶血毒性和肾毒性,并促进药物向感染部位的迁移 而不会对分子水平的药理作用(抗真菌作用)产生不利影响。 乳液含有0.005〜5%的多烯抗真菌抗生素,0.5〜30%的单一脂质,磷脂的量为单质脂的0.15〜2倍,其中各成分的相对比例被控制 得到至少10nm至100nm的平均粒径的细微乳液。 这种乳液可以显着提高多烯抗真菌抗生素如两性霉素B的功效,对于开发药物非常有用。