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公开(公告)号：US5811388A
公开(公告)日：1998-09-22
申请号：US602611
申请日：1996-02-16
申请人： David R. Friend , David Wong
发明人： David R. Friend , David Wong
IPC分类号： A61K9/20 , A61K9/22 , A61K9/28 , A61K9/34 , A61K31/56 , A61K31/58 , A61K38/02 , A61K38/11 , A61K38/22 , A61K38/23 , A61K38/26 , A61K38/27 , A61K38/28 , A61K47/36 , A61P1/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61K9/24 , A61K9/36 , A61K38/00
CPC分类号： A61K31/573 , A61K31/58 , A61K31/606 , A61K9/205 , A61K9/2054 , A61K9/286 , Y10S514/96 , Y10S514/961
摘要： Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition is a unit dosage in the form of a tablet that comprises about 0.01% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.
摘要翻译： 描述了在口服给药组合物之后，将治疗有效量的药物口服递送至结肠而不显着释放上GI道中的药物组合物。 组合物是片剂形式的单位剂量，其包含可用于治疗结肠疾病或从结肠吸收的药物的约0.01重量％至约10重量％ 约40重量％至约98重量％的可从高等植物获得的水胶体胶; 和约2重量％至约50重量％的药学上可接受的粘合剂。 该组合物可用于通过向有需要的受试者施用合适的量来治疗人受试者中较低GI的紊乱。 特别优选的方面是制备片剂形式的这种组合物的方法。
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公开(公告)号：US6139865A
公开(公告)日：2000-10-31
申请号：US942094
申请日：1997-10-01
IPC分类号： C07D307/52 , A61K9/00 , A61K9/20 , A61K9/50 , A61K9/58 , A61K9/62 , A61K31/341 , A61K45/00 , A61K47/32 , A61K47/38 , B01J13/06
CPC分类号： A61K9/5026 , A61K31/341 , A61K9/5042 , A61K9/0007 , A61K9/2081 , Y10S514/937 , Y10S514/963 , Y10S514/974
摘要： A taste-masked microcapsule composition for administration of a drug is provided. The composition comprises microcapsules of drug and a substantially water-insoluble polymeric material, typically a cellulosic polymer. The microcapsule composition may be incorporated into any number of pharmaceutical formulations, including chewable tablets, effervescent tablets, powders, liquid dispersions, and the like. A method for masking the taste of drugs is also provided, involving a phase separation coacervation technique in which drug is coated with relatively high levels of a polymeric material. These high coating levels give rise to effective taste masking, while nevertheless allowing targeted release of drug, so that the drug is released shortly after passage through the mouth.
摘要翻译： 提供了用于给药药物的掩味微胶囊组合物。 组合物包含药物的微胶囊和基本上不溶于水的聚合物材料，通常为纤维素聚合物。 微胶囊组合物可以并入任何数量的药物制剂中，包括咀嚼片，泡腾片，粉末，液体分散体等。 还提供了掩蔽药物味道的方法，其涉及相分离凝聚技术，其中用相当高水平的聚合物材料涂覆药物。 这些高涂层水平产生有效的掩味，同时允许药物的靶向释放，使得药物在通过口腔后不久释放。
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公开(公告)号：US5656294A
公开(公告)日：1997-08-12
申请号：US486974
申请日：1995-06-07
申请人： David R. Friend , David Wong
发明人： David R. Friend , David Wong
CPC分类号： A61K31/573 , A61K31/58 , A61K31/606 , A61K9/205 , A61K9/2054 , A61K9/286
摘要： Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition comprises about 0.5% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 80% by weight of a hydrocolloid gum obtainable from higher plants; and about 10% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating colon disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.
