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    • 3. 发明申请
    • MODIFIED DOSAGE FORMS OF TACROLIMUS
    • TACROLIMUS的改良剂型
    • WO2009022354A2
    • 2009-02-19
    • PCT/IN2008/000179
    • 2008-03-25
    • PANACEA BIOTEC LIMITED.SINGH, AmarjitSINGH, SarabjitPUTHLI, ShivanandJAIN, Rajesh
    • SINGH, AmarjitSINGH, SarabjitPUTHLI, ShivanandJAIN, Rajesh
    • A61K9/22A61K31/341A61K31/365
    • A61K9/146A61K9/1676A61K9/5078A61K9/5084A61K31/436
    • The present invention provides a modified release dosage form of tacrolimus that releases two or more amount of tacrolimus upon oral administration, the first amount of tacrolimus releases from the immediate release dosage unit substantially immediately within 0-2 hours followed by a time interval ranging from about 1-10 hours during which substantially no amount of tacrolimus is released from the dosage form, after which a second amount of tacrolimus is released wherein said second amount is released from the delayed release dosage unit either immediately e.g. within 0-2 hours or over a period of time ranging from about 2-12 hours from its initial release from the delayed release dosage unit. The dosage form may further comprise additional amount of tacrolimus to provide additional pulse of tacrolimus. The dosage forms of tacrolimus exhibit improved bioavailability and reduced flux or fluctuation over existing composition of tacrolimus. A method of preparing the dosage forms is also described.
    • 本发明提供了在口服给药后释放两种或更多量他克莫司的他克莫司的改良释放剂型,基本上立即在0-2小时内立即释放剂量单位中的第一量他克莫司释放 随后是约1-10小时的时间间隔,在此期间基本上没有量的他克莫司从剂型释放,此后释放第二量的他克莫司,其中所述第二量从缓释剂量单位立即释放,例如立即释放 在0-2小时内或在从其最初从缓释剂量单位释放约2-12小时的时间范围内。 剂型可以进一步包含额外量的他克莫司以提供额外的他克莫司脉冲。 他克莫司的剂型表现出比现有组合物他克莫司改善的生物利用度和减少的通量或波动。 还描述了制备剂型的方法。