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1. 发明授权

US5227157A Delivery of therapeutic agents 失效
标题翻译：递送治疗剂
公开(公告)号：US5227157A
公开(公告)日：1993-07-13
申请号：US388321
申请日：1989-07-31
申请人： James W. McGinity , Susan L. Ashley
发明人： James W. McGinity , Susan L. Ashley
IPC分类号： A61K9/18 , A61K9/20 , A61K9/70 , A61K31/44
CPC分类号： A61K31/44 , A61K9/204 , A61K9/2068 , A61K9/7023
摘要： The present invention relates to a composition of matter for the time-dependent liberation of therapeutic agents. This composition of matter comprises a polymeric slab and a homogeneously dispersed enzyme which degrades the polymeric slab in the presence of moisture. The therapeutic agent is physically entrapped in the polymeric slab by inclusion during polymerization to form the polymeric slab or by mixture of the therapeutic agent with a liquid form of the polymeric slab and conversion of the liquid to a solid form. The therapeutic agent is not chemically bound to the polymer, and thus release of the agent is immediately effected upon the specific moisture-activated enzymatic degradation of the polymer slab. Moisture for enzymatic activation is provided by the biological surface on which the slab is emplaced, such as the dermal surface. The composition comprises a polymer such as poly (DL-lactide) and an enzyme such as proteinase K together with chlorpheniramine maleate as the therapeutic agent.
摘要翻译：本发明涉及治疗剂时间依赖性释放的物质组合物。这种物质组合物包括聚合物片和均匀分散的酶，其在水分存在下降解聚合物板。治疗剂通过在聚合期间包含物理地包埋在聚合物板中以形成聚合物板，或通过治疗剂与液体形式的聚合物板的混合物，并将液体转化为固体形式。治疗剂不与化合物结合，因此在聚合物板的特定水分激活的酶降解后立即进行试剂的释放。用于酶活化的水分由其上放置板坯的生物表面提供，例如皮肤表面。组合物包含聚合物如聚（DL-丙交酯）和酶如蛋白酶K和马来酸氯苯那敏作为治疗剂。

2. 发明授权

US09192578B2 Hot-melt extrusion of modified release multi-particulates 有权
标题翻译：改性释放多颗粒的热熔挤出
公开(公告)号：US09192578B2
公开(公告)日：2015-11-24
申请号：US12544963
申请日：2009-08-20
申请人： James W. McGinity , Sandra U. Schilling
发明人： James W. McGinity , Sandra U. Schilling
IPC分类号： A61K9/16 , A61K9/20 , A61K31/522 , B29C47/00 , B29K105/00
CPC分类号： A61K9/2077 , A61K9/1641 , A61K9/1694 , A61K9/2081 , A61K31/522 , B29C47/00 , B29C47/0014 , B29K2105/0035
摘要： The present invention includes compositions and methods of making a modified release pharmaceutical formulation and a method of preparation for the embedding of modified release multi-particulates into a polymeric or wax-like matrix. The modified release multi-particulates comprise an effective amount of a therapeutic compound having a known or desired drug-release profile. Modified release multi-particulates may include a polymeric coat or may be incorporated into particle or core material. The polymer matrix comprises a thermoplastic polymer or lipophilic carrier or a mixture thereof that softens or melts at elevated temperature and allows the distribution of the modified release multi-particulates in the polymer matrix during thermal processing. Formulation compounds and processing conditions are selected in a manner to preserve the controlled release characteristics and/or drug-protective properties of the original modified release multi-particulates.
摘要翻译：本发明包括制备改性释放药物制剂的组合物和方法以及将改性释放多颗粒包埋在聚合物或蜡状基质中的制备方法。改性释放多颗粒包含有效量的具有已知或期望的药物释放曲线的治疗化合物。改性释放多颗粒可以包括聚合物涂层或可以结合到颗粒或芯材料中。聚合物基质包括在高温下软化或熔化的热塑性聚合物或亲脂性载体或其混合物，并且允许在热加工期间将改性释放多颗粒分布在聚合物基质中。选择配制化合物和加工条件以保持原来的改性释放多颗粒的控制释放特性和/或药物保护性质。

