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    • 2. 发明申请
    • ANTIFUNGAL FORMULATIONS
    • 反制公式
    • WO2004037197A2
    • 2004-05-06
    • PCT/US2003/033693
    • 2003-10-23
    • GOLDSTEIN, Jay, A.ROTHMAN, Michael
    • GOLDSTEIN, Jay, A.ROTHMAN, MichaelLO, Whe-Yong
    • A61K
    • A61Q17/005A61K8/63A61K9/0014A61K31/00A61K31/4174A61K31/57A61K45/06A61K47/02A61K47/06A61K47/10A61K47/14A61K47/26A61K47/44A61Q19/00A61K2300/00
    • A topical composition and the method using the composition, which contains an antifungal agent and a low potency anti-inflammatory steroid which is safe and effective such as desonide or its derivative. The low potency steroid agent does not cause side effects such as skin atrophy, striae and hypopigmentation. In a representative example, the low potency anti­inflammatory steroid has the following structure: wherein R I , R 2 , R 3 , and R 4 taken independently can be H, C 1-C 10 alkyl, C 1­C 10 alkenyl, C3 -C 10 cycloalkyl, and phenyl groups; R I and R 2 taken together can be C3-C10 cycloalkyl; and R 3 , and R 4 taken independently can be H, C 1-C 10 alkyl, C 1-C 10 alkenyl, C3 -C 10 cycloalkyl, phenyl, C7-C 10 phenylalkyl, carboxylate, sulfonyl, phosphoryl, and phosphonyl groups. The composition can be formulated in a dosage form such as a cream, ointment, gel, lotion, foam, powder, aerosol, spray, shampoo, or liquid solution. The composition can be used to treat a fungal disease such as tinea pedis, tinea capitis, tinea corporis, tinea versicolor, tinea cruris, and candidiasis as well as intertriginous dermatitis complicated by candidiasis.
    • 一种外用组合物和使用该组合物的方法,该组合物含有抗真菌剂和安全有效的低效消炎类固醇,例如去氧化物或其衍生物。 低效类固醇药物不会引起副作用,如皮肤萎缩,条纹和色素沉着不足。 在代表性的例子中,低效力抗炎类固醇具有以下结构:其中独立取代的R 1,R 2,R 3和R 4可以是H,C 1 -C 10烷基,C 1 C 10烯基,C 3 -C 10环烷基和 苯基; R 1和R 2一起可以是C 3 -C 10环烷基; R 3和R 4独立地可以是H,C 1 -C 10烷基,C 1 -C 10烯基,C 3 -C 10环烷基,苯基,C 7 -C 10苯基烷基,羧酸酯,磺酰基,磷酰基和膦酰基。 组合物可以配制成剂型,例如霜剂,软膏剂,凝胶剂,洗剂,泡沫,粉剂,气雾剂,喷雾剂,洗发剂或液体溶液。 该组合物可用于治疗真菌性疾病,例如足癣,头癣,体癣,花斑斑,斑癣和念珠菌病以及由念珠菌病复杂的间质性皮炎。