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1. 发明申请

WO2011089202A1 METHOD FOR EVALUATING THE SOLUBILITY OF A CRYSTALLINE SUBSTANCE IN A POLYMER 审中-公开
标题翻译：评估聚合物中晶体物质的溶解性的方法
公开(公告)号：WO2011089202A1
公开(公告)日：2011-07-28
申请号：PCT/EP2011/050792
申请日：2011-01-21
申请人： ABBOTT GMBH & CO. KG , ZHANG, Geoff G. Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
发明人： ZHANG, Geoff G. Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
IPC分类号： G01N25/48 , G01N33/15
CPC分类号： G01N33/15 , G01N25/4866 , G01N2013/006
摘要： A method for evaluating the solubility of a crystalline substance in a polymer comprises a) providing at least one sample of an intimate crystalline substance/polymer mixture at a predetermined crystalline substance concentration; b) annealing the sample at a constant temperature T a for a period of time; c) heating the annealed sample while recording the heat flux over time by DSC; d) identifying a DSC dissolution endotherm in the recorded heat flux, if any; e) considering the crystalline substance concentration as a concentration above the crystalline substance solubility in the polymer at temperature T a when there is a DSC dissolution endotherm identified, and considering the crystalline substance concentration as a concentration less than or equal to the crystalline substance solubility in the polymer at temperature T a when there is no DSC dissolution endotherm identified. Thus, the method yields the upper and lower bounds for the equilibrium solubility at a given temperature or the upper and lower bounds for the equilibrium solubility temperature at a given crystalline substance concentration. The method improves accuracy of measurement near the glass transition temperature.
摘要翻译：用于评价结晶物质在聚合物中的溶解度的方法包括a）以预定的结晶物质浓度提供至少一种紧密结晶物质/聚合物混合物的至少一个样品; b）在恒温Ta下将样品退火一段时间; c）加热退火样品，同时通过DSC随时间记录热通量; d）识别记录的热通量中的DSC溶解吸热（如果有的话）; e）当确定DSC溶解吸热时，考虑结晶物质浓度高于结晶物质在聚合物中的溶解度的浓度，考虑到结晶物质浓度小于或等于结晶物质溶解度的浓度聚合物在温度Ta时没有DSC溶解吸热确定。因此，该方法产生在给定温度下的平衡溶解度的上限和下限，或者给定在给定结晶物质浓度下的平衡溶解度温度的上限和下限。该方法提高玻璃化转变温度附近的测量精度。

2. 发明申请

WO2007085024A2 DOSAGE FORM AND METHOD FOR THE DELIVERY OF DRUGS OF ABUSE 审中-公开
标题翻译：用于输送药物的剂型和方法
公开(公告)号：WO2007085024A2
公开(公告)日：2007-07-26
申请号：PCT/US2007/060864
申请日：2007-01-22
申请人： ABBOTT GMBH & CO. KG , BREITENBACH, Jorg , LANDER, Ute , ROSENBERG, Jorg , MAEGERLEIN, Markus , WOEHRLE, Gerd
发明人： BREITENBACH, Jorg , LANDER, Ute , ROSENBERG, Jorg , MAEGERLEIN, Markus , WOEHRLE, Gerd
CPC分类号： A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2095 , A61K31/485
摘要： A dosage form and method for the delivery of drugs, particularly drugs of abuse, characterized by resistance to solvent extraction, tampering, crushing, or grinding, and providing an initial burst of release of drug followed by a prolonged period of controllable drug release.
摘要翻译：用于递送药物，特别是滥用药物的剂型和方法，其特征在于耐溶剂萃取，篡改，破碎或研磨，以及提供药物释放的初始爆发，然后是延长的可控药物释放时间。

3. 发明申请

WO2009135799A2 METHOD FOR EVALUATING THE SOLUBILITY OF A CRYSTALLINE SUBSTANCE IN A POLYMER 审中-公开
标题翻译：评估聚合物中晶体物质的溶解性的方法
公开(公告)号：WO2009135799A2
公开(公告)日：2009-11-12
申请号：PCT/EP2009/055233
申请日：2009-04-29
申请人： ABBOTT GMBH & CO. KG , ZHANG, Geoff, G., Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
发明人： ZHANG, Geoff, G., Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
IPC分类号： G01N33/15
CPC分类号： G01N33/15 , G01N25/4866
摘要： A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning Calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices. The method relies on the detection of the dissolution endpoint of a drug/polymer mixture prepared by cryomilling.
摘要翻译：提高难溶性药物的生物利用度的可行策略是使用无定形固体代替药物制剂中更常用的结晶固体。然而，无定形固体物理上是元稳定的，并且倾向于回复到它们的结晶对应物。稳定无定形药物抗结晶的有效方法是将其分散在聚合物基质中。药物在所选聚合物中的溶解度限定了药物负载的上限，而没有结晶的风险。测量药物在聚合物中的溶解度已经是科学和技术挑战，因为聚合物的高粘度使得难以实现溶解度平衡，并且因为药物重要的药物/聚合物分散体是随时间经历结构松弛的玻璃。本发明提供了一种基于差示扫描量热法（DSC）测量结晶药物在聚合物基质中的溶解度的方法。该方法依赖于通过冷冻法制备的药物/聚合物混合物的溶解终点的检测。

