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1. 发明申请

WO2004006959A1 LIQUID DOSAGE COMPOSITIONS OF STABLE NANOPARTICULATE ACTIVE AGENTS 审中-公开
标题翻译：稳定的纳米颗粒活性剂的液体组合物
公开(公告)号：WO2004006959A1
公开(公告)日：2004-01-22
申请号：PCT/US2003/022187
申请日：2003-07-16
申请人： ELAN PHARMA INTERNATIONAL, LTD , BOSCH, H., William , HILBORN, Matthew, R. , HOVEY, Douglas, C. , KLINE, Laura, J. , LEE, Robert, W. , PRUITT, John, D. , RYDE, Niels, P. , RYDE, Tuula, A. , XU, Shuqian
发明人： BOSCH, H., William , HILBORN, Matthew, R. , HOVEY, Douglas, C. , KLINE, Laura, J. , LEE, Robert, W. , PRUITT, John, D. , RYDE, Niels, P. , RYDE, Tuula, A. , XU, Shuqian
IPC分类号： A61K47/02
CPC分类号： A61K9/0095 , A61K9/143 , A61K9/145 , A61K9/146 , A61K31/192 , A61K31/57 , A61K31/573 , A61K31/58
摘要： The present invention relates to liquid dosage compositions of stable nanoparticulate active agents. The liquid dosage compositions of the invention include osmotically active crystal growth inhibitors that stabilize the nanoparticulate active agents against crystal and particle size growth of the active agent.
摘要翻译：本发明涉及稳定的纳米颗粒活性剂的液体剂量组合物。本发明的液体剂量组合物包括渗透活性晶体生长抑制剂，其稳定纳米颗粒活性剂以防止活性剂的晶体和粒度增长。

2. 发明申请

WO2008054508A3 STABLE NANOSIZED AMORPHOUS DRUG 审中-公开
标题翻译：稳定的纳米非晶药物
公开(公告)号：WO2008054508A3
公开(公告)日：2008-11-06
申请号：PCT/US2007009264
申请日：2007-04-13
申请人： ALZA CORP , WEI MIN , XU SHUQIAN , LAM ANDREW C
发明人： WEI MIN , XU SHUQIAN , LAM ANDREW C
IPC分类号： A61K9/51 , A61K31/445
CPC分类号： A61K9/146 , A61K9/145 , A61K31/445
摘要： Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core includes a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 50 Deg. C, a glass forming ability less than or equal to about 0.85; and water solubility at 25 Deg. C less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the population of nanoparticles exhibits greater than about six months amorphous stability.
摘要翻译：公开了纳米颗粒群以及制备纳米颗粒群的方法，其中一个或多个纳米颗粒包括：具有小于或等于约2.0微米的有效直径的无定形药物核心，其中所述无定形药物核心基本上无掺杂物，并且其中所述无定形药物核心包括具有满足以下关系的性质的药物：玻璃化转变温度大于或等于约50度。 C，玻璃形成能力小于或等于约0.85; 水溶性25度。小于或等于约1mg / ml; 并且至少一种稳定剂吸附在无定形药物核心的表面上; 并且其中所述纳米颗粒群表现出大于约6个月的无定形稳定性。

3. 发明申请

WO2008002485A3 INCREASED AMORPHOUS STABILITY OF POORLY WATER SOLUBLE DRUGS BY NANOSIZING 审中-公开
公开(公告)号：WO2008002485A3
公开(公告)日：2008-01-03
申请号：PCT/US2007/014585
申请日：2007-06-22
申请人： ALZA CORPORATION , WEI, Min , XU, Shuqian , LAM, Andrew, C.
发明人： WEI, Min , XU, Shuqian , LAM, Andrew, C.
IPC分类号： A61K9/14 , A61K31/00
摘要： Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core comprises a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 30 Deg. C; and water solubility at 25 Deg. C less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the at least one stabilizer is present in an amount effective to provide an amorphous stability of the population of nanoparticles that is approximately equal to or greater than an amorphous stability of an amorphous bulk drug substance comprising the drug, as measured over a period of at least four months.

