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    • 43. 发明授权
    • Pharmaceutical composition for intrarectal administration, and
suppository prepared therefrom
    • 用于直肠内给药的药物组合物和由其制备的栓剂
    • US4434159A
    • 1984-02-28
    • US249462
    • 1981-03-31
    • Kunio SekineYoshiki SuzukiGentaro YamashitaHisao Yamaguchi
    • Kunio SekineYoshiki SuzukiGentaro YamashitaHisao Yamaguchi
    • A61K9/02A61K47/12A61K47/18A61K47/22A61K37/26A61K31/70A61K31/725A61K37/00
    • A61K47/183A61K47/12A61K47/22A61K9/02Y10S424/15Y10S514/808
    • A pharmaceutical composition for intrarectal administration comprising a pharmaceutically effective amount of an active ingredient which when administered alone to the rectum, is substantially unabsorbable into the living body through the mucous membrane of the rectum, said composition further containing an absorption aid acting within the rectum in such a way as to induce absorption of said active ingredient through the rectal mucous membrane, said absorption aid being characterized by (1) being substantially nontoxic to living organisms, (2) containing in the molecule at least two hydrophilic groups selected from the class consisting of carboxyl groups, acidic hydroxyl groups, carboxyl groups in the form of pharmaceutically acceptable salts, acidic hydroxyl groups in the form of pharmaceutically acceptable salts, carboxyl groups in the form of amides and acidic hydroxyl groups in the form of esters, (3) containing in the molecule at least two lipophilic groups selected from the class consisting of groups of the formulae ##STR1## and -CH.sub.2 -, the number of the lipophilic groups being not less than that of the hydrophilic groups, and (4) having a molecular weight of from about 100 to about 300; and a suppository prepared therefrom in unit dosage form.
    • 一种用于直肠内给药的药物组合物,其包含药物有效量的活性成分,其当单独施用于直肠时,通过直肠的粘膜基本上不能吸收到生物体中,所述组合物还含有在直肠内作用的吸收辅助剂 所述吸收助剂的特征在于:(1)对活生物体基本上无毒,(2)在分子中含有至少两个选自以下的亲水基团: 羧基,酸性羟基,可药用盐形式的羧基,药学上可接受的盐形式的酸性羟基,酰胺形式的羧基和酯形式的酸性羟基,(3)含有 在分子中至少有两个选自该类的亲脂基团 由式(I)和-CH 2 - 的基团组成,亲油基团的数目不小于亲水基团的数目,和(4)分子量为约100至约300; 和由单位剂型制备的栓剂。