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    • 2. 发明授权
    • Drug composition
    • 药物组成
    • US5474989A
    • 1995-12-12
    • US203863
    • 1994-03-01
    • Masanori HashimotoMasaki OtagiriTeruko Imai
    • Masanori HashimotoMasaki OtagiriTeruko Imai
    • A61K9/14A61K31/19A61K31/73A61K31/355A61K31/40A61K31/56
    • A61K9/146A61K31/19
    • The present invention relates to a drug composition in which the solubility and the dissolution rate of a drug having low water solubility are improved by incoroprating therein a low molecular weight chitosan in an amount of from 0.2 to 10 parts by weight per one part by weight of the poorly water-soluble drug. As the low molecular weight chitosan, those having a weight average molecular weight in the range from 500 to 50,000 and soluble in water were employed. This drug composition is prepared by mixing the components intimately so as to obtain a homogeneous dispersion of the low molecular weight chitosan with the mass of the composition.The drug composition according to the invention can be worked up into various preparation forms, such as, granules etc., as medicaments for administration to living organisms in which the bioabsorptivity and biouptake are improved.
    • 本发明涉及药物组合物,其中水溶性低的药物的溶解度和溶解速度通过其中低分子量壳聚糖的加入量得到改善,所述低分子量壳聚糖的量为每10重量份 水溶性差的药物。 作为低分子量壳聚糖,使用重均分子量为500〜50000且可溶于水的那些。 通过紧密混合各组分制备该药物组合物,以获得低分子量壳聚糖与组合物质量的均匀分散体。 根据本发明的药物组合物可以被加工成各种制剂形式,例如颗粒等,作为用于生物吸收和生物吸收改善的生物体的给药的药物。
    • 3. 发明授权
    • Acetamide derivative and application thereof
    • 乙酰胺衍生物及其应用
    • US5317026A
    • 1994-05-31
    • US25167
    • 1993-03-02
    • Masaki OtagiriTeruko Imai
    • Masaki OtagiriTeruko Imai
    • A61K31/445A61P1/04C07D295/08C07D295/096C07D211/32
    • C07D295/096
    • 2-Substituted-N-{3-[3-(1-piperidinomethyl)phenoxy]propyl}acetamide, derivatives thereof, and pharmaceutically acceptable salts thereof. The substitution group may be aminomethylcyclohexane carbonyl group or N-carbobenzoxy-p-aminomethylhexane carbonyl group. The compounds having the first-mentioned group can be an effective component of an antiulcer drug composition, and the compounds of the last-mentioned group are intermediates for producing the compounds having the first-mentioned group. Disclosed also is an antiulcer drug composition comprising the above compound as an effective component. The antiulcer drug composition exhibits both the gastric acid secretion inhibitive activity and the gastric mucosa protective activity, and is effective as suppression and cure of ulcers.
    • 2-取代的N- {3- [3-(1-哌啶基甲基)苯氧基]丙基}乙酰胺及其衍生物及其药学上可接受的盐。 取代基可以是氨甲基环己烷羰基或N-苄氧羰基对氨基甲基己烷羰基。 具有前述基团的化合物可以是抗溃疡药物组合物的有效成分,并且最后提到的基团的化合物是用于制备具有前述基团的化合物的中间体。 还公开了包含上述化合物作为有效成分的抗溃疡药物组合物。 抗溃疡药物组合物既显示胃酸分泌抑制活性又具有胃粘膜保护作用,并且作为溃疡的抑制和治愈是有效的。