4. 发明申请

WO2008002485A2 INCREASED AMORPHOUS STABILITY OF POORLY WATER SOLUBLE DRUGS BY NANOSIZING 审中-公开
标题翻译：纳米化增加水溶性难溶性药物的非晶形稳定性
公开(公告)号：WO2008002485A2
公开(公告)日：2008-01-03
申请号：PCT/US2007014585
申请日：2007-06-22
申请人： ALZA CORP , WEI MIN , XU SHUQIAN , LAM ANDREW C
发明人： WEI MIN , XU SHUQIAN , LAM ANDREW C
IPC分类号： A61K9/14 , A61K31/00
CPC分类号： A61K9/145 , A61K9/146
摘要： Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core comprises a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 30 Deg. C; and water solubility at 25 Deg. C less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the at least one stabilizer is present in an amount effective to provide an amorphous stability of the population of nanoparticles that is approximately equal to or greater than an amorphous stability of an amorphous bulk drug substance comprising the drug, as measured over a period of at least four months.
摘要翻译：公开了纳米颗粒群，以及制备纳米颗粒群的方法，其中一个或多个纳米颗粒包括：具有小于或等于约2.0微米的有效直径的无定形药物核，其中无定形药物核是基本上不含掺杂剂，并且其中所述无定形药心包含具有满足以下关系的性质的药物：玻璃化转变温度大于或等于约30℃。 C; 和在25℃下的水溶性。 C小于或等于约1mg / ml; 和至少一种吸附在无定形药心表面上的稳定剂; 并且其中所述至少一种稳定剂以有效提供所述纳米颗粒群的无定形稳定性的量存在，所述无定形稳定性近似等于或大于包含所述药物的无定形原料药的无定形稳定性，至少四个月。

5. 发明申请

WO2008054508A2 STABLE NANOSIZED AMORPHOUS DRUG 审中-公开
标题翻译：稳定的纳米非晶药物
公开(公告)号：WO2008054508A2
公开(公告)日：2008-05-08
申请号：PCT/US2007/009264
申请日：2007-04-13
申请人： ALZA CORPORATION , WEI, Min , XU, Shuqian , LAM, Andrew, C.
发明人： WEI, Min , XU, Shuqian , LAM, Andrew, C.
CPC分类号： A61K9/146 , A61K9/145 , A61K31/445
摘要： Disclosed is a population of nanoparticles, together with methods of making a population of nanoparticles, wherein one or more of the nanoparticles includes: an amorphous drug core having an effective diameter less than or equal to about 2.0 microns, wherein the amorphous drug core is substantially free of dopant, and wherein the amorphous drug core includes a drug with properties that satisfy the following relationships: a glass transition temperature greater than or equal to about 50 Deg. C, a glass forming ability less than or equal to about 0.85; and water solubility at 25 Deg. C less than or equal to about 1 mg/ml; and at least one stabilizer adsorbed on a surface of the amorphous drug core; and wherein the population of nanoparticles exhibits greater than about six months amorphous stability.
摘要翻译：公开了纳米颗粒群体以及制备纳米颗粒群体的方法，其中一个或多个纳米颗粒包括：具有小于或等于约2.0微米的有效直径的无定形药物核心其中所述无定形药心基本上不含掺杂剂，并且其中所述无定形药心包括具有满足以下关系的性质的药物：玻璃化转变温度大于或等于约50℃。 C，玻璃形成能力小于或等于约0.85; 和在25℃下的水溶性。 C小于或等于约1mg / ml; 和至少一种吸附在无定形药心表面上的稳定剂; 并且其中纳米颗粒群表现出大于约六个月的非晶稳定性。

6. 发明申请

WO2004006959A8 LIQUID DOSAGE COMPOSITIONS OF STABLE NANOPARTICULATE ACTIVE AGENTS 审中-公开
标题翻译：稳定的纳米颗粒活性剂的液体组合物
公开(公告)号：WO2004006959A8
公开(公告)日：2005-03-31
申请号：PCT/US0322187
申请日：2003-07-16
申请人： ELAN PHARMA INT LTD , BOSCH H WILLIAM , HILBORN MATTHEW R , HOVEY DOUGLAS C , KLINE LAURA J , LEE ROBERT W , PRUITT JOHN D , RYDE NIELS P , RYDE TUULA A , XU SHUQIAN
发明人： BOSCH H WILLIAM , HILBORN MATTHEW R , HOVEY DOUGLAS C , KLINE LAURA J , LEE ROBERT W , PRUITT JOHN D , RYDE NIELS P , RYDE TUULA A , XU SHUQIAN
IPC分类号： A61K9/08 , A61K9/00 , A61K9/14 , A61K9/51 , A61K31/192 , A61K31/57 , A61K31/573 , A61K31/58 , A61K47/02 , A61K47/04 , A61K47/06 , A61K47/10 , A61K47/18 , A61K47/26 , A61K47/28 , A61K47/34 , A61K47/38 , A61K47/42 , A61K47/44 , A61K9/10
CPC分类号： A61K9/0095 , A61K9/143 , A61K9/145 , A61K9/146 , A61K31/192 , A61K31/57 , A61K31/573 , A61K31/58
摘要： The present invention relates to liquid dosage compositions of stable nanoparticulate active agents. The liquid dosage compositions of the invention include osmotically active crystal growth inhibitors that stabilize the nanoparticulate active agents against crystal and particle size growth of the active agent.
摘要翻译：本发明涉及稳定的纳米颗粒活性剂的液体剂量组合物。本发明的液体剂量组合物包括渗透活性晶体生长抑制剂，其稳定纳米颗粒活性剂以防止活性剂的晶体和粒度增长。

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