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    • 33. 发明公开
    • ORAL ITRACONAZOLE COMPOSITION WHICH IS NOT AFFECTED BY INGESTED FOOD AND PROCESS FOR PREPARING SAME
    • 伊曲康唑口服组合未营养受到影响,及其制造方法
    • EP1663231A4
    • 2009-04-29
    • EP04774524
    • 2004-09-07
    • HANMI PHARM IND CO LTD
    • WOO JONG SOOYI HONG GI
    • A61K31/496
    • A61K9/4858A61K31/496
    • An oral itraconazole composition which is not affected by ingested food and a preparation method thereof are provided, which itraconazole composition forms stable emulsified microparticles when it is orally administered to enhance bioavailability of itraconazole, and is not affected by pH and ingested food, so that the difference of absorption in individuals can be reduced. The oral high viscosity glassy composition which is not affected by ingested food comprises itraconazole, acidifying agent, amphiphilic additives, volatile additives, surfactant and oil, wherein the bioavailability ratio of itraconazole before to after digestion is 0.8 or more; the viscosity of the composition is 10,000cps at 25 deg. C; the composition has self-microemulsifying capability; the acidifying agent is selected from phosphoric acid, hydrochloric acid and a solution thereof; the amphiphilic additive is selected from transcutol, dimethyl isosorbide, glycofurol, propylene glycol, propylene carbonate, solutol and a mixture thereof; the surfactant is selected from a reaction product of natural or hydrogenated vegetable oil and ethylene glycol, polyoxyethylene-sorbitan-fatty acid ester, polyoxyethylene fatty acid ester and a mixture thereof; and the oil is tocopherol, its derivatives and a mixture thereof. The method for preparing the oral itraconazole composition which is not affected by ingested food comprises the steps of: (a) dissolving itraconazole in a mixed solution of acidifying agent, amphiphilic additives and volatile additives; (b) adding surfactant and oil into the mixture and dissolving them; and (c) removing the volatile additives from the mixed solution, wherein the volatile additive is C2-C3 alcohol.