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    • 3. 发明申请
    • MODIFIED DOSAGE FORMS OF TACROLIMUS
    • 改良剂量剂型
    • WO2009022354A3
    • 2009-04-09
    • PCT/IN2008000179
    • 2008-03-25
    • PANACEA BIOTEC LTDSINGH AMARJITSINGH SARABJITPUTHLI SHIVANANDJAIN RAJESH
    • SINGH AMARJITSINGH SARABJITPUTHLI SHIVANANDJAIN RAJESH
    • A61K31/4745A61K9/22
    • 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.
    • 本发明提供了他克莫司的释放剂型,其口服给药释放两种或更多量的他克莫司,第一批量的他克莫司基本上立即在0-2小时内立即从立即释放剂量单位释放,之后是从约 1-10小时,其中基本上没有量的他克莫司从剂型中释放出来,之后第二量的他克莫司被释放,其中所述第二量从延迟释放剂量单位释放, 在0-2小时内或超过延迟释放剂量单位从其初始释放约2-12小时的时间段内。 剂型还可包含额外量的他克莫司以提供他克莫司的额外脉冲。 他克莫司的剂型表现出改善的生物利用度和减少通量或波动超过现有组合的他克莫司。 还描述了制备剂型的方法。
    • 4. 发明申请
    • COMPOSITIONS AND METHODS FOR IMPROVED DELIVERY OF BUPROPION
    • 用于改进交付运输的组合物和方法
    • WO2009050726A3
    • 2009-06-25
    • PCT/IN2008000337
    • 2008-05-28
    • PANACEA BIOTEC LTDSINGH AMARJITSINGH SARABJITPRASAD KORLAKUNTEJAIN RAJESH
    • SINGH AMARJITSINGH SARABJITPRASAD KORLAKUNTEJAIN RAJESH
    • A61K9/50A61K9/16A61K31/137
    • A61K31/137A61K9/0043A61K9/141A61K9/48A61K9/5021
    • The present invention provides a pharmaceutical composition comprising micronized bupropion having controlled particle size in the range between 1-60 µm. The pharmaceutical composition of the present invention comprises micronized bupropion having median particle size less than 40 micron, which exhibits outstanding bioavailability via nasal and pulmonary route even without any need for blending the micronized bupropion with large carrier particles. The composition of the present invention comprises micronized bupropion -and one or more pharmaceutically acceptable carriers, surfactants, a dispersing agents, or dispersants, which can be administered in an aerosol formulation as a dry powder for nasal and pulmonary inhalation. Particularly, the composition of the present invention for nasal delivery comprises bioadhesive microparticles of bupropion and carbohydrates like pullulan to prevent and treat diseases such as depression, premenstrual syndrome, premature ejaculation and as an aid to smoking cessation. The invention also provides a process of preparing the compositions of the present invention.
    • 本发明提供一种药物组合物,其包含微粒化的安非他酮,其控制粒度在1-60μm之间。 本发明的药物组合物包含中值粒度小于40微米的微粉化安非他酮,即使不需要将微粉化的安非他酮与大载体颗粒混合,也可以通过鼻和肺途径表现出优异的生物利用度。 本发明的组合物包含微粉化的安非他酮和一种或多种药学上可接受的载体,表面活性剂,分散剂或分散剂,其可以作为用于鼻吸入和肺部吸入的干粉在气溶胶制剂中施用。 特别地,用于鼻腔输送的本发明的组合物包括安非他酮的生物粘附微粒和诸如支链淀粉的碳水化合物,以预防和治疗诸如抑郁症,经前期综合征,早泄以及作为戒烟的辅助之类的疾病。 本发明还提供了制备本发明组合物的方法。