摘要翻译： 描述了在口服给药组合物之后，将治疗有效量的药物口服递送至结肠而不显着释放上GI道中的药物组合物。 该组合物包含约0.5重量％至约10重量％的可用于治疗结肠疾病或从结肠吸收的药物; 约40重量％至约80重量％的可从高等植物获得的水胶体胶; 和约10重量％至约50重量％的药学上可接受的粘合剂。 通过向有需要的受试者施用合适的量，该组合物可用于治疗人类受试者的结肠疾病。 特别优选的方面是制备片剂形式的这种组合物的方法。
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公开(公告)号：US06355270B1
公开(公告)日：2002-03-12
申请号：US09479389
申请日：2000-01-06
IPC分类号： A61K914
CPC分类号： G03F7/00 , A61K9/0097 , A61K9/1676 , A61K9/1694 , A61K9/4891
摘要： Microfabricated, asymmetrical, reservoir-containing particles for use in the oral delivery of biopolymer therapeutic agents such as peptides, proteins and oligonucleotides are disclosed. The particles are encapsulated in enteric-coated capsules or tablets to provide passage through the stomach and release of a suspension of the particles in the intestinal lumen. The particles have a selected shape, and uniform dimensions preferably in the 100 &mgr;m to 1 mm range. The reservoirs open to the face of the particle and are filled with a therapeutic agent and selected excipients. The excipients are selected to delay the dissolution/release of the agent from the particle reservoirs for 5-60 minutes after the particle is released in the intestinal lumen. Alternatively, the pore is plugged with an erodable material. The face of the particle is grafted with a layer of muco-adhesive ligands designed to quickly bind the particle to the intestinal mucosa for several minutes to several hours after release of the particles from the enteric-coated carrier.
摘要翻译： 公开了用于生物聚合物治疗剂例如肽，蛋白质和寡核苷酸的口服递送的微制造的，不对称的，含储层的颗粒。 将颗粒包封在肠溶衣胶囊或片剂中以提供穿过胃的通道并释放颗粒在肠腔中的悬浮液。 颗粒具有选定的形状，并且尺寸均匀，优选在100μm至1mm范围内。 储存器对颗粒的表面开放并填充有治疗剂和选定的赋形剂。 选择赋形剂以在颗粒在肠腔中释放后延迟药剂从颗粒储存器中溶解/释放5-60分钟。 或者，孔被可侵蚀的材料堵塞。 该颗粒的表面用一层粘膜 - 粘合剂配体接枝，其设计用于在从肠溶衣载体上释放颗粒之后将颗粒快速结合至肠粘膜数分钟至数小时。
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公开(公告)号：US6063402A
公开(公告)日：2000-05-16
申请号：US487605
申请日：1995-06-07
CPC分类号： A61K9/205 , C08B37/0087 , C08L5/14
摘要： Disclosed is a substantially anhydrous, powdered, galactomannan composition consisting essentially of a galactomannan hydrocolloid exhibiting about 50% to about 90% by weight of anhydromannose residues and about 10% to about 50% by weight anhydrogalactose residues; less than about 1% by weight of protein material and less than about 3% of other nonaqueous impurities. This material is useful for preparing pharmaceutical compositions both in the substantially anhydrous form but preferably in an anhydrated form which includes about 5-15% by weight water. The pharmaceutical compositions comprise a therapeutically effective amount of a drug, the hydrated powered gallactomannan composition and optionally other pharmaceutically-acceptable excipients. When the hydrated powdered purified glactomannan of the invention is used to form a tablet, one sees improved hardness in the tablet formed. The pharmaceutical composition of the invention is particularly valuable for delivering a therapeutically effective drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition. Unique means to prepare the purified galactomannan in large quantities is provided.
摘要翻译： 公开了基本上无水的，粉状的半乳甘露聚糖组合物，其基本上由显示约50重量％至约90重量％的脱水甘露糖残基和约10重量％至约50重量％的半脱水半乳糖残基的半乳甘露聚糖水胶体组成; 小于约1重量％的蛋白质材料和小于约3％的其它非水性杂质。 该材料可用于制备基本上无水形式的药物组合物，但优选以包含约5-15重量％水的脱水形式。 药物组合物包含治疗有效量的药物，水合动力的甘蔗聚糖组合物和任选的其它药学上可接受的赋形剂。 当使用本发明的水合粉末状纯化甘蓝聚糖来形成片剂时，可以看出形成的片剂的硬度提高。 本发明的药物组合物对于在口服给药组合物之后将治疗有效的药物递送至结肠而不会在上GI道中显着释放药物是特别有价值的。 提供了大量制备纯化的半乳甘露聚糖的独特手段。
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6.发明授权NSADI delivery employing a powdered hydrocolloid gum obtainable from higher plants 失效使用可从高等植物获得的粉状水胶体胶的NSADI递送
公开(公告)号：US5993860A
公开(公告)日：1999-11-30
申请号：US969810
申请日：1997-11-13
IPC分类号： A61K9/20 , A61K31/192 , A61K9/16 , A61K47/30 , A61K47/36
CPC分类号： A61K31/616 , A61K31/192 , A61K9/205 , Y10S514/922 , Y10S514/951 , Y10S514/96 , Y10S514/974
摘要： An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.
