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    • 3. 发明申请
    • PHARMACEUTICAL COMPOSITIONS CONTAINING GAMMA-BUTYROBETAIN FOR TREATMENT OF BLOOD FLOW DISORDERS
    • 用于治疗血液流动性疾病的含有γ-氨基丁酸的药物组合物
    • WO1997006795A1
    • 1997-02-27
    • PCT/LV1996000003
    • 1996-08-20
    • KALVINSH, IvarsVEVERIS, Maris
    • A61K31/205
    • A61K31/205
    • The invention relates to gamma -butyrobetaine-containing pharmaceutical compositions for oral, parenteral, subcutaneous or rectal administrations, that are providing for the treatment blood circulation disturbances of various genesis and localisation. This composition in the experiments on anaesthesized cats at a dose of 10 mg/kg, i.v. increases the total blood flow by 12 %, not considerably changing blood pressure and heart rhythm. The composition arrests adrenaline-induced isolated rabbit ear blood-vessel spasms. In a concentration of 2.0 mM it decreases reperfusion pressure by 18 %. NO-synthase blocking reverses the composition effect on adrenaline-caused blood-vessel spasms. Being infused the composition at a dose of 200 mg/kg significantly increases blood coagulation during phases I-II. In the comparative experiments the disclosed composition demonstrates more potent effect compared to known medicine [3-(2,2,2-trimethylhydrazinium)propionate]. The preparation is distinguished by a low toxicity and wide safety margin.
    • 本发明涉及用于口服,肠胃外,皮下或直肠给药的含有γ-丁酸甜菜碱的药物组合物,其用于治疗各种发生和定位的血液循环障碍。 在10mg / kg剂量的麻醉猫的实验中的这种组合物,i.v。 总血液流量增加12%,不会显着改变血压和心律。 该组合物阻止肾上腺素诱导的分离的兔耳血管痉挛。 浓度为2.0 mM时,再灌注压降低18%。 NO合成酶阻断反转对肾上腺素引起的血管痉挛的组合效应。 以200mg / kg的剂量输注组合物在I-II期期间显着增加血液凝固。 在比较实验中,与已知的药物[3-(2,2,2-三甲基肼)丙酸酯]相比,所公开的组合物显示更强的效果。 该制剂的特点是毒性低,安全性较高。