Abstract:
The present invention provides a method for preparing a suspension of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first organic solvent than in a second solvent which is aqueous. The process includes the steps of : (i) dissolving a first quantity of the pharmaceutically-active compound in the water-miscible first organic solvent to form a first solution ; (ii) mixing the first solution with the second solvent to precipitate the pharmaceutically-active compound ; and (iii) seeding the first solution or the second solvent or the presuspension.
Abstract:
The present invention provides a method of preparing particles with polymorph and size control of a pharmaceutical compound, the method including the steps of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particle size of the particles is less than 7µm. The present invention further provides a polymorphic form of itraconazole.
Abstract:
A method for preparing submicron sized particles of a pharmaceutically-active compound, the solubility of which is greater in a water-miscible first solvent than in a second solvent which is aqueous is disclosed, wherein the process comprises the steps of: (i) dissolving the pharmaceutically-active compound in the water-miscible first solvent to form a solution, the first solvent being selected from the group consisting of N methyl-2-pyrrolidinone, 2-pyrrolidone, dimethyl sulfoxide, dimethylacetamide, lactic acid, methanol, ethanol, isopropanol, 3-pentanol, n-propanol, glycerol, butylene glycol, ethylene glycol, polypropylene glycol, mono- and diacylated monoglycerides, dimethyl isosorbide, acetone, dimethylformamide, 1,4-dioxane, ethyl acetate, propyl acetate, polyethylene glycol, polyethylene glycol esters, polyethylene glycol sorbitans, polyethylene glycol monoalkyl ethers, polypolypropylene glycol, polypropylene alginate, polypolypropylene glycol-10 butanediol, polypolypropylene glycol-10 methyl glucose ether, polypolypropylene glycol-20 methyl glucose ether, polypolypropylene glycol-15 stearyl ether, polypolypropylene glycol dicaprylate, polypropylene glycol dicaprate, polypropylene glycol laurate; (ii) mixing the solution with the second solvent to define a pre-suspension; and (iii) adding energy to the pre-suspension to form particles having an average effective particle size of less than about 2 micron, and said adding energy step comprises homogenization, counter-current flow homogenization, microfluidization or sonication.
Abstract:
The present invention provides a method of preparing particles with polymorp h and size control of a pharmaceutical compound, the method including the step s of: (1) providing pharmaceutical compound in a first phase; (2) seeding the compound; (3) causing a phase change in the pharmaceutical compound to a second phase of a desired polymorphic form; and (4) wherein the mean particl e size of the particles is less than 7~m. The present invention further provid es a polymorphic form of itraconazole.