Patent ID: 6461545
Filing Date: 2002-10-08
Classification: A61K,B01J,Y10S

Abstract:
A method for preparing imidazole derivative active agent containing microspheres, said method comprising(A) nebulizing a solution comprising (a) an imidazole active agent having the formula â€ƒwherein R, R1, and R2 are independently hydrogen or lower alkyl; R3 is hydrogen, methyl or ethyl; R4 is hydrogen or methyl; Ar is phenyl, monohalophenyl, dihalophenyl, trihalophenyl, mono(lower alkyl)phenyl, di(lower alkyl)phenyl, lower alkoxyphenyl, or halothienyl; Ar1 is phenyl, monohalophenyl, dihalophenyl, trihalophenyl, mono(lower alkyl)phenyl, di(lower alkyl)phenyl, lower alkoxyphenyl, or cyanophenyl; and n is 1 or 2; (b) a microsphere forming carrier selected from the group consisting of (i) a proteinoid; (ii) an acylated amino acid or poly amino acid or a salt thereof; (iii) a sulfonated amino acid or poly amino acid or a salt thereof; (iv) a protein or a salt thereof; (v) an enteric coating material; and (vi) any combination thereof; and (c) an active agent and carrier solubilizing effective amount of a solvent comprising an aqueous solution of at least one volatile organic acid; wherein the volume:volume ratio of acid to water in said solvent is at least about 3:7; and (B) decreasing said ratio to less than about 3:7, to yield said microspheres.