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    • 4. 发明授权
    • Quick release pharmaceutical compositions of drug substances
    • 药物快速释放药物组合物
    • US08231899B2
    • 2012-07-31
    • US10758233
    • 2004-01-13
    • Poul Egon BertelsenNiels Gjørløv HansenHermann RuckendorferShigeru Itai
    • Poul Egon BertelsenNiels Gjørløv HansenHermann RuckendorferShigeru Itai
    • A61K9/20A61K9/14
    • A61K9/1617A61K9/1611A61K9/1652
    • The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance) to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a very low solubitity under acidic conditions, i.e. under conditions similar to those present in the stomach and/or drug substances which have a pKa value below about 5.5 such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles passes through sieves 180 μm and the powder is contacted with an aqueous medium to form a particulate composition, which has such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through sieve 180 μm. Furthermore, the composition, when tested in accordance with the dissolution method (I) defined herein employing 0.07 N hydrochloric acid as dissolution medium, releases at least about 50% w/w of the active substance within the first 20 min of the test.
    • 本发明涉及用于给予治疗和/或预防有效量的活性物质(药物物质)以获得治疗和/或预防效果相对快速或快速发作的口服释放药物组合物。 包含在根据本发明的调释释放药物组合物中的药物物质合适地是在酸性条件下具有非常低的溶解度的药物物质,即在与pKa值低于pKa值的胃和/或药物物质中存在的条件相似的条件下 约5.5,例如在约4至约5的范围内。该组合物基于包含治疗和/或预防活性物质的粉末,并且具有如下的粒径:当粉末进行筛分分析时,则 至少约90%w / w的颗粒通过180μm的筛子,并且粉末与水性介质接触以形成颗粒组合物,其具有这样的颗粒尺寸,即当颗粒组合物进行筛分分析时, 颗粒的至少约50%w / w通过筛180μm。 此外,当根据本文定义的溶解方法(I)使用0.07N盐酸作为溶解介质测试时,组合物在试验的最初20分钟内释放至少约50%w / w的活性物质。
    • 5. 发明申请
    • Quick release pharmaceutical compositions of drug substances
    • 药物快速释放药物组合物
    • US20050147668A1
    • 2005-07-07
    • US10758233
    • 2004-01-13
    • Poul BertelsenNiels HansenHermann RuckendorferShigeru Itai
    • Poul BertelsenNiels HansenHermann RuckendorferShigeru Itai
    • A61K9/16A61K9/20
    • A61K9/1617A61K9/1611A61K9/1652
    • The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance) to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a very low solubitity under acidic conditions, i.e. under conditions similar to those present in the stomach and/or drug substances which have a pKa value below about 5.5 such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles passes through sieves 180 μm and the powder is contacted with an aqueous medium to form a particulate composition, which has such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through sieve 180 μm. Furthermore, the composition, when tested in accordance with the dissolution method (1) defined herein employing 0.07 N hydrochloric acid as dissolution medium, releases at least about 50% w/w of the active substance within the first 20 min of the test
    • 本发明涉及一种用于给予治疗和/或预防有效量的活性物质(药物)以获得相对快速或快速起效的治疗和/或预防效果的口服释放药物组合物。该药物 根据本发明的改性释放药物组合物中所含的物质适宜地是在酸性条件下具有非常低的溶解性的药物物质,即在与胃和/或药物物质中存在pK < 低于约5.5,例如在约4至约5的范围内。该组合物基于包含治疗和/或预防活性物质的粉末,并且具有这样的粒径,即当粉末经受 进行筛分分析,然后至少约90%w / w的颗粒通过筛子180μm,粉末与水性介质接触以形成 颗粒组合物具有这样的颗粒尺寸,当颗粒组合物进行筛分分析时,至少约50%w / w的颗粒通过筛子180μm。 此外,当根据本文定义的溶解方法(1)使用0.07N盐酸作为溶解介质测试时,组合物在试验的最初20分钟内释放至少约50%w / w的活性物质
    • 6. 发明授权
    • Quick release pharmaceutical compositions of drug substances
    • 药物快速释放药物组合物
    • US06713089B1
    • 2004-03-30
    • US09786864
    • 2001-07-10
    • Poul BertelsenNiels Gjørløv HansenHermann RuckendorferShigeru Itai
    • Poul BertelsenNiels Gjørløv HansenHermann RuckendorferShigeru Itai
    • A61K914
    • A61K9/2009A61K9/1611
    • The present invention relates to an oral modified release pharmaceutical composition for the administration of a therapeutically and/or prophylactically effective amount of an active substance (a drug substance), to obtain a relatively fast or quick onset of the therapeutic and/or prophylactic effect. The drug substances contained in a modified release pharmaceutical composition according to the invention are suitably a drug substance which has a pKa value below about 5, such as in a range of from about 4 to about 5. The composition is based on a powder comprising a therapeutically and/or prophylactically active substance and has such a particle size that: when the powder is subjected to a sieve analysis, then at least about 90% w/w of the particles pass through a 180 micron sieve, and when the powder is contacted with an aqueous medium to form a particulate composition, which as such a particle size that when the particulate composition is subjected to a sieve analysis, then at least about 50% w/w of the particles passes through a 180 micron sieve. Further more, the composition, when tested in accordance with the dissolution method (I) defines herein, employing 0.07 HCl as dissolution medium, release at least about 50% w/w of the active substance within the first 20 minutes of the test.
    • 本发明涉及用于给予治疗和/或预防有效量的活性物质(药物物质)的口服释放药物组合物,以获得治疗和/或预防效果的相对快速或快速的发作。 包含在根据本发明的改性释放药物组合物中的药物物质合适地是pKa值低于约5,例如在约4至约5范围内的药物。该组合物基于包含 治疗和/或预防活性物质,并且具有这样的粒度:当粉末进行筛分分析时,然后至少约90%w / w的颗粒通过180微米筛,并且当粉末接触时 与水性介质形成颗粒组合物,其颗粒大小使得当颗粒组合物进行筛分分析时,至少约50%w / w的颗粒通过180微米筛。 此外,当根据本文的溶解方法(I)测试时,组合物使用0.07HCl作为溶解介质,在测试的前20分钟内释放至少约50%w / w的活性物质。