Concentrated suspension of water insoluble pharmaceutical substances, comprising:
a) micronized particles of at least one water insoluble pharmaceutical substance with a particle size distribution in which the d(0.5) fraction is less than 3 µm, the span value is less than 2, and such features are retained upon aging the suspension for 90 days; said pharmaceutical substance being present at a concentration of from 5 to 50 times the concentration of a suspension of the same substance for inhalatory administration;
b) an aqueous solution of a pharmaceutically acceptable surfactant as dispersing medium for said micronized particles of pharmaceutical substance;
c) a salt dissolved in said aqueous solution, at a concentration that: i) does not cause coagulation of said particles of pharmaceutical substance; and ii) generates upon dilution an inhalatory suspension in which the concentration of salt in the aqueous phase is not higher than 10 g/l. present at a concentration of from 0.1 to 2.0 g/l.
不溶于
水的药物浓缩悬浮液,包括
a) 至少一种
水不溶性药物的微粉化颗粒,其粒度分布为 d(0.5) 部分小于 3 µm,跨度值小于 2,且悬浮液老化 90 天后仍能保持这些特征;所述药物的浓度为用于吸入给药的相同药物悬浮液浓度的 5 至 50 倍;
b) 医药上可接受的表面活性剂的
水溶液,作为所述药物微粒的分散介质;
c) 溶于所述
水溶液中的盐,其浓度为:i) 不会导致所述药物颗粒凝结;ii) 稀释后产生吸入悬浮液,其中
水相中盐浓度不高于 10 克/升,浓度为 0.1 至 2.0 克/升。