4. 发明申请

WO2004032903A3 METHOD FOR PRODUCING SOLID GALENIC FORMULATIONS USING A CROSSLINKED NON-THERMOPLASTIC CARRIER 审中-公开
标题翻译： [固体剂型的使用网络非热塑性载体
公开(公告)号：WO2004032903A3
公开(公告)日：2004-11-11
申请号：PCT/EP0311205
申请日：2003-10-09
申请人： ABBOTT GMBH & CO KG , ROSENBERG JOERG , BERNDL GUNTHER , MAEGERLEIN MARKUS
发明人： ROSENBERG JOERG , BERNDL GUNTHER , MAEGERLEIN MARKUS
IPC分类号： A61K9/16 , A61K9/20 , A61K31/513
CPC分类号： A61K31/513 , A61K9/2009 , A61K9/2013 , A61K9/2027 , A61K9/2095
摘要： The invention concerns a method for producing solid galenic formulations which consists in: forming a processable paste comprising a) 50 to 99.4 wt. % of at least one non-thermoplastic carrier, b) 0.5 to 30 wt. % of at least an adjuvant selected among thermoplastic polymers, lipids, sugar alcohols and solubilizing agents, c) 0.1 to 49.5 wt. % of at least one active principle, at a temperature not less than the softening temperature of the adjuvant but rising to at least 70 DEG C; then in cooling the resulting paste. Said solid galenic formulations quickly disintegrate in an aqueous medium.
摘要翻译：用于制备固体剂型，其中可模制组合物，其包含：a）50到至少一个非热塑性载体的5重量99.4％，B）0.5至30重量％的至少一种一％的处理将被描述热塑性聚合物，脂质，糖醇，糖醇衍生物和增溶剂，和c）0.1至49.5重量在10或以上的辅助剂的软化点至少包括一种活性物质，在一定温度下％，但至少70℃的形式，然后冷却。 Dosieirungsformen在含水环境中迅速崩解。

5. 发明申请

WO2007085024A3 DOSAGE FORM AND METHOD FOR THE DELIVERY OF DRUGS OF ABUSE 审中-公开
标题翻译：用于输送药物的剂型和方法
公开(公告)号：WO2007085024A3
公开(公告)日：2008-03-13
申请号：PCT/US2007060864
申请日：2007-01-22
申请人： ABBOTT GMBH & CO KG , BREITENBACH JORG , LANDER UTE , ROSENBERG JORG , MAEGERLEIN MARKUS , WOEHRLE GERD
发明人： BREITENBACH JORG , LANDER UTE , ROSENBERG JORG , MAEGERLEIN MARKUS , WOEHRLE GERD
IPC分类号： A61K9/20 , A61K31/485
CPC分类号： A61K9/2027 , A61K9/2031 , A61K9/2054 , A61K9/2095 , A61K31/485
摘要： A dosage form and method for the delivery of drugs, particularly drugs of abuse, characterized by resistance to solvent extraction, tampering, crushing, or grinding, and providing an initial burst of release of drug followed by a prolonged period of controllable drug release.
摘要翻译：用于递送药物，特别是滥用药物的剂型和方法，其特征在于耐溶剂萃取，篡改，破碎或研磨，以及提供药物释放的初始爆发，然后是延长的可控药物释放时间。

6. 发明申请

WO2006084696A9 PRODUCTION OF DOSAGE FORMS COMPRISING A SOLID DISPERSION OF A MICROCRYSTALLINE AGENT 审中-公开
标题翻译：剂型的用微结晶活性的固体分散体制造
公开(公告)号：WO2006084696A9
公开(公告)日：2007-10-25
申请号：PCT/EP2006001164
申请日：2006-02-09
申请人： ABBOTT GMBH & CO KG , ROSENBERG JOERG , MAEGERLEIN MARKUS , LIEPOLD BERND , BREITENBACH JOERG
发明人： ROSENBERG JOERG , MAEGERLEIN MARKUS , LIEPOLD BERND , BREITENBACH JOERG
IPC分类号： A61K9/14 , A61K9/00
CPC分类号： A61K9/146 , A61K9/145
摘要： Disclosed is a method for producing dosage forms comprising a solid dispersion of a microcrystalline agent. According to said method, a thermoplastic polymer having a minimum glass transition temperature Tg of 40 o C is melted, and an agent is homogeneously dissolved in the melt; crystallization of the agent is initiated in the obtained mass; and the mass is cooled. Crystallization of the agent can be initiated by adding a nonsolvent, seed crystals of the agent, or a derivatization reagent. Crystallization can also be initiated by maintaining the mass at a certain temperature for a sufficient amount of time, said temperature being lower than the temperature at which the agent can be fully dissolved in the mass.
摘要翻译：公开了一种用于剂型，其包含熔化具有至少40℃的玻璃化转变温度Tg℃的热塑性聚合物和触发均匀熔融活性成分的微晶的活性成分的固体分散体的制备方法; 在活性成分的所得到的质量开始结晶; 和物料冷却。活性成分的结晶，通过添加非溶剂，通过将活性成分或衍生试剂的晶种引发。另外一个可以通过保持有足够的时间的质量在比在该活性物质是在所述组合物完全可溶于温度低的温度下开始结晶。