3. 发明申请

US20090053315A1 Thermo-Kinetic Mixing for Pharmaceutical Applications 有权
标题翻译：药物应用的热动力学混合
公开(公告)号：US20090053315A1
公开(公告)日：2009-02-26
申请号：US12196154
申请日：2008-08-21
申请人： Chris Brough , James W. McGinity , Dave A. Miller , James C. DiNunzio , Robert O. Williams
发明人： Chris Brough , James W. McGinity , Dave A. Miller , James C. DiNunzio , Robert O. Williams
IPC分类号： A61K9/14 , A61K38/02 , A61K31/7088
CPC分类号： A61K31/573 , A61J3/00 , A61J3/07 , A61J3/10 , A61K9/146 , A61K9/1694 , A61K9/2077 , A61K31/343 , A61K31/496 , A61K47/32 , A61K47/38
摘要： Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
摘要翻译：用于制备药物剂型的组合物和方法包括制备药物组合物，其包含一种或多种活性药物成分（API）与一种或多种药学上可接受的赋形剂，通过热动力学复合制成复合材料。将包含一种或多种API的复合材料与一种或多种赋形剂预处理的组合物和方法包括热动力学复合，其包括将所述API与所述赋形剂的热机械加工成复合材料，其中所述复合材料可以通过本领域已知的常规方法进一步加工，热熔挤出，熔融造粒，压缩成型，片剂压缩，胶囊填充，薄膜包衣或注塑成型。

4. 发明授权

US06488963B1 Hot-melt extrudable pharmaceutical formulation 有权
标题翻译：热熔可挤出药物制剂
公开(公告)号：US06488963B1
公开(公告)日：2002-12-03
申请号：US09260694
申请日：1999-03-02
申请人： James W. McGinity , Feng Zhang
发明人： James W. McGinity , Feng Zhang
IPC分类号： A61K910
CPC分类号： A61K9/2031 , A61K9/2095 , Y10S514/953
摘要： The present invention relates to pharmaceutical formulations comprising a hot-melt extrudable mixture of a therapeutic compound and a high molecular weight poly(ethylene oxide) in an essentially non-film like preparation. In some embodiments, the formulation further comprises poly(ethylene glycol). The present invention also includes efficient methods for hot-melt extruding pharmaceutical formulations in essentially non-film preparations.
摘要翻译：本发明涉及包含基本上非膜状制剂中治疗化合物和高分子量聚（环氧乙烷）的热熔可挤出混合物的药物制剂。在一些实施方案中，制剂还包含聚（乙二醇）。本发明还包括在基本上非薄膜制剂中热熔挤出药物制剂的有效方法。

5. 发明授权

US4537689A Oral lubricant for athletic mouth protector 失效
标题翻译：口腔润滑剂用于运动口保护器
公开(公告)号：US4537689A
公开(公告)日：1985-08-27
申请号：US563239
申请日：1983-12-19
申请人： Robert M. Morrow , William A. Kuebker , James W. McGinity
发明人： Robert M. Morrow , William A. Kuebker , James W. McGinity
IPC分类号： A61K8/02 , A61Q11/00 , A63B71/08 , C10M169/00 , C10M5/00 , C10M1/06
CPC分类号： A61Q11/00 , A61K8/02 , A63B71/085
摘要： An oral lubricant effective in reducing the discomfort associated with the wearing of a mouth protector during periods of activity consisting essentially of a thickening agent, a preservative, a flavoring agent, a sweetener, an emulsifier, if needed, and a liquid diluent.
摘要翻译：一种口服润滑剂，其有效地减少了在活性期间与口罩保护剂相关的不适，基本上由增稠剂，防腐剂，调味剂，甜味剂，乳化剂（如果需要）和液体稀释剂组成。

