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公开(公告)号：US08486456B2
公开(公告)日：2013-07-16
申请号：US11997256
申请日：2006-08-08
IPC分类号： A61K9/14 , A61K31/497
CPC分类号： A61K9/10 , A61K9/146 , A61K31/496
摘要： A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>ΔHtr (1) (wherein ΔHtr represents the endotherm (J/g) accompanying a transition at about 240° C). The solid dispersion product shows an improved bioavailability.
摘要翻译： 包含伊曲康唑和羟丙基甲基纤维素的固体分散产物，其满足式0.35>ΔHtr（1）（其中ΔHtr表示伴随在约240℃的转变的吸热（J / g））。 固体分散产物显示出改进的生物利用度。
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公开(公告)号：US20090214656A1
公开(公告)日：2009-08-27
申请号：US11997256
申请日：2006-08-08
IPC分类号： A61K9/14 , A61K31/496
CPC分类号： A61K9/10 , A61K9/146 , A61K31/496
摘要： A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>ΔHtr (1) (wherein ΔHtr represents the endotherm (J/g) accompanying a transition at about 240° C). The solid dispersion product shows an improved bioavailability.
摘要翻译： 包含伊曲康唑和羟丙基甲基纤维素的固体分散产物，其满足式0.35>ΔHtr（1）（其中ΔHtr表示伴随在约240℃的转变的吸热（J / g））。 固体分散产物显示出改进的生物利用度。
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公开(公告)号：US09060936B2
公开(公告)日：2015-06-23
申请号：US13165398
申请日：2011-06-21
CPC分类号： A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1652
摘要： A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>ΔHtr (1) (wherein AHtr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.
摘要翻译： 包含有效量的一种或多种活性成分和有效量的一种或多种羟基甲基纤维素的固体分散产物，其满足式0.35>＆Dgr; Htr（1）（其中AHtr表示吸热（J / g ）伴随着在约240℃的转变）。 固体分散体产品用于通过口服给予有需要的患者来制备具有改善的所述一种或多种活性成分的生物利用度的剂型。
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公开(公告)号：US20110311595A1
公开(公告)日：2011-12-22
申请号：US13165398
申请日：2011-06-21
CPC分类号： A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1652
摘要： A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>ΔHtr (1) (wherein AHtr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.
摘要翻译： 包含有效量的一种或多种活性成分和有效量的一种或多种羟基甲基纤维素的固体分散产物，其满足式0.35>＆Dgr; Htr（1）（其中AHtr表示吸热（J / g ）伴随着在约240℃的转变）。 固体分散体产品用于通过口服给予有需要的患者来制备具有改善的所述一种或多种活性成分的生物利用度的剂型。
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公开(公告)号：US20090028938A1
公开(公告)日：2009-01-29
申请号：US11997325
申请日：2006-08-08
CPC分类号： A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1652
摘要： A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>ΔHtr (1) (wherein ΔHtr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.
摘要翻译： 包含有效量的一种或多种活性成分和有效量的一种或多种羟丙基甲基纤维素的固体分散产物，其满足式0.35>ΔHtr（1）（其中DeltaHtr表示伴随的吸热（J / g）） 在约240℃的转变）。 固体分散体产品用于通过口服给予有需要的患者来制备具有改善的所述一种或多种活性成分的生物利用度的剂型。
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6.发明申请公开(公告)号：US20080107733A1
公开(公告)日：2008-05-08
申请号：US11597799
申请日：2005-05-30
IPC分类号： A61K9/14
CPC分类号： A61K9/143 , A61K9/146 , A61K9/2095
摘要： A solid dosage form having a matrix with at least one active compound dispersed homogeneously in the matrix, which is obtainable by melting a powder mixture, wherein the powder mixture comprises at least one thermoplastic binder and a combination of highly disperse silica and at least one inorganic pigment, is described. The co-use of the highly disperse silica and the inorganic pigments leads to better flow properties of the powder mixture, has the effect of a faster release of the active compound from the dosage forms obtained, and imparts a visually pleasing appearance to the dosage forms. A process for the preparation of the dosage form is also described.
摘要翻译： 一种固体剂型，其具有通过熔融粉末混合物可获得的具有均匀分散在基质中的至少一种活性化合物的基质，其中所述粉末混合物包含至少一种热塑性粘合剂和高分散二氧化硅与至少一种无机物的组合 颜料。 高度分散的二氧化硅和无机颜料的共同使用导致粉末混合物的更好的流动性质，具有从所获得的剂型中更快释放活性化合物的作用，并赋予剂型视觉上令人满意的外观 。 还描述了用于制备剂型的方法。
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公开(公告)号：US20090302493A1
公开(公告)日：2009-12-10
申请号：US12279385
申请日：2007-03-12
申请人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull , Gunther Berndl
发明人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull , Gunther Berndl
IPC分类号： B29C47/60
CPC分类号： A61J3/00 , A61K9/2027 , A61K9/2095 , A61K9/2893 , A61K47/32 , B01F7/0045 , B29C35/02 , B29C48/022 , B29C48/03 , B29C48/04 , B29C48/08 , B29C48/2564 , B29C48/268 , B29C48/2886 , B29C48/29 , B29C48/395 , B29C48/40 , B29C48/402 , B29C48/404 , B29C48/505 , B29C48/52 , B29C48/54 , B29C48/55 , B29C48/56 , B29C48/57 , B29C48/625 , B29C48/65 , B29C48/67 , B29C48/76 , B29C48/83 , B29C48/865 , B29C48/875 , B29C48/906 , B29C48/914 , B29K2105/0005 , B29K2105/0035 , B29K2105/0038 , B29K2105/0064 , B29K2105/16
摘要： A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (R; A), (ii) at least one reverse-flight section (D), and (iii) a discharging section (E), wherein the processing elements defining the reverse-flight section (R; D) comprise at least one reverse-flight element (14) which is based on a screw-type element having a conveying direction being opposite to the general conveying direction of the extruder.
