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    • 1. 发明申请
    • Macrolide compositions having improved taste and stability
    • 具有改善的味道和稳定性的大环内酯组合物
    • US20090232744A1
    • 2009-09-17
    • US12380378
    • 2009-02-26
    • Manfred KellerEvy Corbanie
    • Manfred KellerEvy Corbanie
    • A61K9/12A61K31/7048A61K31/7028
    • A61K9/0078A61K31/7028A61K31/7048A61K47/12
    • The invention provides an aqueous pharmaceutical composition for administration as an aerosol to the respiratory tract, nose or oropharyngeal region comprising (i) a macrolide having a poor taste and poor chemical stability in aqueous solution; (ii) at least one salt selected from the group consisting of sodium gluconate, sodium aspartate, sodium acetate, sodium lactate, sodium succinate, sodium maleate, magnesium gluconate, magnesium aspartate, magnesium citrate, magnesium acetate, magnesium lactate, magnesium succinate, and magnesium maleate; or mixtures thereof and (iii) a taste-masking agent different from said salt; wherein (a) the concentration of said macrolide in the composition is in the range of about 0.25 wt.-% to about 15 wt.-%; (b) the molar ratio of said macrolide:said salt is in the range from about 1:0.5 to about 1:100; (c) the pH of the composition is in the range of about 3 to 9; and (d) the osmolality of the composition is in the range of about 150 mOsmol/kg to about 1500 mOsmol/kg. The invention further provides a method of generating an aerosol, preferably by means of a nebuliser, which uses such an aqueous pharmaceutical composition. The macrolide may be used alone or in combination with other drugs. The composition is suitable to treat inflammatory disorders and/or infections of the respiratory tract. It has an improved taste and stability.
    • 本发明提供一种用于作为气溶胶施用于呼吸道,鼻或口咽区域的水性药物组合物,其包含(i)具有差的味道和在水溶液中的化学稳定性差的大环内酯类; (ii)至少一种选自葡萄糖酸钠,天冬氨酸钠,乙酸钠,乳酸钠,琥珀酸钠,马来酸钠,葡糖酸镁,天冬氨酸镁,柠檬酸镁,乙酸镁,乳酸镁,琥珀酸镁和 马来酸镁 或其混合物和(iii)不同于所述盐的掩味剂; 其中(a)所述大环内酯在组合物中的浓度在约0.25重量%至约15重量%的范围内; (b)所述大环内酯:所述盐的摩尔比在约1:0.5至约1:100的范围内; (c)组合物的pH在约3至9的范围内; 和(d)组合物的重量摩尔渗透压浓度在约150mOsmol / kg至约1500mOsmol / kg的范围内。 本发明还提供了一种产生气雾剂的方法,优选通过使用这种水性药物组合物的雾化器。 大环内酯可以单独使用或与其他药物组合使用。 该组合物适用于治疗炎症性疾病和/或呼吸道感染。 它具有改善的味道和稳定性。