6. 发明申请

US20140039031A1 PHARMACEUTICAL FORMULATIONS OF ACETYL-11-KETO-B-BOSWELLIC ACID, DIINDOLYLMETHANE, AND CURCUMIN FOR PHARMACEUTICAL APPLICATIONS 审中-公开
标题翻译：乙酰基-11-酮酸B-BOSWELLIC酸，DIINDOLYLMETHANE和CURCUMIN用于药物应用的药物制剂
公开(公告)号：US20140039031A1
公开(公告)日：2014-02-06
申请号：US14001098
申请日：2012-02-23
申请人： Chris Brough , Robert O. Williams, III , James W. McGinity , Dave A. Miller , Justin Hughey , Ryan Bennett
发明人： Chris Brough , Robert O. Williams, III , James W. McGinity , Dave A. Miller , Justin Hughey , Ryan Bennett
IPC分类号： A61K31/404 , A61K31/12 , A61K31/19
CPC分类号： A61K31/19 , A61K31/05 , A61K31/12 , A61K31/404
摘要： The present disclosure is directed to compositions and methods for formulating a pharmaceutical dosage form by forming a composition comprising acetyl-11-keto-β-boswellic acid, diindolylmethane, or curcumin with one or more pharmaceutically acceptable excipients for enhanced solubility to increase bioavailability and improve therapeutic efficacy. The composition can be processed by thermo-kinetic compounding along with conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
摘要翻译：本公开涉及通过形成包含乙酰基-11-酮基-β-乳糖酸，二吲哚基甲烷或姜黄素与一种或多种药学上可接受的赋形剂的组合物来配制药物剂型的组合物和方法，以提高溶解度以提高生物利用度并提高治疗功效。组合物可以通过热动力学混合以及本领域已知的常规方法如热熔体挤出，熔融造粒，压塑，压片，胶囊填充，薄膜包衣或注射成型加工。

7. 发明授权

US06488961B1 Effervescent granules and methods for their preparation 有权
标题翻译：泡腾颗粒及其制备方法
公开(公告)号：US06488961B1
公开(公告)日：2002-12-03
申请号：US09468513
申请日：1999-12-21
申请人： Joseph R Robinson , James W. McGinity
发明人： Joseph R Robinson , James W. McGinity
IPC分类号： A61K946
CPC分类号： A61K9/0007 , A61K9/1694
摘要： Disclosed here are effervescent granules having a controllable rate of effervescence. In some embodiments, the such granules comprise an acidic agent, an alkaline agent, a pharmacologically active agent, hot-melt extrudable binder capable of forming a eutectic mixture with the acidic agent and, optionally, a plasticizer. The effervescent granules are made by a hot-melt extrusion process. The present invention also provides a thermal heat process for preparing a pharmacologically active agent containing effervescent granule. In certain aspects, the granules contain pharmacologically active agents such as narcotics, antidiarrheal agents, antiviral agents, anxiolytic agents, a cholesterol lowering agent, an alpha adrenergic blocking agent, a phenanthrene derivative. By way of example, some of the narcotics that may be included in the granules and in the process of preparing the granules include, by way of example: phenanthrene derivatives (e.g., morphine sulfate), and morphine derivatives (e.g., hydromorphone hydrochloride).
摘要翻译：这里公开了具有可控的泡腾速率的泡腾颗粒。在一些实施方案中，这种颗粒包含酸性试剂，碱性试剂，药理学活性剂，能够与酸性试剂形成共晶混合物的热熔可挤出粘合剂和任选的增塑剂。泡腾颗粒通过热熔挤出方法制成。本发明还提供了制备含有泡腾颗粒的药理活性剂的热加工方法。在某些方面，颗粒含有药理学活性剂如麻醉剂，止泻药，抗病毒剂，抗焦虑剂，降胆固醇剂，α肾上腺素能阻断剂，菲衍生物。作为实例，可以包括在颗粒中和在制备颗粒的过程中的一些麻醉剂包括例如：菲衍生物（例如硫酸吗啡）和吗啡衍生物（例如盐酸氢吗啡酮）。

8. 发明授权

US5597849A Stick formulations for topical drug delivery of therapeutic agents and uses thereof 失效
标题翻译：用于局部药物递送治疗剂的制剂及其用途
公开(公告)号：US5597849A
公开(公告)日：1997-01-28
申请号：US345051
申请日：1994-11-14
申请人： James W. McGinity , Thomas G. Gerding , Roland Bodmeier
发明人： James W. McGinity , Thomas G. Gerding , Roland Bodmeier
IPC分类号： A61K8/63 , A61K9/02 , A61K9/06 , A61K31/135 , A61K31/138 , A61K31/16 , A61K31/167 , A61K31/57 , A61Q15/00 , A61Q19/00 , A61K7/32
CPC分类号： A61K31/135 , A61K31/138 , A61K31/167 , A61K31/573 , A61K8/0229 , A61K8/63 , A61K9/06 , A61Q15/00 , A61Q17/00 , A61Q19/00 , A61K2800/75 , Y10S514/817
摘要： Stick formulations for topical delivery of water soluble and/or water insoluble agents are disclosed. The stick formulations may contain steroids, antibiotics, antifungals, antihistamines anti inflammatories or local anesthetics. The vehicles comprise a combination of waxes and oils and a surfactant in embodiments involving water soluble agents. Methods for preparing the various stick formulations are also disclosed.
摘要翻译：公开了用于局部递送水溶性和/或水不溶性试剂的粘合剂制剂。棒剂可能含有类固醇，抗生素，抗真菌剂，抗组胺药物抗炎剂或局部麻醉剂。车辆包括蜡和油的组合以及涉及水溶性试剂的实施方案中的表面活性剂。还公开了制备各种棒剂制剂的方法。

