Absorption-promoting compounds, compositions thereof with
pharmaceuticals and/or bases for rectal administration and method of use
    95.
    发明授权
    Absorption-promoting compounds, compositions thereof with pharmaceuticals and/or bases for rectal administration and method of use 失效
    吸收促进化合物,其组合物与用于直肠给药的药物和/或碱基和使用方法

    公开(公告)号:US4442090A

    公开(公告)日:1984-04-10

    申请号:US246953

    申请日:1981-03-24

    摘要: Compounds satisfying four specific requirements, namely: (1) a log P value in the range of from 2.5 to 6, (2) a molecular structure with at least one carboxyl group, (3) a pKa value for the carboxyl group of not less than 2.5 and (4) absence of halo substitution, and nontoxic salts thereof promote absorption of pharmacologically-active substance through the rectum into the bloodstream and are effective to raise the concentration of such active substance in the bloodstream even when the active substance is usually unabsorbable or absorbable through the rectum only with considerable difficulty. The compounds are combined with pharmacologically-active ingredients, with pharmaceutical bases suitable for rectal administration of drugs and with appropriate combinations of both.

    摘要翻译: 满足四个具体要求的化合物,即:(1)log值在2.5至6的范围内,(2)具有至少一个羧基的分子结构,(3)羧基的pKa值不低于 超过2.5和(4)不存在卤素取代,并且其无毒盐促进药物活性物质通过直肠吸收到血液中,并且有效地提高这种活性物质在血流中的浓度,即使活性物质通常是不可吸收的 或通过直肠吸收只有相当大的困难。 将化合物与药理学活性成分组合,其中适合于直肠给药的药物基质和两者的适当组合。

    Lower fatty acid glyceride high-HLB lubricating suppository and method
for making and using the same
    98.
    发明授权
    Lower fatty acid glyceride high-HLB lubricating suppository and method for making and using the same 失效
    低脂肪酸甘油酯高HLB润滑栓剂及其制备和使用方法

    公开(公告)号:US4347237A

    公开(公告)日:1982-08-31

    申请号:US239882

    申请日:1981-03-02

    IPC分类号: A61K9/02

    摘要: The disclosed lubricating suppository is formulated to have properties advantageous for coital use, including extraordinary water washability. The ingredients and phase relationships of the suppository composition provide a high degree of compatibility with water and with naturally-occurring vaginal moisture. The suppository composition contains a glyceride lubricant and can be lubricious with or without the presence of moisture. The suppository, which is solid at room temperature but melts in a short time at body temperature, is made by dissolving, for example, 10-30 parts by weight of high-HLB (e.g. >14) nonionic surfactant in 50-70 parts by weight of a molten, water-soluble polyoxyethylene glycol component and by dispersing or emulsifying 10-20 parts by weight of the glyceride (e.g. a triglyceride of C.sub.6 -C.sub.18 aliphatic carboxylic acids) included in the composition. In use, the suppository can be inserted prior to coitus and permitted to melt to a liquid, which is lubricious even in the absence of moisture, but still has the aforementioned extraordinary water washability.

    摘要翻译: 公开的润滑栓剂被配制成具有有利于配偶使用的性质,包括非凡的水洗性。 栓剂组合物的成分和相位关系提供与水和天然存在的阴道水分的高度相容性。 栓剂组合物含有甘油酯润滑剂,并且可以在有或没有水分的情况下润滑。 在室温下固体但在体温短时间熔化的栓剂是通过将例如10-30重量份的高HLB(例如> 14)非离子表面活性剂溶解在50-70份中制成的栓剂 熔融的水溶性聚氧乙烯二醇组分的重量,并通过分散或乳化10-20重量份包含在组合物中的甘油酯(例如C 6 -C 18脂族羧酸的甘油三酯)。 在使用中,栓剂可以在交联之前插入并允许熔化成液体,即使在没有水分的情况下也是润滑的,但仍然具有上述非凡的水洗性。