摘要翻译： 一种口服递送药物组合物，其用于降低哺乳动物上GI肠道中的NSAID的胃刺激作用。 组合物包括（a）可从高等植物获得的粘膜保护量的药学可接受的水胶体胶，（b）分散增强量的另一赋形剂和（c）治疗有效量的NSAID。 还公开了制备该组合物的方法和通过施用该组合物来降低NSAID的胃刺激作用的方法。 此外，公开了特别可用于制备水性悬浮液的组合物。
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7.发明授权
公开(公告)号：US5112541A
公开(公告)日：1992-05-12
申请号：US150056
申请日：1988-01-29
申请人： David R. Friend
发明人： David R. Friend
IPC分类号： B01J13/18 , C10M171/06 , C10N20/06 , C10N50/00 , C10N70/00
CPC分类号： B01J13/18
摘要： Microencapsulating lubricating fluids and additives and a method of preparing microencapsulated lubricants including the steps of preparing an emulsification medium, adding a lubricant to the emulsification medium, emulsifying the emulsification medium and lubricant to form an emulsion, adding a first solution including resorcinol and dimethylol urea to the emulsion, acidifying the first solution and emulsion, adding a second solution consisting of resorcinol and dimethylol urea to the acidified first solution and emulsion while vigorously stirring it to form a microcapsule suspension, adjusting the pH to be basic, filtering and washing the microcapsule suspension to separate the microcapsules from the solution, and drying the microcapsules.
摘要翻译： 微胶囊化润滑液和添加剂以及制备微胶囊化润滑剂的方法，包括以下步骤：制备乳化介质，向乳化介质中加入润滑剂，乳化乳化介质和润滑剂以形成乳液，将包括间苯二酚和二羟甲基脲的第一溶液加入到 乳液，酸化第一溶液和乳液，向酸化的第一溶液和乳液中加入由间苯二酚和二羟甲基脲组成的第二溶液，同时剧烈搅拌形成微胶囊悬浮液，将pH调节至碱性，过滤和洗涤微胶囊悬浮液 将微胶囊与溶液分离，并干燥微胶囊。
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公开(公告)号：US5091122A
公开(公告)日：1992-02-25
申请号：US173071
申请日：1988-03-24
申请人： David R. Friend
发明人： David R. Friend
CPC分类号： B01J13/14 , B01J13/043 , Y10T428/2987
摘要： A method of preparing microencapsulated basic solutions including the steps of preparing a polymer which is hydrophobic at high pH values, preparing a basic solution, dissolving the polymer in an organic solvent, adding a surfactant to the polymer solution, adding the basic solution to the dissolved polymer, emulsifying the basic solution and dissolved polymer and spray drying the emulsion while stirring the emulsion.
摘要翻译： 一种制备微胶囊化碱性溶液的方法，包括制备在高pH值下为疏水性的聚合物的步骤，制备碱性溶液，将聚合物溶解在有机溶剂中，向聚合物溶液中加入表面活性剂，将碱溶液加入到溶解的 聚合物，乳化碱性溶液和溶解的聚合物，并在搅拌乳液的同时喷雾干燥乳液。
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公开(公告)号：US5238933A
公开(公告)日：1993-08-24
申请号：US862387
申请日：1992-04-02
CPC分类号： A61K9/7084 , A61K47/10 , A61K47/14 , A61K9/0014 , Y10S514/947
摘要： Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a lower aliphatic ester of a lower aliphatic carboxylic acid such as ethyl acetate and a lower alkanol such as propylene glycol. Methods and transdermal drug delivery systems for using the compositions are also provided.
摘要翻译： 提供了皮肤渗透增强剂组合物，其增加皮肤对透皮给药的药理学活性剂的渗透性。 组合物含有低级脂族羧酸的低级脂族酯，如乙酸乙酯和低级链烷醇如丙二醇。 还提供了用于使用组合物的方法和透皮药物递送系统。
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