9. 发明授权

US5116619A Vaginal progesterone tablet 失效
标题翻译：阴道孕酮片
公开(公告)号：US5116619A
公开(公告)日：1992-05-26
申请号：US238535
申请日：1988-08-30
申请人： John C. Greco , James W. McGinity
发明人： John C. Greco , James W. McGinity
IPC分类号： A61K9/00 , A61K31/57
CPC分类号： A61K31/57 , A61K9/0034 , Y10S514/843 , Y10S514/935 , Y10S514/967
摘要： A vaginal progesterone suppository is provided in the form of a tablet which delivers biologically effective amounts of progesterone for at least about 48 hours, and blood amounts above basal levels for 72 hours. The tablet is formulated to preferably have a hardness on its edge of 8-13 kg, and disintegrates from its surface to form a milky suspension in 6-8 hours after it is inserted in the vaginal vault. The tablet contains, by weight, about 13-20% progesterone, 65-85% lactose, 2-10% corn starch paste binder, 3-10% corn starch disintegrant, and 0.1-0.9% magnesium stearate as a lubricant. The ratio by weight of progesterone to lactose is preferably 1:6, and the ratio of starch paste binder to starch disintegrant is preferably 1:1. This dosage form is an effective treatment for many progesterone deficiency conditions, and provides enhanced bioavailability.
摘要翻译：提供阴道孕酮栓剂，其片剂形式将生物有效量的孕酮输送至少约48小时，血液量高于基础水平72小时。将片剂配制成优选具有8-13kg边缘的硬度，并且在将其插入阴道穹顶后6-8小时内从其表面分解形成乳状悬浮液。片剂含有约13-20％孕酮，65-85％乳糖，2-10％玉米淀粉糊粘合剂，3-10％玉米淀粉崩解剂和0.1-0.9％硬脂酸镁作为润滑剂。孕酮与乳糖的重量比优选为1:6，淀粉糊粘合剂与淀粉崩解剂的比例优选为1:1。该剂型是许多孕激素缺乏症的有效治疗方法，并提供增强的生物利用度。

10. 发明授权

US06169130A Method for improving the dispersion of redispersible polymer powders 失效
标题翻译：改善可再分散聚合物粉末分散性的方法
公开(公告)号：US06169130A
公开(公告)日：2001-01-02
申请号：US09316815
申请日：1999-05-21
申请人： Roland Bodmeier , James W. McGinity
发明人： Roland Bodmeier , James W. McGinity
IPC分类号： C08K716
CPC分类号： A61K9/5161 , A61K9/2866 , A61K9/2893 , C08J3/05 , C08J2301/08
摘要： The method according to the present invention includes the step of adding sufficient amounts of an alkalinizing agent to an aqueous solution into which a redispersible polymer powder will be dispersed or to an aqueous dispersion which will be dried to form a redispersible polymer powder. The method of the invention is particularly well suited for nonionic polymers. A surfactant, plasticizer and/or preservative can also be used in addition to the alkalinizing agent. Redispersible polymer powders processed according to the invention form acceptable tablet coatings which are comparable in quality to those coatings formed from aqueous polymer dispersions that have not been dried into redispersible polymer powders.
摘要翻译：根据本发明的方法包括向待分散的可再分散聚合物粉末的水溶液中加入足量的碱化剂或将其干燥以形成可再分散聚合物粉末的水分散体的步骤。本发明的方法特别适用于非离子聚合物。除了碱化剂之外，还可以使用表面活性剂，增塑剂和/或防腐剂。根据本发明加工的可再分散聚合物粉末形成可接受的片剂涂层，其质量与由尚未干燥成可再分散聚合物粉末的水性聚合物分散体形成的涂层相当。

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