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; 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.
本发明提供了一种
水基药物组合物,可作为气雾剂用于呼吸道、鼻腔或口咽部,该组合物包含 (i) 在
水溶液中味道差、
化学稳定性差的
大环内酯类药物;(ii) 至少一种盐,选自由
葡萄糖酸钠、天门冬
氨酸
钠、
醋酸钠、
乳酸钠、
琥珀酸钠、
马来酸钠、
葡萄糖酸镁、天门冬
氨酸
镁、
柠檬酸镁、
醋酸镁、
乳酸镁、
琥珀酸镁和
马来酸镁组成的组;和 (iii) 不同于所述盐的掩味剂; 其中 (a) 组合物中所述大环内酯的浓度范围为约 0.25 wt.%至约 15 wt.-%; (b) 所述大环内酯与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 值在约 3 至 9 的范围内;以及 (d) 组合物的渗透压在约 150 mOsmol/kg 至约 1500 mOsmol/kg 的范围内。本发明进一步提供了一种产生气雾剂的方法,最好通过雾化器,使用这种
水性药物组合物。
大环内酯类药物可单独使用,也可与其他药物联合使用。该组合物适用于治疗呼吸道炎症和/或感染。它具有更好的口感和稳定性。