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21. 发明授权

US5874418A Sulfoalkyl ether cyclodextrin based solid pharmaceutical formulations and their use 失效
标题翻译：基于磺基烷基醚环糊精的固体药物制剂及其用途
公开(公告)号：US5874418A
公开(公告)日：1999-02-23
申请号：US851006
申请日：1997-05-05
申请人： Valentino Stella , Roger A. Rajewski , James W. McGinity
发明人： Valentino Stella , Roger A. Rajewski , James W. McGinity
IPC分类号： A61K9/20 , A61K9/28 , A61K47/40 , C08B37/16 , A61K31/735 , C07H13/12
CPC分类号： A61K47/40 , A61K9/205 , A61K9/2846 , A61K9/2866 , Y10S514/964 , Y10S514/965
摘要： Sulfoalkyl ether-cyclodextrin (SAE-CD) based pharmaceutical formulations are provided by the present invention. These formulations comprise SAE-CD derivatives and a therapeutic agent, a major portion of which is not complexed to the SAE-CD. The present formulations are advantageously easier to prepare than other SAE-CD based formulations in the art yet provide similar or improved effectiveness. The SAE-CD derivative can be used to modify the bioavailability and/or rate of bioabsorption of therapeutic agents.
摘要翻译：基于磺基烷基醚 - 环糊精（SAE-CD）的药物制剂由本发明提供。这些制剂包含SAE-CD衍生物和治疗剂，其主要部分不与SAE-CD复合。本发明的制剂有利地比本领域中其他基于SAE-CD的制剂更容易制备，但提供相似或改进的效果。 SAE-CD衍生物可用于改变治疗剂的生物利用度和/或生物吸收速率。

22. 发明授权

US5622993A Stick formulations for topical drug delivery of therapeutic agents and uses thereof 失效
公开(公告)号：US5622993A
公开(公告)日：1997-04-22
申请号：US523084
申请日：1995-09-01
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
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.

23. 发明授权

US5288502A Preparation and uses of multi-phase microspheres 失效
标题翻译：多相微球的制备与应用
公开(公告)号：US5288502A
公开(公告)日：1994-02-22
申请号：US779173
申请日：1991-10-16
申请人： James W. McGinity , Motokazu Iwata
发明人： James W. McGinity , Motokazu Iwata
IPC分类号： A61K9/16 , A61K9/50 , A61K31/135 , A61K31/165 , A61K31/54 , A61K38/00 , A61K38/04 , A61K38/21 , A61K38/22 , A61K38/44 , A61K38/46 , A61K39/00 , A61K47/30 , A61K9/14 , B32B5/16
CPC分类号： A61K9/1694 , A61K9/1647 , A61K9/5031 , A61K9/5089 , Y10T428/2984 , Y10T428/2985 , Y10T428/2987
摘要： Multi-phase polymeric microspheres containing a molecular compound dispersed in a polymeric matrix are described. Methods for preparing the multi-phase microspheres are also described, which includes a multiple emulsion solvent evaporation technique. Drug loading efficiencies between 80 to 100% were achieved using the described methods. Particular ratios of the W/O emulsion to polymer, and concentration of surfactant and dispersion media (mineral oil) provide highly efficient multi-phase microspheres. In particular embodiments, the multi-phase microspheres feature a high loading efficiency of water-soluble drugs, and also eliminates partitioning of the water soluble agent into the polymer acetonitrile (solvent) phase, thus preventing low encapsulation efficiency. The described multi-phase microspheres possess efficient drug loading, release properties, and drug stability, and also provide a vehicle for long term therapeutic release of a biologically active molecule for therapeutically effective periods of time. Molecular compounds which may be incorporated within the multi-phase microspheres include both water-soluble and water-insoluble drugs, proteins (e.g. TNF), peptides, and chemicals. The molecular compound is protected within an oily droplet, and contact with polymer, surfactant, organic solvents, and other potentially denaturing agents is prevented.
摘要翻译：描述了分散在聚合物基质中的分子化合物的多相聚合物微球。还描述了制备多相微球的方法，其包括多重乳液溶剂蒸发技术。使用所述方法实现了80至100％之间的药物负载效率。 W / O乳液与聚合物的比例以及表面活性剂和分散介质（矿物油）的浓度提供了高效的多相微球。在具体实施方案中，多相微球体具有高的水溶性药物的负载效率，并且还消除了水溶性剂分解成聚合物乙腈（溶剂）相，从而防止低的包封效率。所描述的多相微球具有有效的药物加载，释放性质和药物稳定性，并且还提供用于治疗有效时间段的生物活性分子的长期治疗性释放的载体。可以掺入多相微球体的分子化合物包括水溶性和水不溶性药物，蛋白质（例如TNF），肽和化学物质。分子化合物在油滴中被保护，并且防止与聚合物，表面活性剂，有机溶剂和其它潜在的变性剂接触。

24. 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。

25. 发明授权

US4646730A Color stabilized hydrogel dressing and process 失效
标题翻译：颜色稳定的水凝胶敷料和工艺
公开(公告)号：US4646730A
公开(公告)日：1987-03-03
申请号：US866541
申请日：1986-05-23
申请人： Edward Schonfeld , James W. McGinity
发明人： Edward Schonfeld , James W. McGinity
IPC分类号： A61K9/70 , A61K47/00 , A61K47/32 , A61L26/00 , A61L15/00
CPC分类号： A61L26/008 , A61L26/0014 , A61L26/0066 , A61L2300/104 , A61L2300/404
摘要： A polyvinylpyrrolidone(PVP)/Silver Sulfadiazine (SSD) hydrogel dressing in which the gel is formed by the use of electron beam (E-Beam) radiation to cross-link the polyvinylpyrrolidone (PVP); in which the color of the hydrogel dressing has been stabilized by the addition thereto of magnesium trisilicate and, optionally but preferably, also hydrogen peroxide and/or polyacrylic acid is disclosed; and also the process of stabilizing the color by adding magnesium trisilicate, to a water dispersion of PVP and SSD before it is exposed to E-Beam radiation is disclosed.
摘要翻译：聚乙烯吡咯烷酮（PVP）/磺胺二嗪（SSD）水凝胶敷料，其中通过使用电子束（E-Beam）辐射形成凝胶以交联聚乙烯吡咯烷酮（PVP）; 其中水凝胶敷料的颜色已经通过加入三硅酸镁而稳定，并且任选但优选也公开了过氧化氢和/或聚丙烯酸; 并且还公开了在暴露于E-Beam辐射之前，通过加入三硅酸镁将PVP和SSD的水分散体稳定的过程。

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