摘要翻译： 一种制备活性成分的固体分散体的方法，包括将活性成分和基质形成剂加入到挤出机中并形成均匀的挤出物，其中挤出机包括至少两个旋转轴（2），每个轴 2）承载沿轴向布置的多个处理元件，处理元件限定（i）进料和输送段（R; A），（ii）至少一个反向飞行段（D）和（iii） ）排出部分（E），其中限定反向飞行部分（R; D）的处理元件包括至少一个反向飞行元件（14），该反向飞行元件基于螺旋型元件，其具有与 挤出机的一般输送方向。
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公开(公告)号：US09174944B1
公开(公告)日：2015-11-03
申请号：US13328121
申请日：2011-12-16
IPC分类号： C07D239/10 , A61K31/513
CPC分类号： C07D213/64 , C07D239/10
摘要： This invention relates to novel crystalline lopinavir/surfactant adducts, methods for their preparation, therapeutic uses of those crystalline lopinavir/surfactant adducts, and pharmaceutical compositions containing them or made from them.
摘要翻译： 本发明涉及新的结晶洛匹那韦/表面活性剂加合物，其制备方法，那些结晶洛匹那韦/表面活性剂加合物的治疗用途，以及含有它们或由它们制备的药物组合物。
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公开(公告)号：US20090311414A1
公开(公告)日：2009-12-17
申请号：US12279415
申请日：2007-03-12
申请人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull
发明人： Thomas Kessler , Jörg Breitenbach , Christoph Schmidt , Matthias Degenhardt , Jörg Rosenberg , Harald Krull
CPC分类号： A61J3/00 , A61K9/2027 , A61K9/2095 , A61K9/2893 , A61K47/32 , B01F7/0045 , B29C35/02 , B29C48/022 , B29C48/03 , B29C48/04 , B29C48/08 , B29C48/2564 , B29C48/268 , B29C48/2886 , B29C48/29 , B29C48/395 , B29C48/40 , B29C48/402 , B29C48/404 , B29C48/505 , B29C48/52 , B29C48/54 , B29C48/55 , B29C48/56 , B29C48/57 , B29C48/625 , B29C48/65 , B29C48/67 , B29C48/76 , B29C48/83 , B29C48/865 , B29C48/875 , B29C48/906 , B29C48/914 , B29K2105/0005 , B29K2105/0035 , B29K2105/0038 , B29K2105/0064 , B29K2105/16
摘要： A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element (11, 12, 13) that is derived from a screw type element (FIG. 2).
摘要翻译： 一种制备活性成分的固体分散体的方法，包括将活性成分和基质形成剂加入到挤出机中并形成均匀的挤出物，其中挤出机包括至少两个旋转轴（2），每个轴 2）承载多个沿轴向布置的处理元件，处理元件限定（i）进料和输送段（A），（ii）至少一个混合段（B），和（iii）排出段 （E），其中限定混合部分（B）的处理元件包括从螺杆型元件（图2）导出的混合元件（11,12,13）。
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10.发明申请FORMULATION COMPRISING FENOFIBRIC ACID, A PHYSIOLOGICALLY ACCEPTABLE SALT OR DERIVATIVE THEREOF 审中-公开包含非洲酸，生理上可接受的盐或其衍生物的配方公开(公告)号：US20120046360A1
公开(公告)日：2012-02-23
申请号：US13216888
申请日：2011-08-24
IPC分类号： A61K31/216 , A61P3/06 , A61K31/192
CPC分类号： A61K31/56 , A61K9/146 , A61K9/1652 , A61K9/2054 , A61K31/192 , A61K31/205 , A61K31/216 , A61K31/495 , A61K31/58
摘要： A formulation comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients is described. Fenofibric acid, the physiologically acceptable salt or derivative thereof is preferably in the form of a molecular dispersion in these formulations. An advantageous process for their preparation, in particular by melt extrusion, and the use of this formulation for oral administration of fenofibric acid, a physiologically acceptable salt or derivative thereof are likewise described.
摘要翻译： 包含i）非诺贝酸，其生理学上可接受的盐或其衍生物和任选的其它活性物质的制剂，ii）包含至少一种肠溶粘合剂和任选地iii）其它生理上可接受的赋形剂的粘合剂组分。 非诺贝酸，其生理学上可接受的盐或衍生物优选为这些制剂中分子分散体的形式。 同样描述了其制备的有利方法，特别是通过熔融挤出，以及该制剂用于口服非诺贝酸，其生理学上可接受的盐或其衍生物的用途。
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