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    • 4. 发明授权
    • Stable pharmaceutical composition
    • 稳定的药物组成
    • US4857552A
    • 1989-08-15
    • US203836
    • 1988-06-08
    • Leonard S. RosenbergCheryl BlackEarl R. SpeicherDietmar Wagenknecht
    • Leonard S. RosenbergCheryl BlackEarl R. SpeicherDietmar Wagenknecht
    • A61K9/00A61K9/08A61K31/19A61K31/195A61K31/215A61K31/22A61K47/12A61P9/12A61P25/02
    • A61K9/0019A61K31/195A61K31/215A61K47/12
    • An injectable, aqueous pharmaceutical composition for the treatment of cardiac conditions comprising an effective amount of methyl 3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride (esmolol) for treating such a cardiac condition, said composition comprising about 1 mg to 250 mg of esmolol per milliliter of said injectable pharmaceutical composition; 0.01 to 0.02M buffer; said composition having a pH range of 4.5 to 5.5, the esmolol degrading in aqueous solution to produce 3-[4-(3-propionic acid)phenoxy]-1-isopropylamino-2-propanol hydrochloride, said 3-[4-(3-propionic acid)-phenoxyl]-1-isopropylamino-2-propanol hydrochloride having a pK in the pH range of said composition to thereby act as a secondary buffer to increase the buffer capacity and minimize the change in pH as degradation occurs, whereby the stability of esmolol in an aqueous composition is enhanced.
    • 一种用于治疗心脏病症的可注射的水性药物组合物,其包含有效量的用于治疗这种心脏病症的3- [4-(2-羟基-3-异丙基氨基)丙氧基]苯丙酸甲酯(艾司洛尔),所述组合物包含约 每毫升所述可注射药物组合物1mg至250mg艾司洛尔; 0.01〜0.02M缓冲液; 所述组合物的pH范围为4.5至5.5,艾司洛尔在水溶液中降解以产生3- [4-(3-丙酸)苯氧基] -1-异丙基氨基-2-丙醇盐酸盐,所述3- [4-(3 - 丙酸) - 苯氧基] -1-异丙基氨基-2-丙醇盐酸盐,其在所述组合物的pH范围内具有pK,从而充当二级缓冲液,以增加缓冲能力,并且随着劣化发生使pH的变化最小化,由此 艾司洛尔在水性组合物中的稳定性得到提高。