7. 发明申请

WO2009135799A3 METHOD FOR EVALUATING THE SOLUBILITY OF A CRYSTALLINE SUBSTANCE IN A POLYMER 审中-公开
标题翻译：评估聚合物中晶体物质的溶解性的方法
公开(公告)号：WO2009135799A3
公开(公告)日：2010-01-28
申请号：PCT/EP2009055233
申请日：2009-04-29
申请人： ABBOTT GMBH & CO KG , ZHANG GEOFF G Z , YU LIAN , TAO JING , SUN YE , MAEGERLEIN MARKUS
发明人： ZHANG GEOFF G Z , YU LIAN , TAO JING , SUN YE , MAEGERLEIN MARKUS
IPC分类号： G01N33/15 , G01N25/48
CPC分类号： G01N33/15 , G01N25/4866
摘要： A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning Calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices. The method relies on the detection of the dissolution endpoint of a drug/polymer mixture prepared by cryomilling.
摘要翻译：提高难溶性药物的生物利用度的可行策略是使用无定形固体代替药物制剂中更常用的结晶固体。然而，无定形固体物理上是元稳定的，并且倾向于回复到它们的结晶对应物。稳定无定形药物抗结晶的有效方法是将其分散在聚合物基质中。药物在所选聚合物中的溶解度限定了药物负载的上限，而没有结晶的风险。测量药物在聚合物中的溶解度已经是科学和技术挑战，因为聚合物的高粘度使得难以实现溶解度平衡，并且因为药物重要的药物/聚合物分散体是随时间经历结构松弛的玻璃。本发明提供了一种基于差示扫描量热法（DSC）测量结晶药物在聚合物基质中的溶解度的方法。该方法依赖于通过冷冻法制备的药物/聚合物混合物的溶解终点的检测。

8. 发明申请

WO2008037809A1 TRANSMUCOSAL ADMINISTRATION OF FIBRATE COMPOUNDS AND DELIVERY SYSTEM THEREFOR 审中-公开
标题翻译：纤维素化合物的转运管理及其输送系统
公开(公告)号：WO2008037809A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/060347
申请日：2007-09-28
申请人： Abbott GmbH & Co. KG , WESTEDT, Ulrich , SCHNEIDER, Katrin , STEIGER, Norbert , HACH, Harald , RODE, Marc , RIEPEN, Takeo , MAEGERLEIN, Markus , ROSENBERG, Jörg , BREITENBACH, Jörg , MARSH, Kennan
发明人： WESTEDT, Ulrich , SCHNEIDER, Katrin , STEIGER, Norbert , HACH, Harald , RODE, Marc , RIEPEN, Takeo , MAEGERLEIN, Markus , ROSENBERG, Jörg , BREITENBACH, Jörg , MARSH, Kennan
IPC分类号： A61K9/00 , A61K9/70 , A61K31/216
CPC分类号： A61K9/7007 , A61K9/0056 , A61K9/006 , A61K31/216
摘要： The invention provides a method and a delivery system for the administration of a fibrate compound to a subject in need thereof by bringing the delivery system into contact with a mucous membrane of the subject for a time sufficient to deliver a therapeutically effective amount of the fibrate compound. The delivery system is preferably film-shaped and comprises a solid dispersion product wherein the fibrate compound is distributed homogenously in a polymer matrix.
摘要翻译：本发明提供了一种方法和递送系统，用于通过使输送系统与受试者的粘膜接触一段足以递送治疗有效量的贝特类化合物的时间，将需要的对象给予贝特类化合物。递送系统优选是膜状的并且包含固体分散体产物，其中所述贝特类化合物在聚合物基质中均匀分布。

9. 发明申请

WO2007017248A2 ITRACONAZOLE COMPOSITIONS WITH IMPROVED BIOAVAILABILITY 审中-公开
标题翻译：具有改善生物利用度的异烟酸组合物
公开(公告)号：WO2007017248A2
公开(公告)日：2007-02-15
申请号：PCT/EP2006007839
申请日：2006-08-08
申请人： ABBOTT GMBH & CO KG , BARRIER THERAPEUTICS , BERNDL GUNTHER , DEGENHARDT MATTHIAS , MAEGERLEIN MARKUS , DISPERSYN GERRIT
发明人： BERNDL GUNTHER , DEGENHARDT MATTHIAS , MAEGERLEIN MARKUS , DISPERSYN GERRIT
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 > ?H tr (1) (wherein ?H tr 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体产物，其满足式0.35>ηH（1）（其中ΔHT tr）表示伴随的吸热（J / g）在约240℃的过渡）。固体分散产物显示出改进的生物利用度。

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