DRY POWDER FORMULATION OF AZOLE DERIVATIVE FOR INHALATION

摘要

A spray dried-powder composition for inhalation comprising particles (X) containing (a) between 5 and 50% by weight of at least one azole derivative in amorphous state but not in crystalline structure and (b) at least one matricial agent to the composition selected from a group consisting of polyol such as sorbitol, mannitol and xylitol; a monosaccharides such as glucose and arabinose; disaccharide such as lactose, maltose, saccharose and dextrose; cholesterol, and any mixture thereof, wherein the composition provides a dissolution rate of said azole derivative of at least, 5% within 10 minutes, 10% within 20 minutes and 40% within 60 minutes when tested in the dissolution apparatus type 2 of the United States Pharmacopoeia at 50 rotation per minute, 37° C. in 900 milliliters of an aqueous dissolution medium adjusted at pH 1.2 and containing 0.3% of sodium laurylsulfate.

主权项

1. Spray dried particles for inhalation composition comprising:
a) between 5 to 50% by weight of at least one azole compound in an amorphous state; and b) at least one matricial agent to the composition selected from the group consisting of polyol including one of sorbitol, mannitol or xylitol; a monosaccharide including one of glucose or arabinose; disaccharide including one of lactose, maltose, saccharose or dextrose; cholesterol, and any mixture thereof.